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   2015| October-December  | Volume 11 | Issue 44  
    Online since September 16, 2015

 
 
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ORIGINAL ARTICLES
Curcumin attenuates chronic ethanol-induced liver injury by inhibition of oxidative stress via mitogen-activated protein kinase/nuclear factor E2-related factor 2 pathway in mice
Zhang E Xiong, Wei Guo Dong, Bao Ying Wang, Qiao Yun Tong, Zhong Yan Li
October-December 2015, 11(44):707-715
DOI:10.4103/0973-1296.165556  PMID:26600714
Objective: This study aimed to investigate the protective effect of curcumin on chronic ethanol-induced liver injury in mice and to explore its underlying mechanisms. Materials and Methods: Ethanol-exposed Balb/c mice were simultaneously treated with curcumin for 6 weeks. Liver injury was evaluated by biochemical and histopathological examination. Lipid peroxidation and anti-oxidant activities were measured by spectrophotometric method. Anti-oxidative genes expression such as NAD(P)H quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and superoxide dismutase (SOD) were determined by real-time polymerase chain reaction. The nuclear factor E2-related factor 2 (Nrf2) and the phosphorylation states of specific proteins central to intracellular signaling cascades were measured by western blotting. Results: Curcumin treatment protected liver from chronic ethanol-induced injury through reducing serum alanine aminotransferase and aspartate aminotransferase activities, improving liver histological architecture, and reversing lipid disorders indicated by decrease of triglyceride, total cholesterol and low-density lipoprotein-cholesterol levels and increase of High-density lipoprotein-cholesterol levels. Meanwhile, curcumin administration attenuated oxidative stress via up-regulating SOD and glutathione peroxidase activities, leading to a reduction of lipid hydroperoxide production. In addition, curcumin increased Nrf2 activation and anti-oxidative genes expressions such as NQO1, HO-1, and SOD through inducing extracellular signal-regulated kinase (ERK) and p38 phosphorylation. Conclusion: Our data suggested that curcumin protected the liver from chronic-ethanol induced injury through attenuating oxidative stress, at least partially, through ERK/p38/Nrf2-mediated anti-oxidant signaling pathways.
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Pharmacokinetics, intestinal absorption and microbial metabolism of single platycodin D in comparison to Platycodi radix extract
Jinjun Shan, Jiashuang Zou, Tong Xie, An Kang, Wei Zhou, Haishan Deng, Yancao Mao, Liuqing Di, Shouchuan Wang
October-December 2015, 11(44):750-755
DOI:10.4103/0973-1296.165576  PMID:26600720
Background: Platycodi radix, the dried root of Platycodon grandiflorum A. DC, has been widely used as food and herb medicine for treating cough, cold and other respiratory ailments, and platycodin D (PD) is one of the most important compounds in Platycodi Radix. Objective: The purpose of this study was to compare the pharmacokinetic characteristics, intestinal absorption and microbial metabolism of PD in monomer with that in Platycodi radix extract (PRE). Materials and Methods: In the pharmacokinetic study, the concentrations of PD in rat plasma were determined by ultra-performance liquid chromatography-tandem mass spectrometry and the main pharmacokinetic parameters were calculated by data analysis software (DAS). Besides, in vitro Caco-2 cells and fecal lysate were performed to investigate the intestinal absorption and metabolism, respectively. Results: The results from pharmacokinetics showed that the area under the curve, the peak concentration the time to reach peak concentration and mean residence time of PD in PRE were enhanced significantly compared with that in single PD. Caco-2 cells transport study indicated that the absorption of PD both in monomer and in PRE were poor owning that the permeability of PD were <1/10 6 cm/s. The hydrolysis degree of PD in PRE was significantly lower than that in monomer PD in fecal lysate, which might be illustrated by the other ingredients in PRE influenced the hydrolysis of PD via gut microbiota. Conclusion: These findings indicated that the difference of microbial metabolism, not apparent absorption in intestine for PD between in monomer and in PRE contributed to their pharmacokinetic difference.
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Effects of the main active components combinations of Astragalus and Panax notoginseng on energy metabolism in brain tissues after cerebral ischemia-reperfusion in mice
Xiao-Ping Huang, Huang Ding, Bei Wang, Yong-Yuan Qiu, Ying-Hong Tang, Rong Zeng, Chang-Qing Deng
October-December 2015, 11(44):732-739
DOI:10.4103/0973-1296.165572  PMID:26600717
Background: Astragalus and Panax notoginseng are traditional Chinese medicines used for the treatments of cardio-cerebrovascular ischemic diseases, astragaloside IV (AST IV) and ginsenoside Rg1 (Rg1), ginsenoside Rb1 (Rb1), notoginsenoside R1 (R1) are their active components. Objective: The purpose of this work was to investigate the effect of AST IV combined with Rg1, Rb1, R1 on energy metabolism in brain tissues after cerebral ischemia-reperfusion in mice. Materials and Methods: C57BL/6 mice were randomly divided into 11 groups, treated for 3 days. At 1 h after the last administration, the model of cerebral ischemia-reperfusion injury was established, and brain tissues were detected. Results: All drugs increased the contents of adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP) and the level of total adenine nucleotides (TAN), the combinations increased energy charge (EC), the effects of four active components combination were better. The phosphorylation of AMP-activated protein kinaseα1/2 (p-AMPKα1/2) was increased in AST IV, R1, four active components combination, AST IV + Rg1 and AST IV + R1 groups, the increased effect of four active components combination was greater than that of the active components alone and AST IV + Rb1. All drugs increased glucose transporter 3 (GLUT3) mRNA and protein, and the increases of four active components combination were more obvious than those of the active components alone or some two active components combinations. Conclusion: Four active components combination of Astragalus and P. notoginseng have the potentiation on improving of energy metabolism, the mechanism underlying might be associated with promoting the activation of AMPKα1/2, enhancing the expression of GLUT3, thus mediating glucose into nerve cells, increasing the supply and intake of glucose.
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Xanthohumol induces apoptosis and S phase cell cycle arrest in A549 non-small cell lung cancer cells
Wai Kuan Yong, Yen Fong Ho, Sri Nurestri Abd Malek
October 2015, 11(44):275-283
DOI:10.4103/0973-1296.166069  PMID:26664015
Background: Xanthohumol, a major prenylated chalcone found in female hop plant, Humulus lupulus, was reported to have various chemopreventive and anti-cancer properties. However, its apoptotic effect on human alveolar adenocarcinoma cell line (A549) of non-small cell lung cancer (NSCLC) was unknown. Objective: This study aimed to investigate the effects of xanthohumol on apoptosis in A549 human NSCLC cells. Materials and Methods: A549 cell proliferation was determined by sulforhodamine B assay. Morphological changes of the cells were studied via phase contrast and fluorescent microscopy. Induction of apoptosis was assessed by Annexin-V fluorescein isothiocyanate/propidium iodide (Annexin V-FITC/PI ) staining, DNA fragmentation (TUNEL) assay mitochondrial membrane potential assay, cell cycle analysis, and caspase activity studies. Results: Xanthohumol was found to decrease cell proliferation in A549 cells but had relatively low cytotoxicity on normal human lung fibroblast cell line (MRC-5). Typical cellular and nuclear apoptotic features were also observed in A549 cells treated with xanthohumol. Onset of apoptosis in A549 cells was further confirmed by externalization of phosphatidylserine, changes in mitochondrial membrane potential, and DNA fragmentation in the cells after treatment. Xanthohumol induced accumulation of cells in sub G1 and S phase based on cell cycle analysis and also increased the activities of caspase-3, -8, and -9. Conclusion: This work suggests that xanthohumol as an apoptosis inducer, may be a potent therapeutic compound for NSCLC.
  3 1,947 15
Neuroprotective effect of Citrus unshiu immature peel and nobiletin inhibiting hydrogen peroxide-induced oxidative stress in HT22 murine hippocampal neuronal cells
Hyun Woo Cho, Su Young Jung, Gyeong Hwan Lee, Jung Hee Cho, In Young Choi
October 2015, 11(44):284-289
DOI:10.4103/0973-1296.166047  PMID:26664016
Background: Oxidative stress-induced cell damage is common in the etiology of several neurobiological disorders, including Alzheimer's disease and Parkinson's disease. In a case study, nobiletin-rich Citrus reticulata peels could prevent the progression of cognitive impairment in donepezil-preadministered Alzheimer's disease patients. Objective: In this study, we investigated the effects and underlying mechanism of nobiletin and Citrus unshiu immature peel (CUIP) water extract, which contains nobiletin as a major compound, on hydrogen peroxide-induced oxidative stress in HT22 cells, a murine hippocampal neuronal model. Materials and Methods: HT22 cells were treated with hydrogen peroxide in the presence or absence of various concentrations of CUIP and nobiletin. Cytotoxicity and apoptotic protein levels were measured by 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay and Western blotting. Results: Pretreatment with CUIP and nobiletin inhibited cell death due to hydrogen peroxide. Hydrogen peroxide-induced the expression of phospho-Jun N-terminal kinases (p-JNK) and p-p38 proteins in HT22 cells; however CUIP and nobiletin suppressed p-JNK and p-p38 without changing JNK or p38. Regarding apoptosis, caspase 3, B-cell lymphoma 2 (Bcl-2), and Bax protein expression was determined. CUIP and nobiletin suppressed caspase 3 and Bax expression, but they induced Bcl-2 expression in HT22 cells. Conclusion: These results show that CUIP and nobiletin can protect against hydrogen peroxide-induced cell death in HT22 neurons via mitogen-activated protein kinases and apoptotic pathways.
  3 1,584 16
Bioactive extract from moringa oleifera inhibits the pro-inflammatory mediators in lipopolysaccharide stimulated macrophages
Masoumeh Tangestani Fard, Palanisamy Arulselvan, Govindarajan Karthivashan, Siti Khadijah Adam, Sharida Fakurazi
December 2015, 11(44):556-563
DOI:10.4103/0973-1296.172961  PMID:27013794
Introduction: Inflammation is a well-known physiological response to protect the body against infection and restore tissue injury. Nevertheless, the chronic inflammation can trigger various inflammatory associated diseases/disorder. Moringa oleifera is a widely grown plant in most tropical countries and it has been recognized traditionally for several medicinal benefits. Objectives: The objective of this study was to investigate the anti-inflammatory properties of M. oleifera extract on lipopolysaccharide (LPS) - stimulated macrophages. Materials and Methods: The anti-inflammatory effect of M. oleifera hydroethanolic bioactive leaves extracts was evaluated by assessing the inhibition of nitric oxide (NO) production during Griess reaction and the expression of pro-inflammatory mediators in macrophages. Results: Interestingly, we found that M. oleifera hydroethanolic bioactive leaves extract significantly inhibited the secretion of NO production and other inflammatory markers such as prostaglandin E 2 , tumor necrosis factor alpha, interleukin (IL)-6, and IL-1b. Meanwhile, the bioactive extract has induced the production of IL-10 in a dose-dependent manner. In addition, M. oleifera hydroethanolic bioactive leaves extract effectively suppressed the protein expression of inflammatory markers inducible NO synthase, cyclooxygenase-2, and nuclear factor kappa-light-chain-enhancer of activated B-cells p65 in LPS-induced RAW264.7 macrophages in a dose-dependent manner. Conclusion: These findings support the traditional use of M. oleifera plant as an effective treatment for inflammation associated diseases/disorders.
  3 2,208 21
Identification of a herbal powder by deoxyribonucleic acid barcoding and structural analyses
Bhavisha P Sheth, Vrinda S Thaker
December 2015, 11(44):570-574
DOI:10.4103/0973-1296.172963  PMID:27013796
Background: Authentic identification of plants is essential for exploiting their medicinal properties as well as to stop the adulteration and malpractices with the trade of the same. Objective: To identify a herbal powder obtained from a herbalist in the local vicinity of Rajkot, Gujarat, using deoxyribonucleic acid (DNA) barcoding and molecular tools. Materials and Methods: The DNA was extracted from a herbal powder and selected Cassia species, followed by the polymerase chain reaction (PCR) and sequencing of the rbcL barcode locus. Thereafter the sequences were subjected to National Center for Biotechnology Information (NCBI) basic local alignment search tool (BLAST) analysis, followed by the protein three-dimension structure determination of the rbcL protein from the herbal powder and Cassia species namely Cassia fistula, Cassia tora and Cassia javanica (sequences obtained in the present study), Cassia Roxburghii, and Cassia abbreviata (sequences retrieved from Genbank). Further, the multiple and pairwise structural alignment were carried out in order to identify the herbal powder. Results: The nucleotide sequences obtained from the selected species of Cassia were submitted to Genbank (Accession No. JX141397, JX141405, JX141420). The NCBI BLAST analysis of the rbcL protein from the herbal powder showed an equal sequence similarity (with reference to different parameters like E value, maximum identity, total score, query coverage) to C. javanica and C. roxburghii. In order to solve the ambiguities of the BLAST result, a protein structural approach was implemented. The protein homology models obtained in the present study were submitted to the protein model database (PM0079748-PM0079753). The pairwise structural alignment of the herbal powder (as template) and C. javanica and C. roxburghii (as targets individually) revealed a close similarity of the herbal powder with C. javanica. Conclusion: A strategy as used here, incorporating the integrated use of DNA barcoding and protein structural analyses could be adopted, as a novel rapid and economic procedure, especially in cases when protein coding loci are considered.
  2 1,380 17
Antihyperglycemic effect of thymoquinone and oleuropein, on streptozotocin-induced diabetes mellitus in experimental animals
Sibghatullah Muhammad Ali Sangi, Mansour Ibrahim Sulaiman, Mohammed Fawzy Abd El-wahab, Elsamoual Ibrahim Ahmedani, Soad Shaker Ali
October 2015, 11(44):251-257
DOI:10.4103/0973-1296.166017  PMID:26664013
Background: Diabetes mellitus is one of the most important diseases related with endocrines. Its main manifestation includes abnormal metabolism of carbohydrates and lipids and inappropriate hyperglycemia that is caused by absolute or relative insulin deficiency. It affects humankind worldwide. Objectives: Our research was aimed to observe antihyperglycemic activity of thymoquinone and oleuropein. Materials and Methods: In this study, rats were divided into six groups, 6 rats in each. Diabetes was inducted by streptozotocin (STZ). The level of fasting blood glucose was determined for each rats during the experiment, doses of thymoquinone and oleuropein (3 mg/kg and 5 mg/kg) for both, were injected intraperitoneal. Pancreatic tissues were investigated to compare β-cells in diabetic and treated rats. Result and Conclusion: It was found that thymoquinone and oleuropein significantly decrease serum Glucose levels in STZ induced diabetic rats.
  2 2,870 16
Apoptosis of AGS human gastric adenocarcinoma cells by methanolic extract of Dictamnus
Hyun Soo Park, Noo Ri Hong, Tae Seok Ahn, Hyungwoo Kim, Myeong Ho Jung, Byung Joo Kim
October 2015, 11(44):329-336
DOI:10.4103/0973-1296.165994  PMID:26664023
Background: The root bark of Dictamnus dasycarpusTurcz has traditionally been used in East Asia to treat skin diseases such as eczema, atopic dermatitis, and psoriasis. However, it has also been reported to exhibit an anti-proliferative effect on cancer cells. Objective: To investigate the anti-cancer effects of a methanol extract of Dictamnus dasycarpusroot bark (MEDD) on AGS cells (a human gastric adenocarcinoma cell-line). Materials and Methods: An 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium assay, a caspase activity assay, cell cycle analysis, mitochondrial membrane potential (MMP) measurements, and western blotting were used to investigate the anti-cancer effects of MEDD on AGS cells. Results: Treatment with MEDD significantly and concentration-dependently inhibited AGS cell growth. MEDD treatment in AGS cells led to increased accumulation of apoptotic sub-G1 phase cells in a concentration-dependent manner. Also, MEDD reduced the expressions of pro-caspase-3, -8 and -9, and increased the active form of caspase-3. Furthermore, subsequent Western blotting revealed elevated levels of poly (ADP-ribose) polymerase protein. MEDD treatment reduced levels of MMP and anti-apoptotic Bcl-2 and Bcl-xL proteins. Pretreatment with SB203580 (a specific inhibitor of p38 mitogen-activated protein kinases), SP600125 (a potent inhibitor of C-Jun N-terminal kinases), or PD98059 (a potent inhibitor of extracellular signal-regulated kinases) did not modify the effects of MEDD treatment. However, pretreatment with LY294002 (a specific inhibitor of Akt) significantly enhanced MEDD-induced cell death. Conclusion: These results suggest that MEDD-mediated cell death is associated with the intrinsic apoptotic pathway and that inhibition of Akt signaling contributes to apoptosis induction by MEDD.
  2 1,396 15
Effects of 4-hydroxyisoleucine from fenugreek seeds on depression-like behavior in socially isolated olfactory bulbectomized rats
Padmaja B Kalshetti, Ramesh Alluri, Vishwaraman Mohan, Prasad Arvind Thakurdesai
October 2015, 11(44):388-396
DOI:10.4103/0973-1296.168980  PMID:26929572
Context: Antidepressant-like effects of (2S, 3R, 4S)-4-hydroxyisoleucine (4-HI), a major amino acid from fenugreek seeds, has been reported in the animal model of acute depression. Aims: To evaluate effects of subacute administration of 4-HI in animal model of stress-induced depression namely socially isolated olfactory bulbectomized rats. Materials and Methods: Bilateral olfactory bulbectomy (OBX) were induced in 30 Sprague-Dawley rats. After recovery period of 14 days, rats were randomized into five groups of 6 rats each and stressed with social isolation (individual housing). The rats were orally treated with either vehicle (OBX-Iso), positive control, fluoxetine (30 mg/kg) or 4-HI (10, 30, 100 mg/kg) once a day from day 14 onward. Separate group of rats with social isolation but without OBX (Sham-Iso) was also maintained. The behavioral depression and anxiety related parameters using open field test (OFT), sucrose intake test, novelty suppressed feeding (NSF) and forced swim test (FST), and neurochemical estimation (brain monoamines viz., serotonin and nor-adrenaline, serotonin turnover, and serum cortisol) were performed. Statistical Analysis Used: Data was analyzed by either two-way ANOVA (OFT and FST) or one-way ANOVA (sucrose intake test, NSF, and neurochemical estimation) followed by Dunnett's multiple comparisons test. Differences were considered significant at P < 0.05. Results: The significant and dose-dependent protection from behavioral and neurochemical changes were observed in 4-HI co-administrated OBX-Iso rats. Conclusion: 4-HI demonstrated the antidepressant and antianxiety effects in socially isolated stress-induced OBX rats with possible involvement of multiple stress relieving mechanisms.
  2 1,722 16
Ultraviolet-B protective effect of flavonoids from Eugenia caryophylata on human dermal fibroblast cells
Juilee Patwardhan, Purvi Bhatt
October 2015, 11(44):397-406
DOI:10.4103/0973-1296.168979  PMID:26929573
Background: The exposure of skin to ultraviolet-B (UV-B) radiations leads to deoxyribonucleic acid (DNA) damage and can induce production of free radicals which imbalance the redox status of the cell and lead to increased oxidative stress. Clove has been traditionally used for its analgesic, anti-inflammatory, anti-microbial, anti-viral, and antiseptic effects. Objective: To evaluate the UV-B protective activity of flavonoids from Eugenia caryophylata (clove) buds on human dermal fibroblast cells. Materials and Methods: Protective ability of flavonoid-enriched (FE) fraction of clove was studied against UV-B induced cytotoxicity, anti-oxidant regulation, oxidative DNA damage, intracellular reactive oxygen species (ROS) generation, apoptotic morphological changes, and regulation of heme oxygenase-1 (HO-1) gene through nuclear factor E2-related factor 2 antioxidant response element (Nrf2 ARE) pathway. Results: FE fraction showed a significant antioxidant potential. Pretreatment of cells with FE fraction (10–40 μg/ml) reversed the effects of UV-B induced cytotoxicity, depletion of endogenous enzymatic antioxidants, oxidative DNA damage, intracellular ROS production, apoptotic changes, and overexpression of Nrf2 and HO-1. Conclusion: The present study demonstrated for the first time that the FE fraction from clove could confer UV-B protection probably through the Nrf2-ARE pathway, which included the down-regulation of Nrf2 and HO-1. These findings suggested that the flavonoids from clove could potentially be considered as UV-B protectants and can be explored further for its topical application to the area of the skin requiring protection.
  2 2,235 18
Toxicological evaluation of Emblica officinalis fruit extract and its anti-inflammatory and free radical scavenging properties
Sushil Kumar Middha, Arvind Kumar Goyal, Prakash Lokesh, Varsha Yardi, Lavanya Mojamdar, Deepthi Sudhir Keni, Dinesh Babu, Talambedu Usha
October 2015, 11(44):427-433
DOI:10.4103/0973-1296.168982  PMID:26929577
Background: Emblica officinalis (Euphorbiaceae), popularly known as Indian gooseberry or "Amla" in India, is used in Ayurveda as "rejuvenating herb" since ancient times. Objective: This study was carried out to estimate toxicity, anti-inflammatory, and antioxidative activities of the methanolic extract of Emblica officinalis fruit (MEO) in an animal model. Materials and Methods: Antioxidative property of MEO was assessed by in vitro assays such as phosphomolybdenum assay (total antioxidant capacity), free radical scavenging assays 1,1-diphenyl-2-picrylhydrazyl and 2,2'-azino-bis and 3-ethylbenzthiazoline-6-sulphonic acid (DPPH and ABTS method) and lipid peroxidation assay (LPO). The anti-inflammatory property was evaluated by carrageenan-induced acute inflammation in rats by measuring rat paw volume at different time intervals and toxicological analysis using mice. Results and Discussion: High performance liquid chromatography studies revealed the presence of gallic acid (2.10%), mucic acid (4.90%), ellagic acid (2.10%), quercetin (28.00%), rutin (3.89%), and β-glucogallin (1.46%). MEO showed highest antioxidant activities by using DPPH (17.33–89.00%), ABTS (23.03–94.16%), nitric oxide scavenging activity (12.94–70.16%), LPO (56.54%), and phosphomolybdenum assay (142 ± 6.09 μg/ml). The LD50was found to be approximately 1125 mg/kg (p.o). High dose of MEO showed significant reduction (72.71%) in the inflammation after 4 h of treatment, which was comparable to diclofenac (10 mg/kg) (61.57%) treated group. Significant reduction (P < 0.05) in the inflammatory cytokine (interleukin-1β and tumor necrosis factor-α) markers were also observed (57.25% and 35.41%, respectively) in serum of MEO treated animals as compared to control. Conclusion: Taken together, phenolic compounds of MEO may serve as a potential herbal drug for amelioration of acute inflammation due to their modulatory action on free radicals.
  2 4,202 17
Hepatoprotective effect of a polyherbal extract containing Andrographis Paniculata, Tinospora Cordifolia and Solanum Nigrum against paracetamol induced hepatotoxicity
Dewasya Pratap Singh, Harshika Awasthi, Suaib Luqman, Saudan Singh, Dayanandan Mani
October 2015, 11(44):375-379
DOI:10.4103/0973-1296.168945  PMID:26929570
Background: Traditionally, a number of medicinal plants are used to treat various types of hepatic disorders but few of them were pharmacologically evaluated for their safety and efficacy. The combination of Andrographis paniculata (Kalmegha), Tinospora cordifolia (Guduchi), and Solanum nigrum (Kakmachi) was traditionally used in Indian System of Medicine (Ayurveda) for the treatment of various liver-related disorders. Objective: In the present study, an attempt was made to substantiate the ethnopharmacological use of a traditional formulation in hepatoprotection against paracetamol-induced hepatotoxicity. Subjects and Methods: Swiss albino mice (weight 20–25 g) were used for this study. Intraperitoneal injection of paracetamol (500 mg/kg body weight) was used to induce hepatotoxicity. Serum levels of alanine transaminase, aspartate aminotransferase, bilirubin, alkaline phosphatase, were used as indices of liver injury. In addition total cholesterol, triglyceride, low-density lipoprotein, high-density lipoprotein and creatinine were also assayed using the standard procedure. Results: Among the two different doses, pretreatment with Polyherbal extract at 500 mg/kg body weight exhibited a significant (P < 0.05) hepatoprotective activity as compared to paracetamol group. Conclusion: The polyherbal extract exhibits a significant hepatoprotective effect in vivo. The study contributes to its use in traditional ayurveda system for the management of liver diseases.
  1 2,748 18
Xanthii Fructus inhibits allergic response in the ovalbumin-sensitized mouse allergic rhinitis model
Nam-Gil Gwak, Eun-Young Kim, Bina Lee, Jae-Hyun Kim, Yong-Seok Im, Ka-Yeon Lee, Chang Jun-Kum, Ho-Seok Kim, Hyun-Joo Cho, Hyuk-Sang Jung, Youngjoo Sohn
October 2015, 11(44):352-361
DOI:10.4103/0973-1296.166058  PMID:26664025
Background: Xanthii Fructus (XF) is widely used in traditional anti-bacterial and anti-inflammatory Asian medicine. Allergic rhinitis is a common inflammatory disease characterized by markedly increased levels of anti-inflammatory factors and the recruitment of inflammatory cells into the nasal mucosa. We investigated the effects of XF in the allergen-induced rhinitis model. Materials and Methods: Following ovalbumin (OVA)/alum intraperitoneal injection on days 0, 7 and 14, the BALB/c mice (albino, laboratory-bred strain of the house mice) were challenged intranasally with OVA for 10 days a week after the last sensitization. The number of sneezes was recorded for 10 days; additionally, the levels of cytokines, histamine, immunoglobulin E (IgE) and OVA-specific serum IgE were estimated. Eosinophil infiltration, thickness of nasal mucosa and expression of caspase-1 were determined by immunohistochemistry. We also evaluated the effect of XF on the phosphorylation of nuclear factor kappa-B (NF-κB) and inhibitor of nuclear factor kappa B-alpha (IκB-α) in human mast cell-1 (HMC-1), by Western blotting. Results: The administration of XF significantly decreased sneezing and the serum levels of histamine, IgE, OVA-specific IgE, and cytokines such as tumor necrosis factor-alpha (TNF-α), interleukine-1 beta (IL-1β), IL-5, IL-6, monocyte chemoattractant protein-1 (MCP-1) and macrophage inflammatory protein-2 (MIP-2). XF inhibited the changes in thickness of the nasal septum, influx of eosinophils and expression of capase-1. In addition, XF inhibited the phosphorylation of IκB-α and NF-κB in phorbol-myristate-acetate plus calcium ionophore A23187 (A23187) stimulated HMC-1. Conclusion: This study suggests that XF acts a potent anti-allergic drug which alleviates the allergic responses in ovalbumin-sensitized mouse allergic rhinitis model.
  1 1,675 16
Chemical composition of the essential oil and fixed oil Bauhinia pentandra (Bong.) D. Dietr
Macia C. S. de Almeida, Luciana G. S. Souza, Daniele A. Ferreira, Francisco J. Q. Monte, Raimundo Braz-Filho, Telma L. G. de Lemos
October 2015, 11(44):362-364
DOI:10.4103/0973-1296.166015  PMID:26664026
Background: Bauhinia pentandrais popularly known as "mororó" and inhabits the Caatinga and Savannah biomes. Objective: This paper reports the chemical composition of the essential and fatty oils of the leaves from B. pentandra. Materials and Methods: The essential oil was obtained by hydrodistillation and the fixed oil by extraction with hexane, followed by saponification with KOH/MeOH, and methylation using MeOH/HCl. The constituents were analyzed by gas chromatography-mass spectrometry. Results: The major constituent of the essential oil was the phytol (58.78% ±8.51%), and of the fatty oil were palmitic (29.03%), stearic (28.58%) and linolenic (10.53%) acids. Conclusion: Of the compounds identified in the essential oil, three are first reported in this species, and this is the first record of the chemical composition of the fixed oil.
  1 1,223 17
In vitro anti-oxidant, cytotoxic and pro-apoptotic effects of Achillea teretifolia Willd extracts on human prostate cancer cell lines
Elif Burcu Bali, Leyla Açik, Pinar Elçi, Meral Sarper, Ferit Avcu, Mecit Vural
October 2015, 11(44):308-315
DOI:10.4103/0973-1296.166060  PMID:26664020
Background: The majority of Achillea species are the most important native economic plants of Anatolia. They include highly bioactive compounds, so they have therapeutic applications. Objective: In the present study, the aim was to investigate in vitro anti-oxidant, cytotoxic and pro-apoptotic effects of Achillea teretifolia Willd extracts (Turkish name: Beyaz civanperÇemi). Materials and Methods: The anti-oxidant potential of the extracts was analyzed by the free radical 1,1-diphenyl-2-picryl-hydrazyl (DPPH) and total phenolic content methods. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was used to detect cytotoxicity of the extracts onhuman prostate cancer cell lines (DU145 and PC-3) and human gingival fibroblast (HGF) cells. mRNA expression levels of pro-apoptotic (bax, caspase-3) and anti-apoptotic (bcl-2) genes were measured by quantitative real-time polymerase chain reaction. Results: The results showed that extracts exhibited a remarkable DPPH scavenging activity, and total phenolic content of the methanol extract was higher than that of the water extract. As time and concentration were increased, the methanol extract exhibited a more powerful cytotoxic effect on prostate cancer cells. In prostate cancer cells, the levels of mRNA expression of the bax and caspase-3 genes were significantly up-regulated (P < 0.05), whereas the expression of bcl-2 was down-regulated (P < 0.05). In HGF cells, there were no cytotoxic effect and apoptosis induction triggered by the extracts. Conclusion: The methanol extract had more powerful anti-oxidant, cytotoxic and pro-apoptotic effects than the water extract. The extracts could be good anti-oxidant sources, and they might include anti-cancer compounds triggering the cytotoxicity and the apoptosis on prostate cancer cells.
  1 1,488 16
Metabolic differentiation and classification of abnormal Savda Munziq's pharmacodynamic role on rat models with different diseases by nuclear magnetic resonance-based metabonomics
Batur Mamtimin, Guo Xia, Mahmut Mijit, Mawlanjan Hizbulla, Nazuk Kurbantay, Li You, Halmurat Upur
October-December 2015, 11(44):698-706
DOI:10.4103/0973-1296.165551  PMID:26600713
Background: Abnormal Savda Munziq (ASMq) is a traditional Uyghur herbal preparation used as a therapy for abnormal Savda-related diseases. In this study, we investigate ASMq's dynamic effects on abnormal Savda rat models under different disease conditions. Materials and Methods: Abnormal Savda rat models with hepatocellular carcinoma (HCC), type 2 diabetes mellitus (T2DM), and asthma dosed of ASMq. Serum samples of each animal tested by nuclear magnetic resonance spectroscopy and analyzed by orthogonal projection to latent structure with discriminant analysis. Results: Compared with healthy controls, HCC rats had higher concentrations of amino acids, fat-related metabolites, lactate, myoinositol, and citrate, but lower concentrations of α-glucose, β-glucose, and glutamine. Following ASMq treatment, the serum acetone very low-density lipoprotein (VLDL), LDL, unsaturated lipids, acetylcysteine, and pyruvate concentration decreased, but α-glucose, β-glucose, and glutamine concentration increased (P < 0.05). T2DM rats had higher concentrations of α- and β-glucose, but lower concentrations of isoleucine, leucine, valine, glutamine, glycoprotein, lactate, tyrosine, creatine, alanine, carnitine, and phenylalanine. After ASMq treated T2DM groups showed reduced α- and β-glucose and increased creatine levels (P < 0.05). Asthma rats had higher acetate, carnitine, formate, and phenylalanine levels, but lower concentrations of glutamine, glycoprotein, lactate, VLDL, LDL, and unsaturated lipids. ASMq treatment showed increased glutamine and reduced carnitine, glycoprotein, formate, and phenylalanine levels (P < 0.05). Conclusion: Low immune function, decreased oxidative defense, liver function abnormalities, amino acid deficiencies, and energy metabolism disorders are common characteristics of abnormal Savda-related diseases. ASMq may improve the abnormal metabolism and immune function of rat models with different diseases combined abnormal Savda.
  1 1,481 15
Evaluation of Antiplasmodial activity of extracts and constituents from Ampelozizyphus amazonicus
Dominique F. M. do Carmo, Ana Claudia F Amaral, Marta Machado, Dinora Lopes, Aurea Echevarria, Virgílio E Rosário, Jefferson Rocha de A. Silva
October 2015, 11(44):244-250
DOI:10.4103/0973-1296.166071  PMID:26664012
Background: Ampelozizyphus amazonicus Ducke, a plant that is widely used by the population of the Amazonian region to prevent and treat malaria, was investigated in this work, which describes, for the first time, the antiplasmodial activity of its extracts and associates this activity with its isolated constituents. Methods: Different extracts with solvents of increasing polarity (hexane, chloroform, ethanol, and water) were obtained of the root bark. This procedure resulted in extracts that were characterized for their constituents. The cytotoxicity and activity of the extracts against Plasmodium berghei (schizontocidal activity, liver stage) and Plasmodium falciparum (3D7 and Dd2 strains, erythrocyte stage) were assessed in vitro. Results: Of the four extracts assayed against P. berghei, the chloroform extract showed the greatest activity, with an inhibitory concentration 50% (IC50) value of 30.1 µg/mL, followed by the aqueous extract (IC50 = 39.9 µg/mL). The chloroform extract exhibited the highest antiplasmodial activity in the erythrocyte stage of P. falciparum, with an IC50value lower than 15 µg/mL. Fractionation of this more active extract led to the isolation and elucidation of pentacyclic triterpenes, lupeol, betulin and betulinic acid, which showed antiplasmodial activities with IC50values ranging from 5.6 to 80.30 µM. The most active of these, betulinic acid, was further quantified in the extracts by high-performance liquid chromatography-photodiode array detector analyzes. The higher amount was found in the chloroform extract, which was the most active one against P. falciparum. Conclusion: The results obtained in this work may partly explain the popular intake of A. amazonicusas an antimalarial remedy in the Amazon region.
  1 1,613 16
Repellant and insecticidal activities of shyobunone and isoshyobunone derived from the essential oil of Acorus calamus rhizomes
Hai-Ping Chen, Kai Yang, Li-Shi Zheng, Chun-Xue You, Qian Cai, Cheng-Fang Wang
October-December 2015, 11(44):675-681
DOI:10.4103/0973-1296.165543  PMID:26600710
Context: It was found that the essential oil of Acorus calamus rhizomes showed insecticidal activity. Aim: The aim of this study was to determine the chemical composition of the essential oil from A. calamus rhizomes, evaluate insecticidal and repellant activity against Lasioderma serricorne (LS) and Tribolium castaneum (TC), and to isolate any insecticidal constituents from the essential oil. Materials and Methods: Essential oil from A. calamus was obtained by hydrodistillation and analyzed by gas chromatography (GC) flame ionization detector and GC-mass spectrometry. The insecticidal and repellant activity of the essential oil and isolated compounds was tested using a variety of methods. Results: The main components of the essential oil were identified to be isoshyobunone (15.56%), β-asarone (10.03%), bicyclo[6.1.0]non-1-ene (9.67%), shyobunone (9.60%) and methylisoeugenol (6.69%). Among them, the two active constituents were isolated and identified as shyobunone and isoshyobunone. The essential oil showed contact toxicity against LS and TC with LD 50 values of 14.40 and 32.55 μg/adult, respectively. The isolated compounds, shyobunone and isoshyobunone also exhibited strong contact toxicity against LS adults with LD 50 values of 20.24 and 24.19 μg/adult, respectively, while the LD 50 value of isoshyobunone was 61.90 μg/adult for TC adults. The essential oil, shyobunone and isoshyobunone were strongly repellent (98%, 90% and 94%, respectively, at 78.63 nL/cm 2 , after 2 h treatment) against TC. Conclusion: The essential oil, shyobunone and isoshyobunone possessed insecticidal and repellant activity against LS and TC.
  1 1,884 18
Optimization of ultrasound-assisted extraction of phenolic compounds from Cimicifugae rhizoma with response surface methodology
Lin Liu, Bao-Jia Shen, Dong-Hao Xie, Bao-Chang Cai, Kun-Ming Qin, Hao Cai
October-December 2015, 11(44):682-689
DOI:10.4103/0973-1296.165545  PMID:26600711
Background: Cimicifugae rhizoma was a Ranunculaceae herb belonging to the composite family, and the roots of C. rhizoma have been widely used in tradition Chinese medicine. Materials and Methods: Ultrasound-assisted extraction (UAE) of phenolic compounds from C. rhizoma. Caffeic acid (CA), isoferulic acid (IA), ferulic acid (FA), and total phenols were quantified by high-performance liquid chromatography-diode array detection and ultraviolet-visible spectrophotometer. Effects of several experimental parameters, such as ultrasonic power (W), extraction temperature (°C), and ethanol concentration (%) on extraction efficiencies of phenolic compounds from C. rhizoma were evaluated. Results: The results showed that the optimal UAE condition was obtained with ultrasonic power of 377.35 W, extraction temperature of 70°C, and ethanol concentration of 58.37% for total phenols, and ultrasonic power of 318.28 W, extraction temperature of 59.65°C, and ethanol concentration of 64.43% for combination of CA, IA, FA. Conclusions: The experimental values under optimal conditions were in good consistent with the predicted values, which suggested UAE is more efficient for the extraction of phenolic compounds from plant materials.
  1 1,804 15
Phenolic profile and in vitro antioxidant activity of endemic Bulgarian carduus species
Ivanka Dimitrova-Dyulgerova, Iliya Zhelev, Dasha Mihaylova
December 2015, 11(44):575-579
DOI:10.4103/0973-1296.172964  PMID:27013797
Background: Plant species from genus Carduus are widely distributed in the world and represented in Bulgaria by 14 species. Previous investigations on this genus demonstrated a strong antioxidant potential of extract from some Bulgarian Carduus species. Objective: The present study investigates the phenolic profile and the antioxidant potential of different extracts obtained from four endemic Compositae herbs, growing wild in Bulgaria: Carduus armatus Boiss and Heldr., Carduus candicans Waldst. et Kit ssp. globifer (Velen.) Kazmi., Carduus rhodopaeus Velen. and Carduus thracicus (Velen.) Hayek. Materials and Methods: Antioxidant capacity of the obtained extracts was estimated with 2,2-diphenyl-1-picrylhydrazyl, 2,2'- azino-bis (3-ethylbenzothiazoline-6-sulphonic acid), and ferric reducing antioxidant power and copper reduction antioxidant assays. Phenolic profile was estimated by high performance liquid chromatography. Results: Eleven phenolic acids and eight flavonoids were quantified in the inflorescences. Sinapic (2760.72 ± 15.68 mg/g dry weight [dw]), chlorogenic (2564.50 ± 19.73 mg/g dw) and ferulic acids (1648.71 ± 19.57 mg/g dw), as well as luteolin (2345.45 ± 18.61 mg/g dw) and apigenin (1332.75 ± 12.05 mg/g dw) were found to be the predominant compounds. The above contents are the highest values found in C. candicans ssp. globifer. The highest established antioxidant activity (AOA) was in favor of the ethanolic extracts, and the extract of C. rhodopaeus affirmed with the highest AOA among the investigated plant species. Conclusion: All identified phenolic compounds were reported for the 1 st time in the studied endemic Carduus species, as well as their antioxidant capacities. The present study revealed that these plant species could be used as sources of antioxidants with potential medicinal properties.
  1 1,091 17
Modulation of hepatic cytochrome p450 enzymes by curcumin and its pharmacokinetic consequences in sprague-dawley rats
Sang-Bum Kim, Seung-Sik Cho, Hyun-Jong Cho, In-Soo Yoon
December 2015, 11(44):580-584
DOI:10.4103/0973-1296.172965  PMID:27013798
Background: Curcumin (CUR) is a polyphenolic component derived from an herbal remedy and dietary spice turmeric (Curcuma longa). Objective: The aim of this study was to investigate inhibitory effects of CUR on in vitro cytochrome P450 (CYP) activity and in vivo pharmacokinetic consequences of single CUR dose in rats. Materials and Methods: An in vitro CYP inhibition study in rat liver microsomes (RLM) was conducted using probe substrates for CYPs. Then, an in vivo pharmacokinetics of intravenous buspirone (BUS), a probe substrate for CYP3A, was studied with the concurrent administration of oral CUR in rats. Results: In the in vitro CYP inhibition study, CUR inhibited the CYP3A-mediated metabolism of testosterone (TES) with a half maximal inhibitory concentration of 11.0 ΁ 3.3 mM. However, the impact of a single oral CUR dose on the pharmacokinetics of BUS in rats is limited, showing that CUR cannot function as an inhibitor for CYP3A-mediated drug metabolism in vivo. Conclusion: To the best of our knowledge, our results are the first reported data regarding the inhibition of in vitro CYP3A-mediated metabolism of TES and the in vivo impact of a single CUR dose on the pharmacokinetics of BUS in rats. Further study is required to draw a confirmative conclusion on whether CUR can be a clinically relevant CYP3A4 inhibitor.
  1 1,477 16
Anticancer activity of chloroform extract and sub-fractions of nepeta deflersiana on human breast and lung cancer cells: an in vitro cytotoxicity assessment
Mai M Al-Oqail, Ebtesam S Al-Sheddi, Maqsood A Siddiqui, Javed Musarrat, Abdulaziz A Al-Khedhairy, Nida N Farshori
December 2015, 11(44):598-605
DOI:10.4103/0973-1296.172968  PMID:27013801
Background: Cancer is one of the major causes of death worldwide. The plant-derived natural products have received considerable attention in recent years due to their diverse pharmacological properties including anticancer effects. Nepeta deflersiana (ND) is used in the folk medicine as antiseptic, carminative, antimicrobial, antioxidant, and for treating rheumatic disorders. However, the anticancer activity of ND chloroform extract has not been explored so far. Objectives: The present study was aimed to investigate the anticancer activities of chloroform Nepeta deflersiana extract and various sub-fractions (ND-1-ND-15) of ND against human breast cancer cells (MCF-7) and human lung cancer cells (A-549). Materials and Methods: The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and neutral red uptake assays, and cellular morphological alterations using phase contrast light microscope were studied. Cells were exposed with 10-1000 mg/ml of sub-fractions of ND for 24 h. Results: Results showed that selected sub-fractions of the chloroform extract significantly reduced the cell viability of MCF-7 and A-549 cells, and altered the cellular morphology in a concentration-dependent manner. Among the sub-fractions, ND-10 fraction showed relatively higher cytotoxicity compared to other fractions whereas, ND-1 did not cause any cytotoxicity even at higher concentrations. The A-549 cells were found to be more sensitive to growth inhibition by all the extracts as compared to the MCF-7 cells. Conclusion: The present study provides preliminary screening of anticancer activities of chloroform extract and sub-fractions of ND, which can be further used for the development of a potential therapeutic anticancer agent.
  1 2,186 16
Inhibitory effect of spirulina maxima on the azoxymethane-induced aberrant colon crypts and oxidative damage in mice
Isela Alvarez-Gonzalez, Víctor Islas-Islas, Germán Chamorro-Cevallos, Juan Pablo Barrios, Norma Paniagua, Verónica R Vásquez-Garzón, Saúl Villa-Treviño, Osiris-Madrigal-Santillán , José Antonio Morales-González, Eduardo Madrigal-Bujaidar
December 2015, 11(44):619-624
DOI:10.4103/0973-1296.172973  PMID:27013804
Background: Spirulina maxima (Sm) is a cyanobacterium well known because of its high nutritive value, as well as its anti-inflammatory, anti-hyperlipidemic, antioxidant, and anti-genotoxic activities. Objective: To determine the capacity of Sm to inhibit the induction of aberrant colon crypts (AC), as well as the level of lipid peroxidation and DNA oxidative damage in mice treated with azoxymethane (AOM). Materials and Methods: Sm (100, 400, and 800 mg/kg) was daily administered to animals by the oral route during 4 weeks, while AOM (10 mg/kg) was intraperitoneally injected to mice twice in weeks 2 and 3 of the assay. We also included a control group of mice orally administered with distilled water along the assay, as well as other group orally administered with the high dose of Sm. Results: A significant decrease in the number of AC with the three tested doses of Sm, with a mean protection of 51.6% respect to the damage induced by AOM. Also, with the three doses of the alga, we found a reduction in the level of lipoperoxidation, as well as in regard to the percentage of the DNA adduct 8-hydroxy-2'- deoxyguanosine. Conclusion: Sm possesses anti-precarcinogenic potential in vivo, as well as capacity to reduce the oxidative damage induced by AOM.
  1 1,337 17
In vitro antimicrobial activity of traditional plant used in mestizo shamanism from the Peruvian amazon in case of infectious diseases
Vincent Roumy, Andréa-Luz Gutierrez-Choquevilca, Jean Pierre Lopez Mesia, Lastenia Ruiz, Juan Celidonio Ruiz Macedo, Amin Abedini, Ameni Landoulsi, Jennifer Samaillie, Thierry Hennebelle, Céline Rivière, Christel Neut
December 2015, 11(44):625-633
DOI:10.4103/0973-1296.172975  PMID:27013805
Context: Our survey was performed near Iquitos (Peruvian Amazon) and its surroundings and leads us to consider Mestizo ethnomedical practices. The plant species reported here are traditionally used for ailments related to microbial infections. Inhabitants of various ethnic origins were interviewed, and 52 selected plants extracts were evaluated for their antimicrobial properties against a panel of 36 sensitive and multi-resistant bacteria or yeast. The study aimed at providing information on antimicrobial plant extract activities and the ethnomedical context of Mestizo riverine populations from Loreto (Peru). Material and Method: The minimum inhibitory concentrations (MICs) of the plant crude extracts were carried out using the agar dilution method and ranged between 0.075 and 5.0 mg/ml. Results: Of the 40 plants analyzed, 9 species showed MIC ≤0.3 mg/ml (Anacardium occidentale, Couroupita guianensis, Croton lechleri, Davilla rugosa, Erythrina amazonica, Jacaranda copaia subsp. Spectabilis, Oenocarpus bataua, Peperomia macrostachya, and Phyllanthus urinaria) for one or several of the 36 microorganisms and only 6 drug extracts were inactive. Among the 40 plants, 13 were evaluated for the first time for an antibacterial activity. Conclusion: This evaluation of the antimicrobial activity of 40 plants using an approved standard methodology allowed comparing those activities against various microbes to establish antimicrobial spectra of standardized plant extracts, and give support to the traditional use of these plants. It may also help discovering new chemical classes of antimicrobial agents that could serve against multi-resistant bacteria.
  1 2,118 24
Anti-inflammatory and cytotoxic activities of Bursera copallifera
M. F. María C. Columba-Palomares, Dra. María L. Villareal, M. C. Macdiel E. Acevedo Quiroz, M. C. Silvia Marquina Bahena, Dra. Laura P. Álvarez Berber, Dra. Verónica Rodríguez-López
October 2015, 11(44):322-328
DOI:10.4103/0973-1296.166067  PMID:26664022
Background: The plant species Bursera copallifera (DC) bullock is used in traditional medicine to treat inflammation.The leaves of this plant can be prepared as an infusion to treat migraines, bronchitis, and dental pain. Objective: The purpose of this study was to determine the anti-inflammatory and cytotoxic activities of organic extracts from the stems, stem bark, and leaves of B. copallifera, which was selected based on the knowledge of its traditional use. Materials and Methods: We evaluated the ability of extracts to inhibit mouse ear inflammation in response to topical application of 12-O tetradecanoylphorbol-13-acetate. The extracts with anti-inflammatory activity were evaluated for their inhibition of pro-inflammatory enzymes. In addition, the in vitro cytotoxic activities of the organic extracts were evaluated using the sulforhodamine B assay. Results: The hydroalcoholic extract of the stems (HAS) exhibited an anti-infl ammatory activity of 54.3% (0.5 mg/ear), whereas the anti-infl ammatory activity of the dichloromethane-methanol extract from the leaves (DMeL) was 55.4% at a dose of 0.1 mg/ear. Methanol extract from the leaves (MeL) showed the highest anti-inflammatory activity (IC50 = 4.4 μg/mL), hydroalcoholic extract of leaves, and DMeL also reduce the enzyme activity, (IC50 = 6.5 μg/mL, IC50 = 5.7 μg/mL), respectively, from stems HAS exhibit activity at the evaluated concentrations (IC50 =6.4 μg/mL). The hydroalcoholic extract of the stems exhibited the highest cytotoxic activity against a breast adenocarcinoma cell line (MCF7, IC50 = 0.90 μg/mL), whereas DMeL exhibited an IC50 value of 19.9 μg/mL. Conclusion: In conclusion, extracts from leaves and stems inhibited cyclooxygenase-1, which is the target enzyme for nonsteroidal anti inflammatory drugs, and some of these extracts demonstrated substantial antiproliferative effects against the MCF7 cell line. These results validate the traditional use of B. copallifera.
  1 1,461 17
Hypoglycemic effects of a standardized extract of salvia miltiorrhiza roots in rats
Mauro A. M. Carai, Giancarlo Colombo, Barbara Loi, Alessandro Zaru, Antonella Riva, Walter Cabri, Paolo Morazzoni
December 2015, 11(44):545-549
DOI:10.4103/0973-1296.172959  PMID:27013792
Background and Aims: Salvia miltiorrhiza Bunge (Labiatae) is a Chinese medicinal plant, the dried roots of which (known as Dan-Shen) have been used for hundreds of years in the treatment of a series of ailments, including hyperglycemia. This study was designed to evaluate the hypoglycemic effect of a new, standardized extract of S. miltiorrhiza. Materials and Methods: S. miltiorrhiza extract (containing 21% total tanshinones and 3.7% tanshinone IIA) was administered acutely and intragastrically at the doses of 0, 50, 100, and 200 mg/kg to male, healthy, fasted Wistar rats 60 min before the intragastric infusion of a bolus of starch (3 g/kg; a semi-naturalistic experimental condition) (Experiment 1) or glucose (2 g/kg) (Experiment 2). Results: In both experiments, treatment with S. miltiorrhiza extract produced a dose-related decrease in glycemia, evidenced in terms of reduction of peak value and/or area under the curve of the time-course of glycemia. The effect of S. miltiorrhiza extract occurred at doses devoid of any behavioral toxicity in rats. Conclusion: The results of this study suggest that the hypoglycemic effect of S. miltiorrhiza extract was likely secondary to an action on carbohydrate metabolism. These results are consistent with several preclinical and clinical data and add further support to the hypothesis that S. miltiorrhiza extracts may act as effective anti-hyperglycemic remedies.
  1 1,328 17
Cucumis melo ssp. Agrestis var. Agrestis Ameliorates High Fat Diet Induced Dyslipidemia in Syrian Golden Hamsters and Inhibits Adipogenesis in 3T3-L1 Adipocytes
Kripa Shankar, Sumit K Singh, Durgesh Kumar, Salil Varshney, Abhishek Gupta, Sujith Rajan, Ankita Srivastava, Muheeb Beg, Anurag Kumar Srivastava, Sanjeev Kanojiya, Dipak K Mishra, Anil N Gaikwad
December 2015, 11(44):501-510
DOI:10.4103/0973-1296.172945  PMID:27013786
Background: Cucumis melo ssp. agrestis var. agrestis (CMA) is a wild variety of C. melo. This study aimed to explore anti-dyslipidemic and anti-adipogenic potential of CMA. Materials and Methods: For initial anti-dyslipidemic and antihyperglycemic potential of CMA fruit extract (CMFE), male Syrian golden hamsters were fed a chow or high-fat diet with or without CMFE (100 mg/kg). Further, we did fractionation of this CMFE into two fractions namely; CMA water fraction (CMWF) and CMA hexane fraction (CMHF). Phytochemical screening was done with liquid chromatography-mass spectrometry LC- (MS)/MS and direct analysis in real time-MS to detect active compounds in the fractions. Further, high-fat diet fed dyslipidemic hamsters were treated with CMWF and CMHF at 50 mg/kg for 7 days. Results: Oral administration of CMFE and both fractions (CMWF and CMHF) reduced the total cholesterol, triglycerides, low‐density lipoprotein cholesterol, and very low‐density lipoprotein-cholesterol levels in high fat diet-fed dyslipidemic hamsters. CMHF also modulated expression of genes involved in lipogenesis, lipid metabolism, and reverse cholesterol transport. Standard biochemical diagnostic tests suggested that neither of fractions causes any toxicity to hamster liver or kidneys. CMFE and CMHF also decreased oil-red-O accumulation in 3T3-L1 adipocytes. Conclusion: Based on these results, it is concluded that CMA possesses anti-dyslipidemic and anti-hyperglycemic activity along with the anti-adipogenic activity.
  1 1,824 19
Morphological and chemoprofile (liquid chromatography-mass spectroscopy and gas chromatography-mass spectroscopy) comparisons of Cyperus scariosus R. Br and Cyperus rotundus L.
Lavanya Kakarla, Suresh Babu Katragadda, Mahendran Botlagunta
October 2015, 11(44):439-447
DOI:10.4103/0973-1296.168975  PMID:26929579
Background: Cyperus scariosus (CS) R.Br and Cyperus rotundus (CR) L. belongs to Cyperaceae family which is well-reputed in the traditional systems of medicine. Although they grow in different agro-climatic conditions, they are often considered to be synonymous with each other. Objective: The present study was aimed to systematically classify both the species CS and CR through their morphological features and chemical profiling using liquid chromatography-mass spectroscopy (LC-MS), gas chromatography-mass spectroscopy (GC-MS) and thin layer chromatography patterns of the rhizome extracts. Materials and Methods: A method (LC-MS analysis) has been developed on Agilent LC-MSD Trap SL mass spectrometer equipped with Waters HR C18 column (3.9 mm × 300 mm, 6 μm) using isocratic elution with acetonitrile and water (70:30% v/v ratio). GC-MS analysis was performed on a Shimadzu GC-MS-QP 2010 equipped with DB-5 capillary column (30 m × 0.25 mm × 0.25 μm). Results: Chemoprofiling of CS and CR using LC-MS and GC-MS suggested that these two are different based on their deferential spectral pattern, however, some of the common peaks were found in both the species. In addition, we also performed the preliminary phytochemical investigation of hexane and chloroform extracts of these species, which led to the isolation of stigmasterol, β-sitosterol and lupeol as major constituents in CS. Conclusion: In summary, we have developed optimal chromatographic conditions (LC-MS and GC-MS) and morphological profiles to classify both the species, that is, CS and CR. Collectively, our analytical results coupled with the morphological data clearly suggested that CS and CR are morphologically different.
  1 1,876 18
Culture conditions for production of biomass, adenosine, and cordycepin from Cordyceps sinensis CS1197: Optimization by desirability function method
Shashidhar M Ghatnur, Giridhar Parvatam, Manohar Balaraman
October 2015, 11(44):448-456
DOI:10.4103/0973-1296.168946  PMID:26929580
Background: Cordyceps sinensis (CS) is a traditional Chinese medicine contains potent active metabolites such as nucleosides and polysaccharides. The submerged cultivation technique is studied for the large scale production of CS for biomass and metabolites production. Objective: To optimize culture conditions for large-scale production of CS1197 biomass and metabolites production. Materials and Methods: The CS1197 strain of CS was isolated from dead larvae of natural CS and the authenticity was assured by the presence of two major markers adenosine and cordycepin by high performance liquid chromatography and mass spectrometry. A three-level Box-Behnken design was employed to optimize process parameters culturing temperature, pH, and inoculum volume for the biomass yield, adenosine and cordycepin. The experimental results were regressed to a second-order polynomial equation by a multiple regression analysis for the prediction of biomass yield, adenosine and cordycepin production. Multiple responses were optimized based on desirability function method. Results: The desirability function suggested the process conditions temperature 28°C, pH 7 and inoculum volume 10% for optimal production of nutraceuticals in the biomass. The water extracts from dried CS1197 mycelia showed good inhibition for 2 diphenyl-1-picrylhydrazyl and 2,2-azinobis-(3-ethyl-benzo-thiazoline-6-sulfonic acid-free radicals. Conclusion: The result suggests that response surface methodology-desirability function coupled approach can successfully optimize the culture conditions for CS1197.
  1 3,726 21
Synergistic caseinolytic activity and differential fibrinogenolytic action of multiple proteases of Maclura spinosa (Roxb. ex Willd.) latex
BK Venkatesh, Raghu Ram Achar, P Sharanappa, BS Priya, S Nanjunda Swamy
October 2015, 11(44):457-461
DOI:10.4103/0973-1296.168987  PMID:26929581
Background: Kollamalayaali tribes of South India use latex of Maclura spinosa for milk curdling. This action is implicated to proteases which exhibit strong pharmacological potential in retardation of blood flow and acceleration of wound healing. Objective: To validate the presence of a proteolytic enzyme(s) in Maclura spinosa latex (MSL), and to investigate their probable role in hemostasis. Materials and Methods: Processed latex was examined for proteolytic and hemostatic activity using casein and human fibrinogen as substrates, respectively. Caseinoltyic activity was compared with two standard proteases viz., trypsin I and trypsin II. Effect of various standard protease inhibitors viz., iodoacetic acid (IAA), phenylmethylsulfonyl fluoride (PMSF), ethylene glycol tetraacetic acid, and ethylenediaminetetraacetic acid on both caseinolytic and fibrinogenolytic activities were examined. Electrophoretogram of fibrinogenolytic assays were subjected to densitometric analysis. Results: Proteolytic action of MSL was found to be highly efficient over trypsin I and trypsin II in dose-dependent caseinolytic activity (P < 0.05; specific activity of 1,080 units/mg protein). The Aα and Bβ bands of human fibrinogen were readily cleaved by MSL (for 1 μg crude protein and 30 min of incubation time). Furthermore, MSL cleaved γ subunit in dose- and time-dependent manner. Quantitative correlation of these results was obtained by densitometric analysis. The caseinolytic activity of MSL was inhibited by IAA, PMSF. While, only PMSF inhibited fibrinogenolytic activity. Conclusions: MSL contains proteolytic enzymes belonging to two distinct superfamilies viz., serine protease and cysteine proteases. The fibrinogenolytic activity of MSL is restricted to serine proteases only. The study extrapolates the use of M. spinosa latex from milk curdling to hemostasis.
  1 1,350 17
Bio prospecting of marine-derived Streptomyces spectabilis VITJS10 and exploring its cytotoxicity against human liver cancer cell lines
Jemimah Naine Selvakumar, Subathra Devi Chandrasekaran, Mohanasrinivasan Vaithilingam
October 2015, 11(44):469-473
DOI:10.4103/0973-1296.168974  PMID:26929583
Background: Recently, numerous pathogens have developed resistance due to the indiscriminate use of commercial therapeutic drugs. Objective: The main aim of the study was to evaluate the bioactive potential of the Streptomyces spectabilis VITJS10 crude extract. Materials and Methods: The S. spectabilis VITJS10 ethyl acetate extract was tested for antibacterial, antioxidant, and cytotoxic properties. Genotypic characterization was done using 16S r-DNA partial gene amplification and sequencing. The authenticity of the crude chemical constitutes were determined by gas chromatography–mass spectrometry (GC-MS). Results: The antibacterial potential revealed the effective activity against Shigellaflexneri (MTCC No: 1457) (22 mm), Salmonella typhi (MTCC No: 1167) (23 mm), Escherichia coli (MTCC No: 1588) (22 mm), Pseudomonas aeruginosa (MTCC No: 4676) (22 mm) at 20 mg/mL concentration. Scavenging ability of the extract was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay revealing its 95% inhibition at 5 mg/mL concentration. Hepatocellular cancer cells (HepG2) cell line was used to evaluate the cytotoxicity by 3-(4, 5-dimethyl thiazol-2yl)-2, 5-diphenyl tetrazolium bromide assay. The extract showed maximum inhibition at IC50of 250 μg/mL with 53.6% cell viability. The highest 16S rRNA gene sequence homogeneity was observed 99% similar with the novel strain S. spectabilis S3-1. The chemical components of the crude extract of VITJS10 were detected with 37 chemical constituents. However three major compounds were identified, namely Sulfurous acid, 2-ethylhexyl tridecyl ester, Phenol, 2,4-bis (1,1-dimethylethyl), and Trans-2-methyl-4-n-pentylthiane, S, S-Dioxide. Conclusion: Hence the present study justifies the overwhelming circumstantial evidence as the most bioactive metabolites from the marine origin, which has potential utilization in pharmaceutical industry.
  1 1,936 15
Selective cytotoxicity and pro-apoptotic activity of stem bark of Wrightia tinctoria (Roxb.) R. Br. in cancerous cells
Shilpee Chaudhary, Raviraj Anand Devkar, Deepak Bhere, Manganahalli Manjunath Setty, Karkala Sreedhara Ranganath Pai
October 2015, 11(44):481-487
DOI:10.4103/0973-1296.168976  PMID:26929585
Background: Wrightia tinctoria (Roxb.) R. Br. is a widely available shrub in India used traditionally in various ailments, including cancer. However, the anticancer activity of the bioactive fractions has not been validated scientifically. Objective: To investigate the anticancer potential of stem bark of W. tinctoria and establish its phytochemical basis. Materials and Methods: The ethanol extract and subsequent fractions, petroleum ether, ethyl acetate, n-butanol, and aqueous were prepared by standard methods. In vitro cytotoxicity was determined in MCF-7 (breast) and HeLa (cervical) adenocarcinoma cells, and V79 (nontumor fibroblast) cells and apoptogenic activity in MCF-7 cells by acridine orange (AO)/ethidium bromide (EB) staining. Additionally, the antioxidant potential was evaluated using suitable methods. High-performance thin layer chromatography (HPTLC) analysis was performed for identification of active phytoconstituents. Results: Petroleum ether and ethyl acetate fractions were most potent with IC50values of 37.78 and 29.69 μg/ml in HeLa and 31.56 and 32.63 μg/ml in MCF-7 cells respectively in the sulforhodamine B assay. Comparable results were obtained in HeLa cells in 3-(4,5-dimethylthiazolyl-2-yl)-2,5-diphenyl tetrazolium bromide assay and interestingly, the fractions were found to be safe to noncancerous fibroblast cells. Both fractions induced significant (P < 0.05) apoptotic morphological changes observed by AO/EB staining. Moreover, extract/fractions exhibited excellent inhibition of lipid peroxidation with the ethyl acetate fraction being most active (IC50: 23.40 μg/ml). HPTLC confirmed the presence of two anti-cancer triterpenoids, lupeol, and β-sitosterol in active fractions. Conclusion: Extract/fractions of W. tinctoria exhibit selective cytotoxicity against cancerous cells that is mediated by apoptosis. Fractions are less toxic to noncancerous cells; hence, they can be developed as safer chemopreventive agents.
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Reversed-phase high-performance liquid chromatography-ultraviolet photodiode array detector validated simultaneous quantification of six bioactive phenolic acids in Roscoea purpurea tubers and their In vitro cytotoxic potential against various cell lines
Sharad Srivastava, Misra Ankita, Dharmesh Kumar, Amit Srivastava, Anil Sood, AKS Rawat
October 2015, 11(44):488-495
DOI:10.4103/0973-1296.168944  PMID:26929586
Background: Roscoea purpurea or Roscoea procera Wall. (Zingiberaceae) is traditionally used for nutrition and in the treatment of various ailments. Objective: Simultaneous reversed-phase high-performance liquid chromatography-ultraviolet (RP-HPLC) photodiode array detector identification of phenolic acids (PA's) was carried out in whole extract of tuber and their cytotoxic potential was estimated along with radical scavenging action. Bioactivity guided fractionation was also done to check the response potential against the same assay. Materials and Methods: Identification and method validation was performed on RP-HPLC column and in vitro assays were used for bioactivity. Results: Protocatechuic acid, syringic acid, ferulic acid, rutin, apigenin, and kaempferol were quantified as 0.774%, 0.064%, 0.265%, 1.125%, 0.128%, and 0.528%, respectively. Validated method for simultaneous determination of PA's was found to be accurate, reproducible, and linearity was observed between peak area response and concentration. Recovery of identified PA's was within the acceptable limit of 97.40–104.05%. Significant pharmacological response was observed in whole extract against in vitro cytotoxic assay, that is, Sulforhodamine B assay, however, fractionation results in decreased action potential. Similar pattern of results were observed in the antioxidant assay, as total phenolic content and total flavonoid content were highest in whole extract and decreases with fractionation. Radical scavenging activity was prominent in chloroform fraction, exhibiting IC50at 0.25 mg/mL. Conclusion: Study, thus, reveals that R. purpurea exhibit significant efficacy in cytotoxic activity with the potentiality of scavenging free radicals due the presence of PA's as reported through RP-HPLC.
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Modulatory role of Shorea robusta bark on Glucose-metabolizing enzymes in diethylnitrosamine induced hepatocellular carcinoma in rats
A Kalaiselvan, T Anand, K Gokulakrishnan, MC Kamaraj, S Velavan
October 2015, 11(44):496-500
DOI:10.4103/0973-1296.168981  PMID:26929587
Introduction: The modulations of glucose-metabolizing enzyme activities play a vital rolein the depletion of energy metabolism and leads to inhibition of cancer growth. Objective: To find the effect of shorearobusta bark extract on glucose-metbolizing enzymes in diethylnitrosamine (DEN) induced hepatocellular carcinoma rats. Materials and Methods: Biochemical evaluation of glucose metabolizing enzyme were done in before and after shorearobusta bark extract (500mg/kg) treatment in DEN induced rats. Results: A significant increasein the activities of the key glycolytic enzymes viz., hexokinase and phosphoglucoisomerase, with a significant decrease in the gluconeogenic enzymes glucose-6-phosphatase and fructose-1,6-bisphosphatasewere observed in HCC bearing rats, when compared with the control. Administration of shorearobusta extract caused a significant decrease in theactivities of glycolytic enzymes and an increase in the gluconeogenic enzymes activities to near normal values. Conclusion: The current findings suggest that the S. robusta extract has a definite modulating role on the key enzymes ofglucose-metabolism in HCC. The modulatory effect may be due to the phytoactive constituents present in the extract of S. robusta.
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Identity-based high-performance thin layer chromatography fingerprinting profile and tumor inhibitory potential of Anisochilus carnosus (L.f.) wall against ehrlich ascites carcinoma
Nilesh Gupta, Richard Lobo, Nimmy Kumar, Jay Kumar Bhagat, Jessy Elizabeth Mathew
October 2015, 11(44):474-480
DOI:10.4103/0973-1296.168977  PMID:26929584
Context: Anisochilus carnosus (L.f.) wall belonging to the family Lamiaceae is a plant that is widely used in folk medicine for treating eczema, cold, cough, and fever. Objective: In the present study, we explored the anticancer potential of A. carnosus leaves against Ehrlich ascites carcinoma (EAC) and estimated the quantity of luteolin present in various extracts and fractions of A. carnosus by high-performance thin layer chromatography (HPTLC) fingerprinting. Materials and Methods: Various factors such as tumor volume, tumor cell viability, tumor weight, prolongation of lifespan, and hematological parameters were assessed. Result: We observed a significant lowering in tumor volume, tumor weight, and cell viability in EAC-induced mice following intervention with A. carnosus extracts. Also, there was a considerable prolongation of host lifespan and restoration of hematological parameters to almost normal levels with A. carnosus treatment. HPTLC fingerprinting of various extracts and fractions of A. carnosus along with luteolin as the reference standard revealed the occurrence of luteolin in all tested extracts and fractions of A. carnosus with the highest concentration being reported in the ethanol fraction. Conclusion: A. carnosus exhibits potent anti-tumor potential which can most likely be attributed to the occurrence of different phytochemicals such as phytosterols, terpenoids, and flavonoids in the plant. Further studies to isolate compounds from A. carnosus and understand the mechanism of anti-tumor activity would be worthwhile.
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Dosakaya Juice Assuages Development of Sucrose Induced Impaired Glucose Tolerance and Imbalance in Antioxidant Defense
Dommati Anand Kumar, Pisupati S.R Sweeya, Srishti Shukla, Sanga Venkata Anusha, Dasari Akshara, Kuncha Madhusudana, Ashok Kumar Tiwari
October 2015, 11(44):462-468
DOI:10.4103/0973-1296.168985  PMID:26929582
Objective: The objective was to explore the effect of Dosakaya (DK) (Cucumis melo var. chito) juice on sucrose induced dysglycemia and disturbances in antioxidant defense in rats. Materials and Methods: Rats were preconditioned with DK juice before administration of sucrose beverage continuously for 1-month. Blood glucose tolerance test and glutathione (GSH) homeostasis pathways in kidney were analyzed in different group of animals at the end of the study. Results: DK juice diffused (P < 0.001) hypertriglyceridemia inducing effect of sucrose and arrested sucrose induced weight gain. It improved glucose tolerance ability by significantly reducing (P < 0.05) first-hour glycemic excursion and decreasing 2 h glycemic load (P < 0.05) following oral glucose tolerance test in sucrose fed animals. Furthermore, disturbances in antioxidant defense mechanisms in terms of GSH homeostasis in kidney were restored due to juice feeding. DK juice administration checked reduction in GSH-S-transferase and glyoxalase-I activity, thus, significantly mitigated lipid peroxidation (P < 0.05), and formation of advanced glycation end-products (P < 0.001) in kidney and serum (P < 0.01). Quantitative analysis of juice found it a rich source of protein and polyphenols. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis revealed the presence of multiple protein bands in whole fruit juice. Therefore, SDS-PAGE protein fingerprint of DK juice may serve as a quality control tool for standardization of juice. Conclusion: The whole fruit juice of DK may become cost-effective, affordable health beverage in extenuating ill-health effects of sugar consumption. This is the first report identifying DK juice in preventing development dysglycemia, dyslipidemia, and oxidative stress induced due to chronic sucrose feeding in rats.
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Alpha-amylase inhibition and antioxidant activity of marine green algae and its possible role in diabetes management
PS Unnikrishnan, K Suthindhiran, MA Jayasri
December 2015, 11(44):511-515
DOI:10.4103/0973-1296.172954  PMID:27013787
Aim: In the continuing search for safe and efficient antidiabetic drug, marine algae become important source which provide several compounds of immense therapeutic potential. Alpha-amylase, alpha-glucosidase inhibitors, and antioxidant compounds are known to manage diabetes and have received much attention recently. In the present study, four green algae (Chaetomorpha aerea, Enteromorpha intestinalis, Chlorodesmis, and Cladophora rupestris) were chosen to evaluate alpha-amylase, alpha-glucosidase inhibitory, and antioxidant activity in vitro. Materials and Methods: The phytochemical constituents of all the extracts were qualitatively determined. Antidiabetic activity was evaluated by inhibitory potential of extracts against alpha-amylase and alpha-glucosidase by spectrophotometric assays. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl, hydrogen peroxide (H 2 O 2 ), and nitric oxide scavenging assay. Gas chromatography-mass spectrometry (GC-MS) analysis was carried out to determine the major compound responsible for its antidiabetic action. Results: Among the various extracts screened, chloroform extract of C. aerea (IC 50 − 408.9 mg/ml) and methanol extract of Chlorodesmis (IC 50 − 147.6 mg/ml) showed effective inhibition against alpha-amylase. The extracts were also evaluated for alpha-glucosidase inhibition, and no observed activity was found. Methanol extract of C. rupestris showed notable free radical scavenging activity (IC 50 - 666.3 mg/ml), followed by H 2 O 2 (34%) and nitric oxide (49%). Further, chemical profiling by GC-MS revealed the presence of major bioactive compounds. Phenol, 2,4-bis (1,1-dimethylethyl) and z, z-6,28-heptatriactontadien-2-one were predominantly found in the methanol extract of C. rupestris and chloroform extract of C. aerea. Conclusion: Our results demonstrate that the selected algae exhibit notable alpha-amylase inhibition and antioxidant activity. Therefore, characterization of active compounds and its in vivo assays will be noteworthy.
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Sub-chronic administration of methanolic whole fruit extract of lagenaria breviflora (Benth.) roberty induces mild toxicity in rats
Olubukola Sinbad Olorunnisola, Anthony Jide Afolayan, Adewale Adetutu
December 2015, 11(44):516-521
DOI:10.4103/0973-1296.172955  PMID:27013788
Background: The effect of the methanolic whole fruit extract from Lagenaria breviflora on vital organs and antioxidant enzymes was investigated in this study. Materials and Methods: L. breviflora (250, 500 and 1000 mg/kg/b.w.t./day/rat) was fed orally with the cannula to male albino rats for 28 days. At the end of the treatment, the rats were sacrificed and the effect of the extract on histology of the liver, heart, lipid peroxidation, tissue and serum antioxidant enzymes (superoxide dismutase, catalase, glutathione-s-transferase, glutathione peroxidase) activities, glutathione, myocardial marker enzymes (creatine kinase [CK], lactate dehydrogenase [LDH], alanine transaminase [ALT], and aspartate transaminase [AST]) in serum, and heart homogenate were assessed. Results: The extract demonstrated mild organ doses dependent (500 and 1000 mg/kg) pathological alterations in the architectural section of the liver and heart. At 250 mg/kg/b.w.t., the extract caused a significant (P < 0.05) increase in the level of thiobarbituric reacting acids substance and antioxidant enzyme activities, but causes (P < 0.05) decrease in serum and tissue antioxidant capacity at 500 and 1000 mg/kg/b.w.t., respectively. Also on these two doses, a significant (P < 0.05) increase in serum activity of CK, LDH, ALT, and AST and concomitantly decrease (P < 0.05) in heart homogenate were also observed. Conclusion: The results suggested that the Fruit of L. breviflora may contain phytotoxic Substances(s) which may be hepatotoxic, cardiotoxic or able to induce oxidative stress at high concentration. Hence, the consumption of the plant should be taken with caution.
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Chemometrics optimized extraction procedures, phytosynergistic blending and in vitro screening of natural enzyme inhibitors amongst leaves of Tulsi, Banyan and Jamun
Baishakhi De, Koushik Bhandari, Rajeev K Singla, Prakash Katakam, Tanmoy Samanta, Dilip Kumar Kushwaha, Rohit Gundamaraju, Analava Mitra
December 2015, 11(44):522-532
DOI:10.4103/0973-1296.172956  PMID:27013789
Background: Tulsi, Banyan, and Jamun are popular Indian medicinal plants with notable hypoglycemic potentials. Now the work reports chemo-profiling of the three species with in-vitro screening approach for natural enzyme inhibitors (NEIs) against enzymes pathogenic for type 2 diabetes. Further along with the chemometrics optimized extraction process technology, phyto-synergistic studies of the composite polyherbal blends have also been reported. Objective: Chemometrically optimized extraction procedures, ratios of polyherbal composites to achieve phyto-synergistic actions, and in-vitro screening of NEIs amongst leaves of Tulsi, Banyan, and Jamun. Materials and Methods: The extraction process parameters of the leaves of three plant species (Ficus benghalensis, Syzigium cumini and Ocimum sanctum) were optimized by rotatable central composite design of chemometrics so as to get maximal yield of bio-actives. Phyto-blends of three species were prepared so as to achieve synergistic antidiabetic and antioxidant potentials and the ratios were optimized by chemometrics. Next, for in vitro screening of natural enzyme inhibitors the individual leaf extracts as well as composite blends were subjected to assay procedures to see their inhibitory potentials against the enzymes pathogenic in type 2 diabetes. The antioxidant potentials were also estimated by DPPH radical scavenging, ABTS, FRAP and Dot Blot assay. Results: Considering response surface methodology studies and from the solutions obtained using desirability function, it was found that hydro-ethanolic or methanolic solvent ratio of 52.46 ΁ 1.6 and at a temperature of 20.17 ΁ 0.6 gave an optimum yield of polyphenols with minimal chlorophyll leaching. The species also showed the presence of glycosides, alkaloids, and saponins. Composites in the ratios of 1:1:1 and 1:1:2 gave synergistic effects in terms of polyphenol yield and anti-oxidant potentials. All composites (1:1:1, 1:2:1, 2:1:1, 1:1:2) showed synergistic anti-oxidant actions. Inhibitory activities against the targeted enzymes expressed in terms of IC 50 values have shown that hydro-ethanolic extracts in all cases whether individual species or composites in varying ratios gave higher IC 50 values thus showing greater effectivity. Conclusion: Current research provides the state-of-the-art of search of NEIs amongst three species by in-vitro assays which can be further utilized for bioactivity-guided isolations of such enzyme inhibitors. Further, it reports the optimized phyto-blend ratios so as to achieve synergistic anti-oxidative actions.
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Secondary metabolites from leaves of Manilkara subsericea (Mart.) Dubard
Fernanda Borges de Almeida, Caio Pinho Fernandes, Wanderson Romao, Gabriela Vanini, Helber Barcelos Costa, Hildegardo Seibert França, Marcelo Guerra Santos, José Carlos Tavares Carvalho, Deborah Quintanilha Falcão, Leandro Rocha
December 2015, 11(44):533-537
DOI:10.4103/0973-1296.172957  PMID:27013790
Background: Manilkara subsericea (Sapotaceae) is a species widely spread in the sandbanks of Restinga de Jurubatiba National Park (Rio de Janeiro, Brazil). It is commonly known as "maηaranduba", "maηarandubinha" and "guracica," being used in this locality as food, and timber. However, M. subsericea remains almost unexplored regarding its chemical constituents, including secondary metabolites from the leaves. Objective: Identify the chemical constituents from the leaves of M. subsericea. Materials and Methods: Leaves were macerated with ethanol (96% v/v), and dried crude ethanolic extract was sequentially washed with the organic solvents in order to obtain an ethyl acetate fraction. Substances from this fraction were identified by different techniques, such as negative-ion electrospray ionization Fourier and 1 H and 13 C nuclear magnetic resonance (NMR). Fresh leaves from M. subsericea were also submitted to hydrodistillation in order to obtain volatile substances, which were identified by gas chromatograph coupled to mass spectrometer. Results: NMR 1 H and 13 C spectra allowed for the identification of the compounds myricetin, quercetin, and kaempferol from the ethyl acetate fraction. The negative-ion electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry mass spectrum also revealed the presence in this fraction of a polyhydroxytriterpene acid (pomolic acid), and some flavonoids, such as quercitrin, and myricitrin. In all 34 volatile compounds were identified by gas chromatography-mass spectrometry, including monoterpenes, sesquiterpenes, and long chain hydrocarbons. Conclusion: This study describes the first reports concerning the phytochemical information about leaves from M. subsericea.
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Chemometrics-based approach in analysis of Arnicae flos
Dimitrina Zh Zheleva-Dimitrova, Vessela Balabanova, Reneta Gevrenova, Irini Doichinova, Antonina Vitkova
December 2015, 11(44):538-544
DOI:10.4103/0973-1296.172958  PMID:27013791
Introduction: Arnica montana flowers have a long history as herbal medicines for external use on injuries and rheumatic complaints. Objective: To investigate Arnicae flos of cultivated accessions from Bulgaria, Poland, Germany, Finland, and Pharmacy store for phenolic derivatives and sesquiterpene lactones (STLs). Materials and Methods: Samples of Arnica from nine origins were prepared by ultrasound-assisted extraction with 80% methanol for phenolic compounds analysis. Subsequent reverse-phase high-performance liquid chromatography (HPLC) separation of the analytes was performed using gradient elution and ultraviolet detection at 280 and 310 nm (phenolic acids), and 360 nm (flavonoids). Total STLs were determined in chloroform extracts by solid-phase extraction-HPLC at 225 nm. The HPLC generated chromatographic data were analyzed using principal component analysis (PCA) and hierarchical clustering (HC). Results: The highest total amount of phenolic acids was found in the sample from Botanical Garden at Joensuu University, Finland (2.36 mg/g dw). Astragalin, isoquercitrin, and isorhamnetin 3-glucoside were the main flavonol glycosides being present up to 3.37 mg/g (astragalin). Three well-defined clusters were distinguished by PCA and HC. Cluster C1 comprised of the German and Finnish accessions characterized by the highest content of flavonols. Cluster C2 included the Bulgarian and Polish samples presenting a low content of flavonoids. Cluster C3 consisted only of one sample from a pharmacy store. Conclusion: A validated HPLC method for simultaneous determination of phenolic acids, flavonoid glycosides, and aglycones in A. montana flowers was developed. The PCA loading plot showed that quercetin, kaempferol, and isorhamnetin can be used to distinguish different Arnica accessions.
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In silico screening of antibacterial compounds from herbal sources against vibrio cholerae
Sabah Perveen, Hotam Singh Chaudhary
December 2015, 11(44):550-555
DOI:10.4103/0973-1296.172960  PMID:27013793
Background: The prolonged use of antibiotic viz., tetracycline, quinolones, ampicillin, etc., to reduce the infection of cholera, may failed due to the emergence of new Vibrio cholerae antibiotics resistant strains. Moreover, these antibiotics even restricted for patient suffering from severe dehydration. Hence, there is a call to find an alternative therapeutics against V. cholerae. The natures serve different herbs in its lap which might contain several natural therapeutic compounds almost all diseases. Computer-aided designing is the initial steps for screening the novel inhibitors. Objective: To identify and evaluate natural compounds with low side effects with high efficacy against V. cholerae has been done. Materials and Methods: In silico screening, absorption, digestion, metabolism, and excretion (ADME), and docking of herbal compounds have been performed on to the target ToxT (transcriptional activator of V. cholerae). The compound with good ADME properties and drug-likeness property were subjected to docking. Results: From 70 herbal compounds, some compounds such as aloin, campesterol, lupeol, and ursolic acid showed a violation of the rule of five and compounds such as lupeol and beta carotene showed negative binding energy. Luteolin, catechin, brevifolin, etc., compounds were selected based on ADME, drug-likeness property, and docking studies. Conclusion: Two compounds named catechin and luteolin showed better inhibition properties against ToxT and good ADME and drug-likeness property were selected as a better lead molecule for drug development in future. The Genetic Optimization for Ligand Docking fitness score for catechin is 48.74 kcal/mol and luteolin 38.12 kcal/mol.
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In vitro cytotoxic activities and molecular mechanisms of angelica shikokiana extract and its isolated compounds
Amira Mira, Kuniyoshi Shimizu
December 2015, 11(44):564-569
DOI:10.4103/0973-1296.172962  PMID:27013795
Background: Angelica shikokiana is a Japanese medicinal herb that is included among food and drug preparations protecting against cancer; however, there is no previous report about the cytotoxicity of A. shikokiana or its bioactive compounds. Objective: This study was designed to investigate the cytotoxic activities of A. shikokiana methanol extract (AME) and its isolated compounds and to identify the molecular mechanisms of the cytotoxicity. Materials and Methods: Cytotoxicity and selectivity was investigated by measuring the IC 50 values on five cancer cell lines; human hepatocellular carcinoma, rhabdomyosarcoma (RD), colorectal carcinoma, human epithelioma and human breast adenocarcinoma and one normal cell line; human lung fibroblasts. The effects on tubulin polymerization and histone deacetylase 8 (HDAC8), were examined to determine the mechanism of cytotoxicity. Docking study was designed to examine the binding affinity to the target molecules. Results: Methanol extract and some of its isolated coumarins and flavonoids showed potent, selective cytotoxicity against cancer cell lines. AME and all isolated compounds inhibited tubulin polymerization. Angelicin and kaempferol-3-O-rutinoside were the most active compounds. Phenolic compounds and furanocoumarins showed binding affinity to colchicine binding site rather than the vinblastine binding site of tubulin microtubules. On the other side, quercetin, kaempferol, luteolin, chlorogenic acid, and methyl chlorogenate exhibited the strongest activity against HDAC8 and the highest affinity to trichostatin A binding site. Conclusion: These findings provide the first scientific evidence of the cytotoxicity of AME through inhibition of tubulin polymerization and HDAC8 activity through its coumarin and flavonoid content.
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In silico analysis for predicting fatty acids of black cumin oil as inhibitors of P-glycoprotein
Babar Ali, Qazi Mohd Sajid Jamal, Showkat R Mir, Saiba Shams, Naser A Al-Wabel, Mohammad A Kamal
December 2015, 11(44):606-610
DOI:10.4103/0973-1296.172969  PMID:27013802
Background: Black cumin oil is obtained from the seeds of Nigella sativa L. which belongs to family Ranunculaceae. The seed oil has been reported to possess antitumor, antioxidant, antibacterial, anti-inflammatory, hypoglycemic, central nervous system depressant, antioxidant, and immunostimulatory activities. These bioactivities have been attributed to the fixed oil, volatile oil, or their components. Seed oil consisted of 15 saturated fatty acids (17%) and 17 unsaturated fatty acids (82.9%). Long chain fatty acids and medium chain fatty acids have been reported to increase oral bioavailability of peptides, antibiotics, and other important therapeutic agents. In earlier studies, permeation enhancement and bioenhancement of drugs has been done with black cumin oil. Objective: In order to recognize the mechanism of binding of fatty acids to P-glycoprotein (P-gp), linoleic acid, oleic acid, margaric acid, cis-11, 14-eicosadienoic acid, and stearic acid were selected for in silico studies, which were carried out using AutoDock 4.2, based on the Lamarckian genetic algorithm principle. Materials and Methods: Template search with BLAST and HHblits has been performed against the SWISS-MODEL template library. The target sequence was searched with BLAST against the primary amino acid sequence of P-gp from Rattus norvegicus. Results: The amount of energy needed by linoleic acid, oleic acid, eicosadienoic acid, margaric acid, and stearic acid to bind with P-gp were found to be − 10.60, −10.48, −9.95, −11.92, and − 10.37 kcal/mol, respectively. The obtained data support that all the selected fatty acids have contributed to inhibit P-gp activity thereby enhances the bioavailability of drugs. Conclusion: This study plays a significant role in finding hot spots in P-gp and may offer the further scope of designing potent and specific inhibitors of P-gp.
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Nitric oxide production inhibition and anti-mycobacterial activity of extracts and halogenated sesquiterpenes from the Brazilian red alga laurencia dendroidea J. Agardh
Thatiana Lopes Biá Ventura, Fernanda Lacerda da Silva Machado, Marlon Heggdorne de Araujo, Lísia Mônica de Souza Gestinari, Carlos Roland Kaiser, Francisco de Assis Esteves, Elena B Lasunskaia, Angélica Ribeiro Soares, Michelle Frazão Muzitano
December 2015, 11(44):611-618
DOI:10.4103/0973-1296.172972  PMID:27013803
Background: Red algae of the genus Laurencia J. V. Lamouroux are a rich source of secondary metabolites with important pharmacological activities such as anti-tumoral, anti-inflammatory, anti-fungal, anti-viral, anti-leishmanial, anti-helminthic, anti-malarial, anti-trypanosomal, anti-microbial as well as anti-bacterial against Mycobacterium tuberculosis. Objective: In the present study, we evaluated the inhibition of nitric oxide (NO) and tumor necrosis factor-a production and the anti-mycobacterial activity of crude extracts from the red Alga Laurencia dendroidea (from the South-Eastern coast of Brazil). Halogenated sesquiterpenes elatol (1), obtusol (2) and cartilagineol (3), previously isolated from this Alga by our group, were also studied. Materials and Methods: The lipopolysaccharide-activated macrophage cells (RAW 264.7) were used as inflammation model. Cytotoxic effect was determined using a commercial  lactate dehydrogenase (LDH) kit and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The growing Mycobacterium inhibition was verified against Mycobacterium bovis Bacillus Calmette-Guιrin and M. tuberculosis H 37 Rv strains. Results: The crude extract from Alga collected at Angra dos Reis, RJ, Brazil, was the most active inhibitor of both mycobacterial growth (half maximal inhibitory concentration [IC 50 ] 8.7 ± 1.4 mg/mL) and NO production by activated macrophages (IC 50 5.3 ± 1.3 mg/mL). The assays with isolated compounds revealed the anti-mycobacterial activity of obtusol (2), whereas (-)-elatol (1) inhibited the release of inflammatory mediators, especially NO. To our knowledge, this is the first report describing an anti-mycobacterial effect of L. dendroidea extract and demonstrating the association of this activity with obtusol (2). Conclusion: The described effects of active compounds from L. dendroidea are promising for the control of inflammation in infectious diseases and specifically, against mycobacterial infections associated with exacerbated inflammation.
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Phytochemical analysis on quantification and the inhibitory effects on inflammatory responses from the fruit of xanthii fructus
Sae-Rom Yoo, Chang-Seob Seo, Na-Ri Lee, Hyeun-Kyoo Shin, Soo-Jin Jeong
December 2015, 11(44):585-591
DOI:10.4103/0973-1296.172966  PMID:27013799
Objective: Xanthii fructus (Compositae) is a traditional herbal medicine used for treating headache, toothache, pruritus, empyema, and rhinitis. In this study of the quality control of X. fructus, we performed simultaneous analysis of nine marker compounds: Protocatechuic acid (1), chlorogenic acid (2), caffeic acid (3), 4,5-dicaffeoylquinic acid (4), ferulic acid (5), 3,5-dicaffeoylquinic acid (6), 1,3-dicaffeoylquinic acid (7), 1,4-dicaffeoylquinic acid (8), and 4,5-dicaffeoylquinic acid (9). Materials and Methods: Nine components were separated using reversed-phase SunFire™ C 18 analytical column and analyzed using high-performance liquid chromatography. We examined the biological effects of the nine marker compounds by determining their anti-inflammatory activities in the murine macrophage cell line RAW 264.7. Results: Among the nine marker compounds, eight significantly inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor-alpha (TNF-a) production. 1, 3, 5 had significant inhibitory effects on LPS-induced prostaglandin E 2 (PGE 2 ) production in RAW 264.7 cells. None of the tested marker compounds had a significant effect on interleukin-6 production in LPS-treated RAW 264.7 cells. Our data demonstrated that each marker compound from X. fructus exerts anti-inflammatory activity by targeting different inflammation-related pathways such as the TNF-a or PGE 2 pathway. Conclusion: Further experiments using in vitro and in vivo models are needed to identify the mechanisms responsible for the anti-inflammatory properties of each marker compound.
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Effects of aronia melanocarpa fruit juice on isolated rat hepatocytes
Magdalena Kondeva-Burdina, Stefka Valcheva-Kuzmanova, Tsvetelina Markova, Mitka Mitcheva, Anna Belcheva
December 2015, 11(44):592-597
DOI:10.4103/0973-1296.172967  PMID:27013800
Background: Aronia melanocarpa (Michx.) Elliot fruits are very rich in polyphenols - procyanidins, flavonoids, and phenolic acids. Objective: On rat hepatocytes, isolated by two-stepped collagenase perfusion, we investigated the effect of A. melanocarpa fruit juice (AMFJ) in two models of liver toxicity caused by (i) metabolic bioactivation of carbon tetrachloride (CCl 4 ), and (ii) tert-butyl hydroperoxide (t-BuOOH)-induced oxidative stress. Materials and Methods: Isolated rat hepatocytes are a suitable model for hepatotoxicity studies. We determined the main parameters of the functional and metabolic status of rat hepatocytes: Cell viability (measured by trypan blue exclusion) and the levels of lactate dehydrogenase (LDH), reduced glutathione (GSH), and malondialdehyde (MDA). These parameters were used to investigate the protective effects of AMFJ in the two toxicity models. The effects of AMFJ were compared with those of silymarin. The cells were treated either with AMFJ or silymarin at increasing concentrations of 5 mg/ml, 10 mg/ml, 30 mg/ml, 50 mg/ml, and 100 mg/ml which were used for measuring of IC 50 . Results: In both toxicity models - CCl 4 and t-BuOOH, AMFJ showed statistically significant cytoprotective and antioxidant activities. AMFJ prevented the loss of cell viability and GSH depletion, decreased LDH leakage and MDA production. The effects of AMFJ at the concentrations of 5, 10, 30, and 50 mg/ml were similar to those of the same concentrations of silymarin, while the effect of the highest AMFJ concentration of 100 mg/ml was higher than that of the same silymarin concentration. The effects were concentration-dependent and more prominent in the t-BuOOH model, compared to those in the CCl 4 model. Conclusion: The cytoprotective and antioxidant effects of AMFJ established in this study might be due to its polyphenolic ingredients, which could influence the cytochrome P450-mediated metabolism of the experimental hepatotoxic substances (CCl 4 and t-BuOOH) and could act as free radical scavengers. The stronger effects of the highest AMFJ concentration in comparison with that of silymarin were possibly due to the combined presence of different polyphenols in the juice.
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Phenolic alkaloids from Menispermum dauricum inhibits BxPC-3 pancreatic cancer cells by blocking of Hedgehog signaling pathway
Zhong-guang Zhou, Chao-ying Zhang, Hong-xin Fei, Li-li Zhong, Yun Bai
October-December 2015, 11(44):690-697
DOI:10.4103/0973-1296.165548  PMID:26600712
Background: The Hedgehog (Hh) signaling pathway plays an important role in pancreatic cancer (PC) cells. Phenolic alkaloids from Menispermum dauricum (PAMD), a traditional Chinese medicine used for the treatment of immune disorders, have been reported to have antitumor activity recently. Objective: To investigate the efficacy and mechanism of PAMD against PC cell BxPC-3. Materials and Methods: F assay was used to assess cell proliferation inhibition of PAMD; the apoptotic induction and cell cycle arrest was detected by flow cytometry; the BxPC-3 xenograft was established to evaluate the tumor growth inhibition of PAMD; hematoxylin-eosin staining was applied to analyze the pathological morphology of tumor tissues; immunohistochemistry (IHC) and Western blot was adopted to detect the protein levels; quantitative real-time polymerase chain reaction was used to determine the mRNA expressions. Results: PAMD shows time-and dose-dependent proliferation inhibition on the BxPC-3 cell, induced G0/G1 phase arrest and cell apoptosis in vitro. PAMD also showed better inhibition of tumor growth and a preferable safety profile compared with chemotherapeutic regimen 5-fluoro-2, 4 (1 H, 3 H) pyrimidinedione in BxPC-3 xenograft in vivo. Furthermore, PAMD directly decreases the protein and mRNA levels of Sonic Hedgehog (Shh) and its downstream transcription factor Gli-1 in the BxPC-3 tumor tissues. Conclusion: The treatment of PAMD displayed Hh signaling pathway blockade through decreasing the protein and mRNA levels of Shh and its downstream transcription factor Gli-1, suggesting a promising strategy in treating human PC.
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Structure elucidation and anti-tumor activities of water-soluble oligosaccharides from Lactarius deliciosus (L. ex Fr.) Gray
Xiang Ding, Yiling Hou, Wanru Hou, Yuanxiu Zhu, Lei Fu, Hongqing Zhu
October-December 2015, 11(44):716-723
DOI:10.4103/0973-1296.165559  PMID:26600715
Background: Oligosaccharides are composed of a variable number of monosaccharide units and very important in the biologically diverse of biological systems. Materials and Methods: Crude water-soluble oligosaccharide was extracted from the fruiting bodies with water and then successively purified by DEAE-cellulose 52 and Sephadex G-100 column chromatography, yielding one major oligosaccharides fractions: LES-A. Structural features of Lactarius deliciosus (L. ex Fr.) Gray oligosaccharide (LDGO-A) were investigated by a combination of monosaccharide component analysis by thin layer chromatography, infrared spectra, nuclear magnetic resonance spectroscopy, scanning electron microscopy, and high-performance gel permeation chromatography analysis. Result: The results indicated that LDGO-A was composed of D-glucose and D-xylose, and the average molecular sizes was approximately 945 Da. The anti-tumor activity of LDGO-A was evaluated in vivo. The inhibitory rate in mice treated with 40 mg/kg LDGO-A can reach 40.02%, being the highest in the three doses, which may be comparable to mannatide. Histology of immune organs shows that the tissues arranged more regular and firmer, but the tumor tissue arranged looser in LDGO-A group than those in the control group. Meanwhile, there is no obvious damage to other organs, such as heart. The anti-tumor activity of the LDGO-A was usually believed to be a consequence of the stimulation of the cell-mediated immune response because it can significantly promote the lymphocyte and macrophage cells in the dose range of 100-400 μg/mL in vitro. LDGO-A also effected the expression of some housekeeping genes mRNA in S180 tumor. Conclusion: Accordingly, the LDGO-A might serve as an effective healthcare food and source of natural anti-tumor compounds.
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Effects of fermented Cordyceps sinensis on oxidative stress in doxorubicin treated rats
Rong Wu, Jian-Ping Gao, Hui-Lin Wang, Yan Gao, Qian Wu, Xiao-Hua Cui
October-December 2015, 11(44):724-731
DOI:10.4103/0973-1296.165562  PMID:26600716
Background: Cordyceps sinensis (CS) is one of the rare traditional Chinese herbs, only a very limited amount of natural CS is produced. Fermented CS, as a substitute for natural CS, is widely used in the field of supplementary medical treatment and health products. Its antagonistic effect on oxidative stress (OS) in vivo has not been investigated. Objective: Our aim was to investigate the antagonistic effect of fermented CS on OS in doxorubicin (DOX) treated rats and to compare the anti-OS effects in heart and liver tissues. Materials and Methods: OS rats were induced by tail-intravenous injection of DOX (total of 7.5 mg/kg), and then administered intragastrically with fermented CS (1.5 g/kg) for 4 weeks. At the end of the experiment, heart, liver and serum samples were taken for and biochemical analyses. Results: Fermented CS significantly increased the activities of glutathione peroxidase and catalase and the scavenging activity of O2 in serum, and the total superoxide dismutase activity in cardiac tissue; reduced the malondialdehyde content in liver and cardiac tissues. Conclusion: Fermented CS can inhibit DOX-induced OS reactions, and the anti-OS effects have high selectivity to heart and liver, especially to heart. Thus, fermented CS may be a candidate used for the prevention against various cardiac diseases induced by OS.
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Species classification and bioactive ingredients accumulation of BaiJiangCao based on characteristic inorganic elements analysis by inductively coupled plasma-mass spectrometry and multivariate analysis
Li Wen-Lan, Zhang Xue, Yang Xin-Xin, Wang Shuai, Zhao Lin, Zhao Huan-Jun, Bao Yong-Rui, Ji Chen-Feng, Chen Ning, Xiang Zheng
October-December 2015, 11(44):756-763
DOI:10.4103/0973-1296.165577  PMID:26600721
Background: Patrinia scabiosaefolia Fisch and Patrinia villosa (Thunb.) Juss., two species herbs with the same Chinese name "BaiJiangCao", are important ancient herbal medicines widely used for more than 2000 years. The clinical application of two species herb is confused due to the difficult identification. Objective: The objective was to authenticate the species of BaiJiangCao and analyze the accumulation of bioactive ingredients based on characteristic inorganic elements analysis. Materials and Methods: Content of 32 inorganic elements in BaiJiangCao from different habitats were determined by inductively coupled plasma-mass spectrometry (ICP-MS), and the characteristic inorganic elements were picked to distinguish the species of the herb by principal component analysis and cluster analysis. Contents of two bioactive ingredients, luteoloside, and oleanolic acid, in the samples, were also analyzed by high-performance liquid chromatography method. Relationship between accumulation of bioactive ingredients and content of macroelements in BaiJiangCao was established by statistics. Results: A 4 macroelements (Na, Mg, K, Fe) in 32 determined inorganic elements were picked for characteristic inorganic elements. Content of Na, Mg, K and Fe showed positive correlations with that of luteoloside, content of Na, Mg showed positive correlations with that of oleanolic acid, but content of K and Fe showed negative correlations with that of oleanolic acid. Conclusion: It is for the first time to utilize the characteristic inorganic elements as an index to classify the herb species by the method of ICP-MS and multivariate analysis. And it is also the first report to investigate the influence of inorganic elements in herb on the accumulation of bioactive components which could affect the pharmacological efficacy of the herb medicine. And this method could also be utilized in research of corresponding aspects.
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In vitro α-amylase and α-glucosidase inhibitory effects and cytotoxic activity of Albizia antunesiana extracts
Talent Chipiti, Mohammed Auwal Ibrahim, Moganavelli Singh, Md. Shahidul Islam
October 2015, 11(44):231-236
DOI:10.4103/0973-1296.166018  PMID:26664010
Context: Diabetes mellitus is a chronic disease, and its incidence is tremendously increasing globally. Decreasing postprandial hyperglycemia by retarding glucose absorption through inhibiting carbohydrates digesting enzymes (α-amylase and α-glucosidase) is one of many approaches used for the management of this disease.Objectives: The leaf and root aqueous and ethanol extracts of Albizia antunesianawere investigated for α-amylase and α-glucosidase inhibitory and cytotoxic activity in vitro.Materials and Methods: The α-amylase and α-glucosidase activities were measured in the presence of aqueous and ethanol extracts of the plant parts using starch and p-nitrophenyl-D-glucopyranoside as substrates respectively. Furthermore, cytotoxic effects of the extracts were investigated on HEK (human embryonic kidney) 293 cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay.Results: The results showed that ethanolic root extract of A. antunesianahad mild α-amylase and strong α-glucosidase inhibitory activity with half-maximal inhibitory concentration values of 30.68 and 4.35 µg/mL, respectively. The aqueous root extract showed mild α-glucosidase but no α-amylase inhibitory activity. Cytotoxicity studies on the extracts using the MTT assay revealed that the ethanolic (leaf and root) extracts were relatively nontoxic at tested concentrations on the HEK 293 cell lines. However, the aqueous extracts (leaf and root) were cytotoxic at concentrations above 50 µg/mL.Conclusion: Data from this study suggest that the ethanolic root extract of A. antunesianapossess in vitro α-amylase and α-glucosidase inhibitory activities and are not cytotoxic at least in an in vitro condition.
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Poncirus trifoliata Rafin. induces the apoptosis of triple-negative breast cancer cells via activation of the c-Jun NH(2)-terminal kinase and extracellular signal-regulated kinase pathways
Hye-Yeon Han, Mi Heon Ryu, Yonghae Son, Guemsan Lee, Seung-Hwa Jeong, Hyungwoo Kim
October 2015, 11(44):237-243
DOI:10.4103/0973-1296.166056  PMID:26664011
Background: Poncirus trifoliataRafin. is a traditional medicine with known anti-inflammatory and anti-cancer properties. Traditionally, it is used to control chronic inflammation, allergy and gastrointestinal diseases such as digestive ulcers gastritis in China, Japan, and Korea. Objectives: To evaluate the apoptosis-inducing activity of a P. trifoliatamethanol extract (MEPT) and elucidate the molecular mechanisms. Materials and Methods: The anti-cancer effect of MEPT and its underlying mechanisms were investigated in breast cancer cells using 3,4,5-dimethyl N-methylthiazol-2-yl-2, 5-d-phenyl tetrazolium bromide assay, cell cycle analysis, and western blotting. Results: MEPT suppressed the proliferation of MDA-MB-231 cells with inhibition dose 50% value of 119.44 μg/mL at 24 h, which have features typical of triple-negative breast cancer cells. MEPT also altered the characteristic features of the MDA-MB-231 cells and increased the proportion of cells undergoing sub-G1 arrest. In addition, MEPT increased levels of caspase 8 and 3 in MDA-MB-231 cells, whereas caspase 9 was not detected. In addition, MEPT-induced tumor necrosis factor receptor (TNFR) and TNFR type 1-associated death domain (TRADD) protein and the activations of c-Jun NH(2)-terminal kinase (JNK) and extracellular signal-regulated kinases (ERK). Conclusion: Our results indicate that MEPT has chemotherapeutic potential in triple-negative breast cancer and that at the molecular level its effects are derived from the activations of TNFR and of the mitogen-activated protein kinase pathway.
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High performance liquid chromatography time of flight electrospray ionization mass spectrometry for quantification of sesquiterpenes in Chrysanthemi indici Flos active extract
Ling Fu, Pan Wang, Yiqun Sun, Yangyang Wang, Jing Zhao, Yuting Ye, Yanbin Zhang, Yuefeng Bi
October-December 2015, 11(44):740-744
DOI:10.4103/0973-1296.165574  PMID:26600718
Background: Chrysanthemi indici Flos, a traditional herbal medicine is used to clearing heat-toxicity, removing the liver fire, and improving eyesight. In our preliminary work, an  active extract of CTC in C. An indici Flos with anti-hepatitis B virus and liver protective activity was found by HepG2.2.1.5 test and experiment of protein synthesis in mice's injured liver. In this work, we aimed to study the active faction CTC further by qualitative and quantitative analysis method. Materials and Methods: High performance liquid chromatography time of flight electrospray ionization mass spectrometry (HPLC TOF ESI-MS) analysis method of the CTC was established. Cumambrin A and angeloylcumambrin B in CTC were analyzed by high performance liquid chromatography-ultraviolet-evaporative light scattering detector (HPLC-UV-ELSD) analysis methods. A binary gradient elution program was conducted for chromatographic separation with acetonitrile (A) and ultrapure water (B) as follows: 0-10 min, 42-46% A; 10-20 min, 46-55% A; 20-25 min, 55-60% A; and 25-35 min, 60-75% A. The column temperature and UV wavelength were set at 30°C and 205 nm. Result: Ten constituents including (3R, 5R, 6S, 7S, 10R)-7-(2-hydroxy-2-propyl)-10-methyl-4-methyleneperhy, dronaphthal-ene-3, 5, 6-triol acetone solvate; (+)-edusmance-4, (14)-ene-11, 13-diol; linarin; luteolin; apigenin; tricin; 5, 3',4'- trimethyl-6,7-dimethoxy flavones; cumambrin A; acacetin; and angeloylcumambrin B in CTC were identified by HPLC TOF ESI-MS. The contents of sesquiterpenes in CTC were decreased by storing years. Conclusions: The results showed that both UV and ELSD methods were feasible, accurate, and the determination results were in good consistency. The contents of two sesquiterpenes decreased with storing years. Two sesquiterpenes could be used as quality control for C. indici flos CTC.
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A study of the substance dependence effect of the ethanolic extract and iridoid-rich fraction from Valeriana jatamansi Jones in mice
Lin Yu, Xu Ke-ke, Chen Chao-yong, Zhang Rui-tong, Lan Ming, Li Shao-hua, Pan Ling-zhen, Zhang Tian-e, Yan Zhi-yong
October-December 2015, 11(44):745-749
DOI:10.4103/0973-1296.165575  PMID:26600719
Background: Recently we found the ethanolic extract and iridoid-rich fraction from Valeriana jatamansi Jones, which is a traditional Chinese medicine exhibited anxiolytic properties. Objective: This study aims to the substance dependence effect of the ethanolic extract and iridoid-rich fraction. Materials and Methods: The study included two experiments: Mice were given orally with ethanolic extract for 12 weeks or iridoid-rich fraction for 16 weeks in experiment I and experiment II, respectively. Diazepam was used as a control drug and the normal mice groups were administered with 0.5% carboxymethyl cellulose Na in both experiments. All groups were administered twice daily. Natural withdrawal symptoms, withdrawal-induced body weight change, audiogenic tail-erection test (in experiment I), and pentylenetetrazol (PTZ)-induced convulsion test (in experiment II) were measured. Results: (1) Compared to normal group in both experiments, the diazepam-treated group exhibited obvious withdrawal symptoms of tail-erection, irritability, teeth chattering, etc; the body weight of them after withdrawal had a period of significant loss (P < 0.05 or P < 0.01); and the ratios of tail-erection and seizure in two experiments were improved significantly when mice were induced by mixer noise ringtone (experiment I) or PTZ (experiment II) (P < 0.05 or P < 0.01).(2) In experiment I and II, there were no significant differences between mice that received ethanolic extract or iridoid-rich fraction and normal group in terms of natural withdrawal symptoms and withdrawal-induced body weight change (P > 0.05); in audiogenic tail-erection test, it found that the significant difference compared with normal group was just in ethanolic extract 900 mg/kg dose group on week 8 (P < 0.05); in PTZ-induced convulsion test, mice in iridoid-rich fraction groups had a slightly tail-erection and seizure, all results of them were with no significant difference compare to normal mice (P > 0.05), while significant lower than diazepam group (P < 0.01). Conclusion: (1) The two experiments successfully established the physical dependence of diazepam by gradually increasing the dose.(2)There were just a few mice received with ethanolic extract for 12 weeks or iridoid-rich fraction for 16 weeks appearing some slight withdrawal symptoms after precipitated withdrawal, but it didn't show significant difference compared to normal mice. Therefore, these indicated that the risks of potential drug dependence about ethanolic extract and iridoid-rich fraction were far lower than that of diazepam.
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Selectivity of Pinus sylvestris extract and essential oil to estrogen-insensitive breast cancer cells Pinus sylvestris against cancer cells
Nguyen Thi Hoai, Ho Viet Duc, Do Thi Thao, Anne Orav, Ain Raal
October 2015, 11(44):290-295
DOI:10.4103/0973-1296.166052  PMID:26664017
Background: So far, the anticancer action of pine tree extracts has mainly been shown for the species distributed widely around the Asian countries. Objective: Therefore, this study was performed to examine the potential cytotoxicity of Scots pine (Pinus sylvestrisL.) native also to the European region and growing widely in Estonia. Materials and Methods: The cytotoxic activity of methanol extract and essential oil of Scots pine needles was determined by sulforhodamine B assay in different human cancer cell lines. Results: This needle extract was found to suppress the viability of several human cancer cell lines showing some selectivity to estrogen receptor negative breast cancer cells, MDA-MB-231(half maximal inhibitory concentration [IC50] 35 μg/ml) in comparison with estrogen receptor-positive breast cancer cells, MCF-7 (IC50 86 μg/ml). It is the strongest cytotoxic effect at all measured, thus far for the needles and leaves extracts derived from various pine species, and is also the first study comparing the anticancer effects of pine tree extracts on molecularly different human breast cancer cells. The essential oil showed the stronger cytotoxic effect to both negative and positive breast cancer cell lines (both IC50 29 μg/ml) than pine extract (IC50 42 and 80 μg/ml, respectively). Conclusion: The data from this report indicate that Scots pine needles extract and essential oil exhibits some potential as chemopreventive or chemotherapeutic agent for mammary tumors unresponsive to endocrine treatment.
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Curcumin half analog modulates interleukin-6 and tumor necrosis factor-alpha in inflammatory bowel disease
Phani Krishna Kondamudi, Hemalatha Kovelamudi, Pawan G Nayak, Mallikarjuna Chamallamudi Rao, Rekha Raghuveer Shenoy
October 2015, 11(44):296-302
DOI:10.4103/0973-1296.165991  PMID:26664018
Background: The present study was aimed at examining the effect of dehydrozingerone (DHZ), half analogue of curcumin which is the active constituent of turmeric (Curcuma longa) in the di-nitrochlorobenzene (DNCB) induced model for inflammatory bowel disease (IBD). Materials and Methods: Male Wistar rats (200–220 g) were divided into four groups (n = 6). Chemical induction of IBD was done by sensitizing with 300 µL of 20 g/L of DNCB (in acetone) onto the nape of rats for 14 days followed by intra-colonic instillation of 250 µL of DNCB (0.1% DNCB in 50% alcohol) solution on day 15. Rats in Group 1 (normal control) and Group 2 (DNCB control) were treated with vehicle. Rats in Group 3 were treated with DHZ (100 mg/kg, p.o.; 8 days) and Group 4 animals were treated with sulfasalazine (SS) (100 mg/kg, p.o.; 8 days). On 24th day, the rats were killed, colon removed and the macroscopic, biochemical, and histopathological evaluations were performed. Results: The levels of myeloperoxidase, thiobarbituric acid reactive substrate, and nitrite increased significantly (P < 0.05) in the DNCB group whereas reduced significantly in the DHZ and SS treated groups. Serum nitrite levels were found to be insignificant between the different groups. Interleukin-6, tumor necrosis factor-alpha level was significantly high in the DNCB group. Conclusion: These findings show that DHZ can be a promising molecule for the treatment of IBD.
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Neuroprotective compounds of Tilia amurensis
Bohyung Lee, Jin Bae Weon, Min Rye Eom, Youn Sik Jung, Choong Je Ma
October 2015, 11(44):303-307
DOI:10.4103/0973-1296.166065  PMID:26664019
Background: Tilia amurensis (Tiliacese) has been used for anti-tumor and anti-inflammatory in Korea, China, and Japan. Objective: In this study, we isolated five compounds from T. amurensis and determined whether protected neuronal cells against glutamate-induced oxidative stress in HT22 cells. Materials and Methods: Compounds were isolated using chromatographic techniques including silica gel, Sephadex LH-20 open column and high performance liquid chromatography analysis, and evaluated neuroprotective effect in HT22 cells by 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay. Results: β-D-fructofuranosyl α-D-glucopyranoside (1), (-)-epicatechin (2), nudiposide (3), lyoniside (4), and scopoletin (5) were isolated by bioactivity-guided fractionation from the ethyl acetate fraction of T. amurensis. Among them, (-)-epicatechin, nudiposide, lyoniside, and scopoletin had significant neuroprotective activities against glutamate-injured neurotoxicity in HT22 cells. Conclusion: These results demonstrated that compound two, three, four, and five have a pronounced protective effect against glutamate-induced neurotoxicity in HT22 cells.
  - 1,022 16
Reversed-phase-liquid chromatography method for separation and quantification of gallic acid from hydroalcoholic extracts of Qualea grandiflora and Qualea parviflora
Mariana L de Mesquita, Waleska F Leão, Magda R. A. Ferreira, José E de Paula, Laila S Espindola, Luiz A. L. Soares
October 2015, 11(44):316-321
DOI:10.4103/0973-1296.166062  PMID:26664021
Background: Qualea parvifloraand Qualea grandiflora (Vochysiaceae), commonly known in Brazil as "pau-terra" and "pau-terrinha," respectively, have been widely used in the treatment of ulcer and gastritis. These therapeutic effects are attributed to various compounds present in the plants, including phenolic compounds such as gallic acid, due to their important antioxidant activity. Objective: The aim of the present study was to validate a high performance liquid chromatography with diode array detection (HPLC-DAD) method for the quantitative determination of gallic acid in the stem bark of Q. parviflora and Q. grandiflorahydroalcoholic extracts. Materials and Methods: The chromatography analysis was successfully achieved on a Dionex column, Acclaim® 120 (250 mm × 4.60 mm, 5 µm) with a gradient elution of water and methanol at a flow rate of 0.8 mL/min and ultraviolet detection at 280 nm. Results: The validation data, including linearity, precision, specificity, accuracy and robustness of this method demonstrated good reliability and sensitivity. Conclusion: The method is able to quantify gallic acid in the stem bark of both species. What is more, the chromatographic peaks showed good resolution and there are also the advantages of easy sample preparation and a short time between each injection.
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Herbal therapy: A review of emerging pharmacological tools in the management of diabetes mellitus in Africa
Cromwell Mwiti Kibiti, Anthony Jide Afolayan
October 2015, 11(44):258-274
DOI:10.4103/0973-1296.166046  PMID:26664014
Background: Diabetes mellitus is a chronic physiological glucose metabolic disorder. It has affected millions of people all over the world thereby having a significant impact on quality of life. The management of diabetes includes both nonpharmacological and conventional interventions. Drawbacks in conventional therapy have led to seeking alternative therapy in herbal medicine. Therefore, the need to review, elucidate and classify their mode of action in therapy for diabetes disease arises. Materials and Methods: Comprehensive literature reports were used to review all conventional agents and herbal therapy used in the management of diabetes. An online database search was conducted for medicinal plants of African origin that have been investigated for their antidiabetic therapeutic potentials. Results: The results showed that of the documented sixty five plants used, fourteen inhibit intestinal absorption of glucose, three exhibit insulin-mimetic properties, seventeen stimulate insulin secretion from pancreatic beta cells, twelve enhance peripheral glucose uptake, one promotes regeneration of beta-cell of islets of Langerhans, thirteen ameliorate oxidative stress and twenty induces hypoglycemic effect (mode of action is still obscure). Thirteen of these plants have a duplicate mode of actions while one of them has three modes of actions. These agents have a similar mechanism of action as the conventional drugs.Conclusion: In conclusion, antidiabetic activities of these plants are well established; however, the molecular modulation remains unknown. It is envisaged that the use of herbal therapy will promote good health and improve the status of diabetic patients.
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Cissus quadrangularis Linn. Stem ethanolic extract liberates reactive oxygen species and induces mitochondria mediated apoptosis in KB cells
Saba Sheikh, Sahabjada Siddiqui, Anupam Dhasmana, Safia , Ejazul Haque, Mohammed Kamil, Mohtashim Lohani, Mohammad Arshad, Snober Shabnam Mir
October 2015, 11(44):365-374
DOI:10.4103/0973-1296.168972  PMID:26929569
Background: Cissus quadrangularis Linn. (CQ) commonly known as Hadjod (Family: Vitaceae) is usually distributed in India and Sri Lanka and contains several bioactive compounds responsible for various metabolic and physiologic effects. Objective: In this study, the biological effects of CQ ethanolic extract were evaluated by in vitro and supported by in silico analysis on KB oral epidermoid cancer cell line. Materials and Methods: Anti-cancer potential of ethanolic extract of CQ stem against KB oral epidermoid cancer cells was evaluated in terms of morphological analysis, nuclei staining, liberation of reactive oxygen species (ROS), cell cycle arrest, mitochondrial membrane potential (MMP) and p53 and Bcl-2 protein expression which reveal the induction of apoptosis along with supporting in silico analysis. Results: Ethanolic extract of CQ stem contains various bioactive compounds responsible for cancer cell morphological alterations, liberation of ROS, G1 phase cell cycle arrest and decreased MMP along with up-regulation of p53 and down-regulation of Bcl-2. By employing in silico approach, we have also postulated that the CQ extract active constituents sequester Bcl-2 with higher affinity as compared to p53, which may be the reason for induction of growth arrest and apoptosis in KB cells. Conclusion: Our data indicate that the CQ extract has a remarkable apoptotic effect that suggests that it could be a viable treatment option for specific types of cancers.
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Stability, clinical efficacy, and antioxidant properties of Honeybush extracts in semi-solid formulations
Gezina S. F. W. Gerber, Lizelle T Fox, Minja Gerber, Jan du Preez, Sterna van Zyl, Banie Boneschans, Jeanetta du Plessis
October 2015, 11(44):337-351
DOI:10.4103/0973-1296.166063  PMID:26664024
Background: Honeybush extracts (Cyclopia spp.) can be incorporated into skin care products to treat conditions such as skin dryness and can function as an anti-oxidant. Objective: To formulate Honeybush formulations and test it for antioxidant activity, skin penetration, and skin hydrating effects. Materials and Methods: Semi-solid formulations containing either Cyclopia maculata (2%) or Cyclopia genistoides (2%) underwent accelerated stability studies. Membrane release studies, Franz cell skin diffusion and tape stripping studies were performed. Antioxidant potential was determined with the 2-thiobarbituric acid-assay and clinical efficacy studies were performed to determine the formulations' effect on skin hydration, scaliness, and smoothness after 2 weeks of treatment on the volar forearm. Results: The formulations were unstable over 3 months. Membrane release, skin diffusion studies, and tape stripping showed that both formulations had inconclusive results due to extremely low concentrations mangiferin and hesperidin present in the Franz cell receptor compartments, stratum corneum-epidermis, and epidermis-dermis layers of the skin. Honeybush extracts showed antioxidant activity with concentrations above 0.6250 mg/ml when compared to the toxin; whereas mangiferin and hesperidin did not show any antioxidant activity on their own. The semisolid formulations showed the potential to emit their own antioxidant activity. Both formulations improved skin smoothness, although they did not improve skin hydration compared to the placebos. C. maculata reduced the skin scaliness to a larger extent than the placebos and C. genistoides. Conclusion: Honeybush formulations did not penetrate the skin but did, however, show antioxidant activity and the potential to be used to improve skin scaliness and smoothness.
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Toxicogenomics of Phenylhydrazine Induced Hematotoxicity and its Attenuation by Plumbagin from Plumbago zeylanica
Pooja Shukla, RK Singh
October 2015, 11(44):380-387
DOI:10.4103/0973-1296.168983  PMID:26929571
Background: High regenerative and proliferative capacity of blood and its components renders it to be at higher risk of adverse drug reactions (ADRs) which are manifested in several treatment regimens against various ailments such as cancers, viral diseases, and several metabolic disorders. Objective: It is prudent to come up with some therapeutic entity that can prevent this damage and protects the blood from these ADRs. Materials and Methods: We examined protective effects of Plumbago zeylanica (PZ) and its active constituent plumbagin (PL) on Sprague Dawley (SD) rats using a phenylhydrazine (Phz) induced hematotoxicity model. Hemoglobin (Hgb), red blood cells (RBCs), mean corpuscular volume, mean corpuscular Hgb (MCH), MCH concentration (MCHC), leukocytes and platelets were studied. Anti-oxidant enzymes superoxide dismutases 2 and 3 (SODs) and nuclear erythroid 2 p45-related factor 1 and 2 (Nfer-1 and 2) were also studied using quantitative real-time polymerase chain reaction (PCR). Results: In Phz treated rats, the positive hematotoxic response was obtained in terms of deviated endpoints of blood indices. In PLtreated groups protective response was obtained in terms of normal endpoints of blood indices. In PCR studies, we observed the similar trend. Thus, it can be postulated that PL exerts its protective effects via modulation of anti-oxidant enzymes. Conclusion: The study proves that PL can be employed against combatting the ADRs associated with several therapeutic treatment regimens. Similar studies employing such pharmacological entities and their combinations may further prove to be effective against ADRs, especially in the context of blood cells.
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The isolation, characterization and preclinical studies of metal complex of Thespesia populnea for the potential peroxisome proliferator-activated receptors-γ agonist activity
Mohini Ashok Phanse, Manohar Janardhan Patil, Konde Abbulu
October 2015, 11(44):434-438
DOI:10.4103/0973-1296.168984  PMID:26929578
Background: Diabetes mellitus is an international public health problem since ancient days. The condition is predominantly more severe in developing countries like India where, life is more sedentary due to the even changing lifestyles in this fast-paced global scenario. Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes mellitus in India for years. The aim of this work is to explore the anti-diabetic activity of the isolated compound. Materials and Methods: The sesquiterpene isolated from hexane fraction of bark of T. populnea modified synthetically then identified by using analytical techniques such as electron paramagnetic resonance spectra for confirmation and the anti-diabetic activity was evaluated by anti-hyperglycemic, hypoglycemic potential. Result: In the present work, we have studied the anti-hyperglycemic and hypoglycemic activity of the vanadium complex in glucose loaded and normal animals were shown significantly decreased in plasma blood glucose level. The results derived from preclinical studies confirm the potential of new sesquiterpene. Conclusion: The findings could provide evidence regarding the anti-diabetic potential of T. populnea by lowering blood glucose level.
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Anti-inflammatory, Anti-estrogenic, and Anti-implantation activity of Bergia suffruticosa (Delile) Fenzl
Sandeep Kumar Bind, Mehul Jivrajani, Sheetal Anandjiwala, Manish Nivsarkar
October 2015, 11(44):407-413
DOI:10.4103/0973-1296.168973  PMID:26929574
Background: Bergia suffruticosa (Delile) Fenzl (Syn. Bergia odorata Edgew) (Elatinaceae family) is used traditionally to repair bones and is applied as a poultice on sores. It is also used for stomach troubles and as an antidote to scorpion stings. So far, very little scientific work has been reported to validate its ethnomedical uses in the alleviation of pain, bone repair, etc., Objective: This study was designed to explore the anti-inflammatory and anti-implantation potential of n-hexane extract of B. suffruticosa whole plant in mice along with identification of its chemical constituents. Materials and Methods: n-Hexane extract of B. suffruticosa whole plant was screened for acute and chronic anti-inflammatory activity followed by an anti-estrogenic activity. Eventually, n-hexane extract was tested for anti-implantation activity by exploiting markers of uterine receptivity, lipid peroxidation, and superoxide enzyme activity. The extract was administered orally at a dose of 100 mg/kg body weight in each study. Results: Thin layer chromatography fingerprint profile of n-hexane extract revealed the presence of lupeol and β-sitosterol. The n-hexane extract reduced the edema by 80% in acute inflammation, whereas it reduced edema to 75% on the 5th day in chronic inflammation. The n-hexane extract reduced elevated malonaldehyde level from 6 to 2.5 nmol/g × 10−5 and increased superoxide dismutase enzyme activity from 0 to 350 units/g in treated animals on the 5th day of pregnancy. Moreover, extract decreased uterine weight from 0.33 to 0.2 g in estradiol treated animals. Conclusion: These results indicate that n-hexane extract of B. suffruticosa is having potent anti-inflammatory, anti-estrogenic, and anti-implantation activity. This is the first report of all the pharmacological activities of B. suffruticosa mentioned above.
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Molecular docking and molecular dynamics to identify a novel human immunodeficiency virus inhibitor from alkaloids of Toddalia asiatica
R Priya, Rajendrarao Sumitha, C George Priya Doss, C Rajasekaran, S Babu, R Seenivasan, R Siva
October 2015, 11(44):414-422
DOI:10.4103/0973-1296.168947  PMID:26929575
Background: Acquired immunodeficiency syndrome caused by human immunodeficiency virus (HIV) is an immunosuppressive disease. Over the past decades, it has plagued human health due to the grave consequences in its harness. Objective: For this reason, anti-HIV agents are imperative, and the search for the same from natural resources would assure the safety. Materials and Methods: In this investigation we have performed molecular docking, molecular property prediction, drug-likeness score, and molecular dynamics (MD) simulation to develop a novel anti-HIV drug. We have screened 12 alkaloids from a medicinal plant Toddalia asiatica for its probabilistic binding with the active site of the HIV-1-reverse transcriptase (HIV-1-RT) domain (the major contributor to the onset of the disease). Results: The docking results were evaluated based on free energies of binding (ΔG), and the results suggested toddanol, toddanone, and toddalenone to be potent inhibitors of HIV-1-RT. In addition, the alkaloids were subjected to molecular property prediction analysis. Toddanol and toddanone with more rotatable bonds were found to have a drug-likeness score of 0.23 and 0.11, respectively. These scores were comparable with the standard anti-HIV drug zidovudine with a model score 0.28. Finally, two characteristic protein-ligand complexes were exposed to MD simulation to determine the stability of the predicted conformations. Conclusion: The toddanol-RT complex showed higher stability and stronger H-bonds than toddanone-RT complex. Based on these observations, we firmly believe that the alkaloid toddanol could aid in efficient HIV-1 drug discovery.
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Assessment of pharmacodynamic and pharmacokinetic interaction of aqueous extract of Cassia auriculata L. and metformin in rats
Hemnath Elango, Sivasankaran Ponnusankar, Sankar Sundaram
October 2015, 11(44):423-426
DOI:10.4103/0973-1296.168986  PMID:26929576
Background: Cassia auriculata L. (CA) leaf extract might increase the body's production of insulin thereby suppressing the elevated blood glucose and lipid levels in diabetic rats. CA has been used as dietary supplement in India from ancient times. Objective: The present study was to elucidate the synergistic pharmacodynamic (PD) and pharmacokinetic (PK) interaction of metformin (MT) with CA. Materials and Methods:A simple, precise reverse phase high performance liquid chromatography - UV detection mode method was developed to quantify MT in rat plasma. In PD interaction, streptozotocin (45mg/kg, intraperitoneally) induced diabetic Wistar rats weighing 180–250 g of either sex were randomized to receive MT (90 mg/kg, MT-HD), CA (500 mg/kg) separately and in combination of MT (90 mg/kg, MT-HD) + CA (500 mg/kg), and MT (45 mg/kg, MT-LD) + CA (500 mg/kg) (all oral) along with normal and diabetic control groups for 21 days. PK of MT was carried out in normal rats with preadministration of CA (500 mg/kg) for 14 days. Results: PD data showed reasonable blood glucose lowering effect of CA. The reduction of MT dose with combination of CA achieved a similar blood glucose lowering effect of MT alone. PK data showed enhanced time taken to achieve maximum plasma concentration (Cmax), area under the curve (AUC0-t), and Cmaxin combination group of MT (90mg/kg) and CA (500mg/kg), and reduction of MT dose in Group III had a reduced Cmaxand AUC0-tcompared to MT alone treated groups. Conclusion: Co-administration of CA with MT at varying dose showed a synergistic herb-drug interaction. Thus using the synergistic herb-drug interaction, the dose level of MT may be reduced to produce the same therapeutic effect as when taken alone.
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