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   2014| May  | Volume 10 | Issue 38  
    Online since May 28, 2014

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Luteolin, a bioflavonoid inhibits azoxymethane-induced colon carcinogenesis: Involvement of iNOS and COX-2
Ashok Kumar Pandurangan, Suresh Kumar, Prakash Dharmalingam, Sudhandiran Ganapasam
May 2014, 10(38):306-310
DOI:10.4103/0973-1296.133285  PMID:24991108
Colon cancer (CRC) is a serious health problem through worldwide. Development of novel drug without side effect for this cancer was crucial. Luteolin (LUT), a bioflavonoid has many beneficial effects such as antioxidant, anti-inflammatory, anti-proliferative properties. Azoxymethane (AOM), a derivative of 1, 2-Dimethyl hydrazine (DMH) was used for the induction of CRC in Balb/C mice. CRC was induced by intraperitoneal injection of AOM to mice at the dose of 15 mg/body kg weight for 3 weeks. Mouse was treated with LUT at the dose of 1.2 mg/body kg weight orally until end of the experiment. The expression of inducible nitric oxide synthase (iNOS) and cyclooxygense (COX)-2 were analyzed by RT-PCR and immunohistochemistry. The expressions of iNOS and COX-2 were increased in the case of AOM induction. Administration of LUT effectively reduced the expressions of iNOS and COX-2. The present study revealed that, LUT suppresses both iNOS and COX-2 expressions and act as an anti-inflammatory role against CRC.
  10 2,565 73
Flavonols and derivatives of gallic acid from young leaves of Toona sinensis (A. Juss.) Roemer and evaluation of their anti-oxidant capacity by chemical methods
Huan Yang, Qinying Gu, Tingting Gao, Xubo Wang, Phenwei Chue, Qinan Wu, Xiaobin Jia
April-June 2014, 10(38):185-190
DOI:10.4103/0973-1296.131034  PMID:24914286
Background: Toona sinensis (A. Juss.) Roemer is an endemic species of Toona genus native to Asia. Its crude extract exhibits an effective anti-oxidant capacity against oxidative models, but the intrinsic substances responsible for this capacity in the extract remains unclear and is yet to be studied comprehensively. Objective: To investigate the chemical constituents of the young leaves of Toona sinensis and its anti-oxidant capacity. Materials and Methods: Silica gel column chromatography, preparative high-performance liquid chromatography (HPLC), nuclear magnetic resonance (NMR), and mass spectrometry (MS) were used to isolate and characterize the chemical constituents. Four chemical-induced oxidative models including DPPH free-radical scavenging assay, phenazine methosulphate (PMS) nicotinamide adenine dinucleotide (NADH) PMS-NADH-NBT superoxide anion scavenging assay, FeCl 3 -K 3 Fe (CN) 6 reducing power assay, and FeCl 2 -FerroZine metal chelation assay were applied in the present study for evaluating anti-oxidant capacity. Results: Five flavonols and three derivatives of gallic acid, including quercetrin, kaempferol-3-O-α-L-rhamopyranoside, astragalin, quercetin, kaempferol, methyl gallate, ethyl gallate, and 1, 2, 3, 4, 6-penta-O-galloyl-β-D-glucopyranose were isolated from the leaves. Results showed that these compounds exhibited various antioxidant properties, markedly either as the strong scavengers for superoxide and free radicals or as molecules that were reducing or metal chelating in nature. Conclusion: The findings suggested that the 8 compounds in the young leaves of T. sinensis that were isolated in our study were the active compounds responsible for its antioxidant activity. These compounds can be utilized as a potential health supplement, as an available source of natural antioxidants, and as an effective material in pharmaceutical applications.
  6 2,293 42
Anti-cholinesterase activity of the standardized extract of Syzygium aromaticum L.
Manoj K. Dalai, Santanu Bhadra, Sushil K. Chaudhary, Arun Bandyopadhyay, Pulok K. Mukherjee
May 2014, 10(38):276-282
DOI:10.4103/0973-1296.133275  PMID:24991103
Background: Clove (Syzygium aromaticum) is a well-known culinary spice with strong aroma; contains a high amount of oil known as clove oil. The major phyto-constituent of the clove oil is eugenol. Clove and its oil possess various medicinal uses in indigenous medicine as an antiseptic, anti-oxidant, analgesic and neuroprotective properties. Thus, it draws much attention among researchers from pharmaceutical, food and cosmetic industries. Objective: The aim of the present study was to determine the anti-cholinesterase activity of the methanol extract of clove, its oil and eugenol. Materials and Methods: In vitro anti-cholinesterase activity of S. aromaticum was performed by a thin layer chromatography bio autography, 96 well micro titer plate and kinetic methods. Reverse phase high performance liquid chromatography (RP-HPLC) analysis was carried out to identify the biomarker compound eugenol in clove oil. Results: Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition study revealed that eugenol possess better inhibition of the enzymes than extract and oil. Clove extract, its oil and eugenol showed better inhibition of AChE than BChE. Polyphenolic compound eugenol was detected through RP-HPLC analysis. The content of eugenol in essential oil was found to be 0.5 μg/ml. Kinetic analysis of the cholinesterase inhibition study of the extract; clove oil and eugenol have shown that they possess mixed type of inhibition for AChE and non-competitive type of inhibition for BChE. Conclusion: These results might be useful in explaining the effect of clove as anti-cholinesterase agent for the management of cognitive ailments like Alzheimer's disease.
  5 3,413 85
Evaluation of antidiabetic, antioxidant and antiglycating activities of the Eysenhardtia polystachya
Rosa Martha Perez Gutierrez, Efren Garcia Baez
May 2014, 10(38):404-418
DOI:10.4103/0973-1296.133295  PMID:24991120
Background: Many diseases are associated with oxidative stress caused by free radicals. The aim of the present study was to evaluate the antidiabetic, antioxidant and antiglycation properties of Eysenhardtia polystachya (EP) bark methanol-water extract. Materials and Methods : The antioxidant capacities were evaluated by studying in vitro the scavenging of DPPH and ABTS free radical, reactive oxygen species such as RO 2 , O 2· - , H 2 O 2 , OH . , H 2 O 2 , ONOO-, NO, HOCl, 1 O 2 , chelating ability, ORAC, β-carotene-bleaching and lipid peroxidation. The antiglycation activities of EP were evaluated by haemoglobin, bovine serum albumin (BSA)-glucose, BSA-methylglyoxal and BSA-glucose assays. Oral administration of EP at the doses of 100 mg/kg, 200 mg/kg and 400 mg/g was studied in normal, glucose-loaded and antidiabetic effects on streptozotocin-induced mildly diabetic (MD) and severely diabetic (SD) mice. Results: EP showed Hdonor activity, free radical scavenging activity, metal chelating ability and lipid peroxidation Antioxidant activity may be attributed to the presence of phenolic and flavonoid compounds. EP is an inhibitor of fluorescent AGE, methylglyoxal and the glycation of haemoglobin. In STZ-induced diabetic mice, EP reduced the blood glucose, increased serum insulin, body weight, marker enzymes of hepatic function, glycogen, HDL, GK and HK while there was reduction in the levels of triglyceride, cholesterol, TBARS, LDL and G6Pase. Conclusions: Eysenhardtia polystachya possesses considerable antioxidant activity with reactive oxygen species (ROS) scavenging activity and demonstrated an anti-AGEs and hepatoprotective role, inhibits hyperglycemic, hyperlipidemic and oxidative stress indicating that these effects may be mediated by interacting with multiple targets operating in diabetes mellitus.
  5 2,725 57
Revisiting "Vegetables" to combat modern epidemic of imbalanced glucose homeostasis
Ashok Kumar Tiwari
May 2014, 10(38):207-213
DOI:10.4103/0973-1296.133211  PMID:24991093
Vegetables have been part of human food since prehistoric times and are considered nutritionally necessary and good for health. Vegetables are rich natural resource of biological antioxidants and possess capabilities of maintaining glucose homeostasis. When taken before starch-rich diet, juice also of vegetables such as ridge gourd, bottle gourd, ash gourd, chayote and juice of leaves of vegetables such as radish, Indian Dill, ajwain, tropical green amaranth, and bladder dock are reported to arrest significantly the rise in postprandial blood glucose level. Juice of vegetables such as ash gourd, squash gourd, and tropical green amaranth leaves are observed to tone-down sweet-beverages such as sucrose, fructose, and glucose-induced postprandial glycemic excursion. On the other hand, juice of egg-plant and juice of leaves of Ceylon spinach, Joyweed, and palak are reported to augment starch-induced postprandial glycemic excursion; and juice of leaves of Ceylon spinach, Joyweed, and radish supplement to the glucose-induced postprandial glycemia. Vegetables possess multifaceted antihyperglycemic activities such as inhibition of pancreatic α-amylase and intestinal α-glucosidase, inhibition of protein-tyrosine phosphatase 1β in liver and skeletal muscles, and insulin mimetic and secretagogue activities. Furthermore, they are also reported to influence polyol pathway in favor of reducing development of oxidative stress, and consequently the development of diabetic complications. In the wake of emergence of modern maladaptive diet-induced hyperglycemic epidemic therefore, vegetables may offer cost-effective dietary regimen to control diet-induced glycemic over load and future development of diabetes mellitus. However, for vegetables have been reported to do both, mitigate as well as supplement to the diet-induced postprandial glycemic load, care is required in selection of vegetables when considered as medicament.
  4 4,240 183
Anti-tumor activity of safranal against neuroblastoma cells
Saeed Samarghandian, Mohammad Ebrahim Shoshtari, Javad Sargolzaei, Hosna Hossinimoghadam, Jabbari Azad Farahzad
May 2014, 10(38):419-424
DOI:10.4103/0973-1296.133296  PMID:24991121
Objective: Safranal (2,6,6-trimethyl-1,3-cyclohexadiene-1-carboxaldehyde, C10H14O) is an active ingredient in the saffron, which is used in traditional medicine, and also, the biological activity of saffron in anti-cancer is in development. It has been reported to have anti-oxidant effects, but its anti-tumor effects remain uncertain. The aim of this study was to evaluate effects of safranal on anti-tumor on neuroblastoma cells. Materials and Methods: Neuroblastoma cells were cultured and exposed to safranal (0, 10, 15, 20, 50 μg/ml). Cell proliferation was examined using the 3-(4, 5-dimethyl thiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assay. Apoptotic cells, cell cycle distribution, and sub-G1 fraction were analyzed using flow cytometric analysis after propidium iodide staining. Results: Safranal inhibited the growth of malignant cells in a dose-and time-dependent manner. The IC (50) values against the neuroblastoma cell line were determined as 11.1 and 23.3 μg/ml after 24 and 48 h, respectively. Safranal induced a sub-G1 peak in the flow cytometry histogram of treated cells compared to control cells indicating that apoptotic cell death is involved in safranal toxicity. Conclusions: Our pre-clinical study demonstrated a neuroblastoma cell line to be highly sensitive to safranal-mediated growth inhibition and apoptotic cell death. Although the molecular mechanisms of safranal action are not yet clearly understood, it appears to have potential as a therapeutic agent.
  4 1,902 51
Effect of ultrasound on the isoflavonoid production in Genista tinctoria L. suspension cultures
Lenka Tumova, Jiri Tuma, Helena Hendrychova
May 2014, 10(38):425-429
DOI:10.4103/0973-1296.133297  PMID:24991122
Background: Application of ultrasound (US) to biotechnology is relatively new but several processes that take place in the presence of cells or enzymes are activated by ultrasonic waves. Genista tinctoria L. (Fabaceae) is rich on various kind of flavonoids, including isoflavones with valuable estrogenic activity. Objective: This study verified use of low-energy US elicitor to enhance secondary metabolite production in plant cell cultures. Materials and Methods: Suspension cultures of G. tinctoria cells was exposed to low-power US (with fixed frequency 35 kHz and power level 0.1 mW/cm 3 ) for period 1-5 min. Results: The US exposure significantly stimulated genistin content (0.8 mg/g DW) after 3 min of US treatment (sampled after 72 h). The highest daidzein level (1.4 mg/g DW) was reached after US irradiation for 5 min and 168 h sampling. Conclusion: The achieved results suggest that US can act as a potent abiotic elicitor to induce the defense responses of plant cells and to stimulate secondary metabolite production in plant cell cultures.
  3 1,815 45
Cytotoxic neviotane triterpene-type from the red sea sponge Siphonochalina siphonella
Rihab F. Angawi, Esraa Saqer, Ahmed Abdel-Lateff, Farid A. Badria, Seif-Eldin N. Ayyad
May 2014, 10(38):334-341
DOI:10.4103/0973-1296.133292  PMID:24991112
Background: Siphonochalina siphonella is a marine sponge collected from saudi Red Sea water and scare study from this region. Objective: To isolate the anticancer triterpenes with potent cytotoxicity from marine sponge, Siphonochalina siphonella and state the mode of action in cancer cell lines. Materials and Methods: The sponge material was collected, extracted with organic solvent, and fractionated on different adsorbents. The structure of the pure metabolites were elucidated employing different spectroscopic techniques including 1D ( 1 H and 13 C) and 2D (COSY, HMQC and HMBC) NMR, and MS spectroscopy. Results: A new Neviotine-C (1) was obtained, along with four known metabolites (2-5). All compounds, except 5, were tested towards MCF-7, PC-3 and A549 and showed effects with IC 50 in range 7.9-87 μM, whilst, 3 showed potent anti-proliferative activity against PC-3 and A549 with IC 50 = 7.9 ± 0.120 and 8.9 ± 0.010 μM, respectively. Conclusion: Compounds (1-4) showed significant cytotoxic activities, while 3 showed potent effect. The antiproliferative of 3 was attributed to significant S-phase cell cycle arrest.
  3 1,912 42
Pyrostegia venusta heptane extract containing saturated aliphatic hydrocarbons induces apoptosis on B16F10-Nex2 melanoma cells and displays antitumor activity in vivo
Carlos R Figueiredo, Alisson L Matsuo, Felipe V Pereira, Aline N Rabaca, Camyla F Farias, Natalia Girola, Mariana H Massaoka, Ricardo A Azevedo, Jorge A.B Scutti, Denise C Arruda, Luciana P Silva, Elaine G Rodrigues, Joćo Henrique G Lago, Luiz R Travassos, Regildo M.G Silva
May 2014, 10(38):363-376
DOI:10.4103/0973-1296.133284  PMID:24991116
Background: Pyrostegia venusta (Ker. Gawl.) Miers (Bignoniacea) is a medicinal plant from the Brazilian Cerrado used to treat leucoderma and common diseases of the respiratory system. Objective: To investigate the antitumor activity of P.venusta extracts against melanoma. Materials and Methods: The cytotoxic activity and tumor induced cell death of heptane extract (HE) from P. venusta flowers was evaluated against murine melanoma B16F10-Nex2 cells in vitro and in a syngeneic model in vivo. Results: We found that HE induced apoptosis in melanoma cells by disruption of the mitochondrial membrane potential, induction of reactive oxygen species and late apoptosis evidenced by plasma membrane blebbing, cell shrinkage, chromatin condensation and DNA fragmentation, exposure of phosphatidylserine on the cell surface and activation of caspase-2,-3,-8,-9. HE was also protective against singeneyc subcutaneous melanoma HE compounds were also able to induce cell cycle arrest at G2/M phases on tumor cells. On fractionation of HE in silica gel we isolated a cytotoxic fraction that contained a mixture of saturated hydrocarbons identified by 1 H NMR and GC-MS analyses. Predominant species were octacosane (C 28 H 58 -36%) and triacontane (C 30 H 62 -13%), which individually showed significant cytotoxic activity against murine melanoma B16F10-Nex2 cells in vitro and a very promising antitumor protection against subcutaneous melanoma in vivo. Conclusion: The results suggest that the components of the heptane extract, mainly octasane and triacontane, which showed antitumor properties in experimental melanoma upon regional administration, might also be therapeutic in human cancer, such as in the mostly epidermal and slowly invasive melanomas, such as acral lentiginous melanoma, as an adjuvant treatment to surgical excision.
  3 3,100 81
Vegetables' juice influences polyol pathway by multiple mechanisms in favour of reducing development of oxidative stress and resultant diabetic complications
Ashok K Tiwari, D Anand Kumar, Pisupati S.R Sweeya, H Anusha Chauhan, V Lavanya, K Sireesha, K Pavithra, Amtul Zehra
May 2014, 10(38):383-391
DOI:10.4103/0973-1296.133290  PMID:24991118
Objective: Hyperglycemia induced generation of free radicals and consequent development of oxidative stress by polyol pathway is one of the crucial mechanisms stirring up development of diabetic complications. We evaluated influence of ten vegetables' juice on polyol pathway along with their antioxidant and antioxidative stress potentials. Materials and Methods: Aldose reductase activity was determined utilising goat lens and human erythrocytes. In goat lens, utilization of nicotinamine adenine dinucleotide phosphate (NADPH) and aldose reductase inhibition was assayed. In human erythrocytes, sorbitol formation was measured as an index of aldose reductase activity under normoglycemic and hyperglycemic conditions. Ability of juices in inhibiting oxidative damage to deoxyribose sugar and calf thymus DNA and inhibitory activity against hydrogen peroxide induced hemolysis of erythrocytes was also analysed. Phytochemical contents like total polyphenol, total flavonoid and total protein were measured to find their influence on biological activities. Results: Vegetables' juice displayed varying degrees of inhibitory potentials in mitigating NADPH dependent catalytic activity of aldose reductase in goat lens, accumulation of sorbitol in human erythrocytes under different glucose concentrations; Fenton-reaction induced oxidative damage to deoxyribose sugar, and calf thymus DNA. Substantial variations in vegetables phytochemicals content were also noticed in this study. Conclusions: Vegetables' juice possesses potent activities in influencing polyol pathway by various mechanisms in favour of reducing development of oxidative stress independent of their inherent antioxidative properties. Juice of ivy gourd followed by green cucumber and ridge gourd were among the most potent for they displayed strong activities on various parameters analysed in this study. These vegetables' juice may become part of mechanism-based complementary antioxidant therapy to prevent development of diabetic complications.
  3 3,556 66
Protective effect and mechanism of Ginkgo biloba extract-EGb 761 on STZ-induced diabetic cardiomyopathy in rats
Arminder Singh Saini, Rajeev Taliyan, Pyare Lal Sharma
April-June 2014, 10(38):172-178
DOI:10.4103/0973-1296.131031  PMID:24914284
Diabetes mellitus (DM) is a complex metabolic disorder which leads to development of various long-term complications including cardiomyopathy. Oxidative stress due to hyperglycemia plays a key role in the development and progression of diabetic cardiomyopathy (DC). Oxidative stress causes the opening of mitochondrial permeability transition pore (mPTP) eventually leading to myocardium dysfunction. The Ginkgo biloba extract (EGb 761) has antioxidant and mitochondrial membrane potential stabilizing property. Therefore, this study was designed to evaluate the effect of EGb 761 and its possible mechanism of action in DC. Materials and Methods: DM was induced by single injection of Streptozotocin (STZ) (50 mg/kg, i.p.) and cardiac dysfunction was developed on 8 th weeks after STZ injection. Cardiac dysfunction was assessed by measuring left ventricle weight/body weight (LVW/BW) ratio, left ventricle (LV) collagen content, LV protein content, serum lactate dehydrogenase (LDH) level. Results: EGb 761 treatment (started after 7 th week of STZ injection and continued for 3 weeks) attenuated cardiac dysfunction in diabetic rats as evidenced by a decrease in LV collagen content, protein content, LVW/BW ratio, serum LDH level. Moreover, EGb 761 attenuated the oxido-nitrosative stress (thiobarbituric acid reactive substances, superoxide anion generation, myocardium nitrite) and concomitantly improved the antioxidant enzyme (reduced glutathione) level as compared to untreated diabetic rats. However, protective effect of EGb 761 was inhibited by atractyloside (mPTP opener) that was given for 3 weeks, 30 min before the EGb 761 treatment. These results indicate that EGb 761 corrects diabetic cardiac dysfunction probably by its direct radical scavenging activity and its ability to inhibit the opening of mPTP channel since the cardioprotective effect of EGb 761 was completely abolished by atractyloside.
  3 2,393 50
Protective effects of curcumin against genotoxicity induced by 131-iodine in human cultured lymphocyte cells
Nayereh Shafaghati, Monireh Hedayati, Seyed Jalal Hosseinimehr
April-June 2014, 10(38):106-110
DOI:10.4103/0973-1296.131020  PMID:24914274
Background: 131-radioiodine has been widely used as an effective radionuclide for treatment of patients with thyroid diseases. The purpose of the present study is to investigate the radioprotective effects of curcumin as a natural product that protects against the genotoxic effects of 131 I in human cultured lymphocytes. Materials and Methods: Whole blood samples from human volunteers were incubated with curcumin at doses of 5, 10, and 50 μg/mL. After 1-hour incubation, the lymphocytes were incubated with 131 I (100 μCi/1.5 ml) for 2 hours. The lymphocyte cultures were then mitogenically stimulated to allow for evaluation of the number of micronuclei in cytokinesis-blocked binucleated cells. Results: Incubation of lymphocytes with 131 I at dose 100 μCi/1.5 mL induced genotoxicity shown by increase in micronuclei frequency in human lymphocytes. Curcumin at 5, 10, and 50 μg/mL doses significantly reduced the micronuclei frequency. Maximal protective effects and greatest decrease in micronuclei frequency were observed when whole blood was incubated with 50 μg/mL dose of curcumin with 52%. Conclusion: This study has important implications for patients undergoing 131 I therapy. Our results indicate a protective role for curcumin against the genetic damage and side effects induced by 131 I administration.
  3 2,133 41
Podophyllotoxin and 6-methoxy podophyllotoxin Production in Hairy Root Cultures of Liunm mucronatum ssp. mucronatum
Afsaneh Samadi, Morad Jafari, Nasim Mohammad Nejhad, Farah Hossenian
April-June 2014, 10(38):154-160
DOI:10.4103/0973-1296.131027  PMID:24914281
Aim: Two bacterial strains of Agrobacterium rhizogenes, A13 and 9534 were evaluated for induction of transformed hairy roots in Linum mucronatum ssp. mucronatum, a high value medicinal plant. Materials and Methods: The hairy roots were successfully initiated, through infecting the hypocotyl and root explants and the A13 strain performed a high transformation frequency for hairy roots induction. Transgenic status of hairy roots was confi rmed by polymerase chain reaction (PCR) analysis of the rol genes. Growth kinetics of transgenic roots induced by two strains indicated a similar pattern of growth, with maximum growth occurring between 42 to 56 days. The lignan contents in hairy roots were analyzed using high-performance liquid chromatography (HPLC) method. Results: Transformed cultures showed signifi cant differences (P < 0.05) in lignan content. The highest amount of Podophyllotoxin (PTOX, 5.78 mg/g DW) and 6-methoxy podophyllotoxin (MPTOX, 49.19 mg/g DW) was found in transformed lines induced by strain A13, which was four times higher than those of non-transformed roots. The results showed that hairy root cultures of L. mucronatum are rich sources of MPTOX. Conclusion: hairy root cultures from L. mucronatum can be used as a useful system for scale-up producing MPTOX and precursors for the production of antitumor agents in substitution with PTOX by considering the appropriate optimizations in future studies.
  3 2,966 74
Chitosan and blueberry treatment induces arginase activity and inhibits nitric oxide production during acetaminophen-induced hepatotoxicity
Eda Ozcelik, Sema Uslu, Dilek Burukoglu, Ahmet Musmul
May 2014, 10(38):217-224
DOI:10.4103/0973-1296.133234  PMID:24991095
Background: Liver diseases have become a major problem of the worldwide. More than 50% of all cases of liver failure can be attributed to drugs. Among these, acetaminophen is the most common cause. Objective: The aim of this study was to investigate the the hepatoprotective effects of blueberry and chitosan on tissue arginase activity, ornithine and nitric oxide levels during the acetaminophen-induced hepatotoxicity. Materials and Methods: Acetaminophen (250 mg/kg body weight per day), blueberry (60 mg/kg body weight per day) and, chitosan (200 mg/kg body weight per day) were administered to the rats by oral gavage during the experimental period. Results: Blueberry and chitosan significantly decreased liver arginase activity and ornithine levelsand and increased nitric oxide levels. Glutathione levels were remarkably increased by chitosan and blueberry treatments. Conclusion: The results of the present study indicate that blueberry and chitosan effectively protected against the acetaminophen-induced hepatotoxicity. The hepatoprotective effect afforded by blueberry and chitosan can be attributed to its antioxidant and anti-inflammatory activities.
  3 2,739 86
Inhibitory effects of ginseng seed on melanin biosynthesis
Yeonmi Lee, Kyoung-Tack Kim, Sung Soo Kim, Jinyoung Hur, Sang Keun Ha, Chang-Won Cho, Sang Yoon Choi
May 2014, 10(38):272-275
DOI:10.4103/0973-1296.133271  PMID:24991102
Background: Ginseng root has been traditionally used for the treatment of many diseases in Korea. However, so far ginseng seed has been mostly unused and discarded. As part of our ongoing research on the ginseng seeds, the inhibitory effect of ginseng seeds on melanin production was verified to assess their potential as a skin depigmenting substance. Materials and Methods: The present study measured the inhibitory effect of ginseng seeds on melanin production through the tyrosinase inhibitory effect and analyzed their effects on melanin production in melan-a-cells. Results: Ethanol extract of ginseng seed was applied to melan-a-cells at a concentration of 100 ppm and melanin production was reduced by 35.1% without cytotoxicity. In addition, the ethanol extract of ginseng seed was shown to reduce tyrosinase activity. Conclusion: Because the results showed excellent melanin inhibitory activity compared with that obtained by arbutin, ethanol extracts of ginseng leaf and ginseng root at the same concentration, it can be concluded that ginseng seeds show great potential as a skin depigmenting substance.
  3 2,592 69
Molecular docking studies of flavonoids for their inhibition pattern against β-catenin and pharmacophore model generation from experimentally known flavonoids to fabricate more potent inhibitors for Wnt signaling pathway
Hira Iftikhar, Sajid Rashid
May 2014, 10(38):264-271
DOI:10.4103/0973-1296.133269  PMID:24991101
Background: Canonical Wnt signaling plays a key role in tumor cell proliferation, which correlates with the accumulation of β-catenin in cell due to inactivation of glycogen synthetase kinase-3 β. However, uncontrolled expression of β-catenin leads to fibromatosis, sarcoma and mesenchymal tumor formation. Recently, a number of polyphenolic compounds of naturally occurring flavonoid family have been screened for the inhibition of Wnt signaling. Objective: Elucidation of the binding mode of inhibitors to β-catenin, reporting more potent inhibitors for the disease-causing protein and designing a pharmacophore model based on naturally occurring compounds, flavonoids. Materials and Methods: In this study, a comparative molecular docking analysis was performed to elucidate the binding mode of experimentally reported and unknown inhibitors. Based on the knowledge of geometry, binding affinity and drug score, we described a subset of novel inhibitors. Results: The binding energy of known inhibitors (isorhamnetin, fisetin, genistein and silibinin) was observed in a range of −5.68 to −4.98 kcal/mol, while novel inhibitors (catechin, luteolin, coumestrol and β-naphthoflavone) exhibited −6.50 to −5.22 kcal/mol. We observed good placement and strong interactions of selected compounds inside the binding pocket of β-catenin. Moreover, flavonoid family members and T cell factors 4 (TCF4) compete for β-catenin binding by sharing common binding residues. Conclusion: This study will largely help in understanding the molecular basis of β-catenin/TCF4 inhibition through flavonoids by exploring their structural details. Finally, the novel inhibitors proposed in this study need further attention to uncover cancer treatment and with the generated pharmacophore model, more and potent β-catenin inhibitors can be easily screened.
  2 2,896 85
Neuroprotective and cognitive enhancing activity of the fermented Bozhougyiqi-Tang
Jin Bae Weon, Bohyoung Lee, Bo-Ra Yun, Jiwoo Lee, Jin Yeul Ma, Choong Je Ma
May 2014, 10(38):249-255
DOI:10.4103/0973-1296.133266  PMID:24991099
Background: Alzheimer's disease is a neurodegenerative disease related to memory impairments and neuronal cell death. Bozhougyiqi-Tang (BZYQT), a traditional herbal medicine, has been therapeutically used for the treatment of pulmonary tuberculosis. Objective: The aim of this study is to evaluated the neuroprotective effect of the fermented BZYQT and compared with unfermented BZYQT in HT22 cells by MTT assay and tested the beneficial effect on memory impairments induced by scopolamine (1 mg/kg, i.p.) using the passive avoidance and Morris water maze tests. Results: Compared with unfermented BZYQT, the neuroprotective effect of fermented BZYQT on glutamate induced neurotoxicity in HT22 cells increased at a concentration of 100 μg/mL. Fermented BZYQT increased the step-through latency of the passive avoidance response. Furthermore, in Morris water maze test for evaluation of spatial learning and memory, escape latency time was significantly reduced by fermented BZYQT. Conclusion: These results suggest that the fermentation process of BZYQT led to improve neuroprotective and cognitive enhancing effect.
  2 1,948 57
Antiproliferative activity of Vallaris glabra Kuntze (Apocynaceae)
Siu Kuin Wong, Yau Yan Lim, Sui Kiong Ling, Eric Wei Chiang Chan
May 2014, 10(38):232-239
DOI:10.4103/0973-1296.133238  PMID:24991097
Background: Our earlier study on the antiproliferative (APF) activity of leaf extracts of ten Apocynaceae species showed that leaves of Vallaris glabra possessed strong and broad-spectrum properties. Materials and Methods: In this study, sequential extracts of leaves, flowers and stems, and fractions and isolated compounds from dichloromethane (DCM) leaf extract of V. glabra were assessed for APF activity using the sulphorhodamine B (SRB) assay. Apoptotic effect of MDA-MB-231 cancer cells treated with DCM leaf extract of V. glabra was studied using Hoechst 33342 dye and caspase colorimetry. Results: Both DCM extracts of leaves and flowers possessed broad-spectrum APF activity against HT-29, MCF-7, MDA-MB-231 and SKOV-3 cancer cells. From DCM leaf extract, stearic acid (SA) and ursolic acid (UA) were isolated by column chromatography, and identified by NMR and MS analyses. APF activity of SA from DCM leaf extract displayed weak inhibitory activity and scientific literature showed UA has anticancer properties against those cancer cells used in this study. MDA-MB-231 cancer cells treated with DCM leaf extract and stained with Hoechst 33342 dye provided evidence that the extract had an apoptotic effect on the cells. Caspase colorimetry showed that the apoptotic effect involved activation of caspase-8, -9 and -3, but not caspase-6. Conclusion: The potential of V. glabra as a candidate species for anticancer drugs warrants further investigation.
  2 2,362 51
Pharmacodynamic studies on the isolated active fraction of Acacia farnesiana (L.) willd
Bino Kingsley, Saminathan Kayarohanam, Pemaiah Brindha, Appian Subramoniam
May 2014, 10(38):283-287
DOI:10.4103/0973-1296.133277  PMID:24991104
Background: Acacia farnesiana is a medicinal plant that grows throughout tropical parts of Indian subcontinent, particularly in sandy soils of river beds in Northern India. The objective of the present study was to evaluate the anti-hyperglycemic activity of the extracts using glucose tolerance test. Isolation of an active fraction (AF) from the active extract (water extract) using alcohol precipitation and to get insight to the mechanism of action of the AF of A. farnesiana. Materials and Methods: Glucose uptake by isolated rat diaphragm of the AF was performed. Further the effect of release of Insulin from isolated and cultured pancreatic β-cell was determined. Besides, effect of oral administration of the AF was compared with that of intraperitonial administration. The effect of AF on serum glucose levels in orally glucose loaded rats was compared with that of intraperitoneal glucose loaded rats. Results: The water extract significantly lowered the blood glucose level. When precipitated with alcohol, the activity was found in the soluble fraction. Glucose uptake in the isolated rat hemidiaphragm, was increased by the AF at 40 μg/ml concentration, the AF did not significantly influence insulin release from cultured islets. The AF was found to be effective in orally glucose loaded in contrast to intraperitonial route. Conclusion: Our findings suggest that this plant is promising for further studies leading to the development of valuable medicine for diabetes.
  2 2,053 51
Quantification of allicin by high performance liquid chromatography-ultraviolet analysis with effect of post-ultrasonic sound and microwave radiation on fresh garlic cloves
Sankhadip Bose, Bibek Laha, Subhasis Banerjee
May 2014, 10(38):288-293
DOI:10.4103/0973-1296.133279  PMID:24991105
Background: Garlic (Allium sativum L.) has been accepted universally to be applied in food, spice and traditional medicine. The medicinal and other beneficial properties of garlic are attributed to organosulfur compounds. Objective: As of today no simultaneous analysis has been performed; hence the transformation of allicin to its degraded products during cultivation and storage is open into doubt. Materials and Methods: In our present work, we have tried to develop a sensitive and reproducible analytical method to measure allicin by high performance liquid chromatography-ultraviolet analysis with effect of post-acoustic waves and microwave radiation on fresh garlic cloves. Results: The process revealed the effect of different radiation techniques on fresh garlic retains the principle component, allicin in its pure form and generated higher yield than the conventional way of extraction. Conclusion: Therefore, materializing these techniques in the pharmaceutical industry will definitely be proved beneficial in term of time as well as money. Most interestingly, the methods ruled out possibilities of degradation of organosulfur compounds as well.
  2 3,137 107
Effect of Aronia melanocarpa fruit juice on amiodarone-induced pneumotoxicity in rats
Stefka Valcheva-Kuzmanova, Galya Stavreva, Violeta Dancheva, Ljudmil Terziev, Milena Atanasova, Angelina Stoyanova, Anelia Dimitrova, Veneta Shopova
April-June 2014, 10(38):132-140
DOI:10.4103/0973-1296.131024  PMID:24914278
Background: The fruits of Aronia melanocarpa (Michx.) Elliot is extremely rich in biologically active polyphenols. Objective: We studied the protective effect of A. melanocarpa fruit juice (AMFJ) in a model of amiodarone (AD)-induced pneumotoxicity in rats. Materials and Methods: AD was instilled intratracheally on days 0 and 2 (6.25 mg/kg). AMFJ (5 mL/kg and 10 mL/kg) was given orally from day 1 to days 2, 4, 9, and 10 to rats, which were sacrificed respectively on days 3, 5, 10, and 28 when biochemical, cytological, and immunological assays were performed. Results: AMFJ antagonized AD-induced increase of the lung weight coefficient. In bronchoalveolar lavage fluid, AD increased significantly the protein content, total cell count, polymorphonuclear cells, lymphocytes and the activity of lactate dehydrogenase, acid phosphatase and alkaline phosphatase on days 3 and 5. In AMFJ-treated rats these indices of direct toxic damage did not differ significantly from the control values. In lung tissue, AD induced oxidative stress measured by malondialdehyde content and fibrosis assessed by the hydroxyproline level. AMFJ prevented these effects of AD. In rat serum, AD caused a significant elevation of interleukin IL-6 on days 3 and 5, and a decrease of IL-10 on day 3. In AMFJ-treated rats, these indices of inflammation had values that did not differ significantly from the control ones. Conclusion: AMFJ could have a protective effect against AD-induced pulmonary toxicity as evidenced by the reduced signs of AD-induced direct toxic damage, oxidative stress, inflammation, and fibrosis.
  2 1,816 36
ACE and platelet aggregation inhibitors from Tamarix hohenackeri Bunge (host plant of Herba Cistanches) growing in Xinjiang
Yachao Xing, Jing Liao, Yingzhan Tang, Peng Zhang, Chengyu Tan, Hui Ni, Xueqin Wu, Ning Li, Xiaoguang Jia
April-June 2014, 10(38):111-117
DOI:10.4103/0973-1296.131021  PMID:24914275
Background: Tamarix hohenackeri Bunge is a salt cedar that grows widespread in the desert mountains in Xinjiang. T. hohenackeri has not been investigated earlier, although there are many reports of phytochemical work on other Tamarix species. Materials and Methods: To find out natural angiotensin-converting enzyme (ACE) inhibitor and platelet aggregation inhibitors, the bioactive extract (ethyl acetate [EtOAc] fraction) from the dried aerial parts of T. hohenackeri were investigated. The active fraction was purified by repeated column chromatography, including silica gel, Sephadex LH-20 column, medium-pressure liquid chromatography (MPLC) (polyamide column) and high-performance liquid chromatography (HPLC). The isolated major constituents were tested for their anti-platelet aggregation activity. Results: Bioassay-directed separation of the EtOAc fraction of the 70% ethanol extract from the air-dried aerial parts of T. hohenackeri led to the isolation of a new triterpenoid lactone (1), together with 13 known compounds (2-14). It was the first time to focus on screening bioactive constituents for this plant. The chemical structures were established on the basis of spectral data (ESI-MS and NMR). The results showed that the flavonoid compounds (7 and 8) and phenolic compounds (9, 10, 11, and 14) were potential ACE inhibitors. And the flavonoid compounds (5 and 7) showed significant anti-platelet aggregation activities. Conclusion: On the basis of the chemical and biological data, the material basis of ACE inhibitory activity for the active part was the phenolic constituents. However, the flavonoid compounds were responsible for the anti-platelet aggregation. The primary structure and activity relationship were also discussed respectively.
  2 3,056 43
Leucas aspera inhibits the Dalton's ascitic lymphoma in Swiss albino mice: A preliminary study exploring possible mechanism of action
Bibin Baby Augustine, Suvakanta Dash, Mangala Lahkar, Usha Sarma, Pavan Kumar Samudrala, Jaya Mary Thomas
April-June 2014, 10(38):118-124
DOI:10.4103/0973-1296.131022  PMID:24914276
Background: North East India is a rich source of medicinal plants and a number of plant extracts are used by tribal peoples living in this area for various disorders. L.aspera is such a plant, traditionally used as an antitumor agent. Aim: In the present study, aerial parts of L.aspera were investigated for antitumor activity in Dalton's lymphoma (DAL) bearing mice. The ability of plant extract in free radical scavenging, neoangiogenesis inhibition and macrophage stimulation were also checked. Materials and Methods: Based on the preliminary in vitro cytotoxicity studies ethyl acetate fraction of L.aspera (EALA) was selected for the detailed study. DAL ascites tumor model was performed to check the antitumor activity of EALA (200 and 400mg/kg of body weight). Hematological and histopathological parameters were estimated. Antioxidant levels, neoangiogenesis and peritoneal macrophage count were also determined. Results: In vitro MTT and Trypan blue assay results showed the cytotoxic effect of EALA in DAL cells lines. EALA treatment resulted in significant decrease in ascites tumor volume and viable cell count. Hematological and liver antioxidant parameters were normalised by EALA treatment. It was also found that EALA treatment inhibits neovascularisation and produce macrophage stimulation in treated mice. Conclusion: The results showed that EALA is a promising anticancer agent and its activity is comparable to the standard drug 5-Flouro uracil (5-FU).
  2 2,302 44
Effect of ambrex (a herbal formulation) on oxidative stress in hyperlipidemic rats and differentiation of 3T3-L1 preadipocytes
A Jamuna Devi, Rekha Ravindran, M Sankar, Johanna Rajkumar
April-June 2014, 10(38):165-171
DOI:10.4103/0973-1296.131030  PMID:24914283
Background: Ambrex is a polyherbal formulation which consists of Withania somnifera, Orchis mascula, Cycas circirnalis, Shorea robusta with amber. Objective: The present study was designed to explore the potential effects of ambrex on the antioxidant status in high fat diet fed rats and to investigate the possible mechanisms focusing on the gene expression involved in adipogenesis and inflammation in 3T3-L1 cell line. Materials and Methods: Male Wistar rats were divided into four groups (n = 6); Group A received normal diet, Group B received high fat diet for 30 days, Group C and D received high fat diet for 30 days and treated with ambrex (40 mg/kg b.w) and atorvastatin (10 mg/kg b.w) for successive 15 days respectively. This study also assesses the effect of ambrex on adipogenesis in 3T3-L1 adipocytes. Results: The serum total cholesterol and triglycerides were significantly decreased in ambrex treated hyperlipidemic animals when compared to untreated animals. The activities of catalase, superoxide dismutase and reduced glutathione were significantly augmented in the serum, liver, and heart of hyperlipidemic rats treated with ambrex when compared to control. Ambrex treated rats had significant reductions in malondiadehyde levels in the serum, liver and heart compared to untreated rats. In addition, we observed that treatment with ambrex resulted in a major inhibition of pre-adipocyte differentiation of 3T3-L1 cells in vitro by suppression of peroxisome proliferator activated receptor gamma, sterol regulatory binding proteins, tumor necrosis factor-α, inducible nitricoxide synthase, leptin, and upregulation of thioredoxin 1 (TRX1) and TRX2 mRNA expression. Conclusion: Therefore, ambrex may be a potential drug for treatment of hyperlipidemia and related disorders.
  2 2,263 65
Anti-inflammatory effects of Cryptotympana atrataFabricius slough shed on contact dermatitis induced by dinitrofluorobenzene in mice
Miyoung Kim, Hanna Kim, Jeonghyun Ryu, Suzy Jo, Guemsan Lee, Mi Heon Ryu, Hyungwoo Kim, Su In Cho
May 2014, 10(38):377-382
DOI:10.4103/0973-1296.133288  PMID:24991117
Background: The slough shed of Cryptotympana atrata Fabricius is widely used to treat skin diseases in China, Japan, and Korea. Objective: To investigate the anti-inflammatory effects of C. atrata on contact dermatitis. Materials and Methods: We investigated the effects of C. atrata methanol extract (MECA) on ear swelling, histophathological changes and cytokine production in 1-fluoro-2,4-dinitrofluorobenzene (DNFB)-induced contact dermatitis (CD) mice. Results: Topical application of MECA effectively inhibited enlargement of ear swelling (30 and 100 μ/ear, P < 0.05; 300 μg/ear, P < 0.01). MECA treatment also inhibited hyperplasia, spongiosis (100 and 300 μg/ear, P < 0.001), and immune cell infiltration (30 μg/ear, P < 0.05; 100 and 300 μg/ear, P < 0.001) induced by DNFB. In addition, treatment with MECA suppressed the increase in the levels of TNF-α (P < 0.05), IFN-g (3, 100 μg/ear, P < 0.05; 300 μg/ear, P < 0.01), and IL-6 (100 μg/ear, P < 0.05; 300 μg/ear, P < 0.01) production. Conclusion: These data suggest that MECA has the potential for use in the treatment of inflammatory skin diseases, including CD. Moreover, the results presented herein indicate that anti-inflammatory actions of MECA are mediated by decreasing production of TNF-α, IFN-γ, and IL-6 in inflamed tissues.
  2 1,990 33
Hemostatic, milk clotting and blood stain removal potential of cysteine proteases from Calotropis gigantea (L.) R. Br. Latex
Omana Sukumaran Bindhu, Maheshwari Kumari Singh
May 2014, 10(38):350-356
DOI:10.4103/0973-1296.133294  PMID:24991114
Introduction: Plant latex is a natural source of biologically active compounds and several hydrolytic enzymes responsible for their diverse health benefits. Recent past has witnessed substantial progress in understanding their supplementary industrial and pharmaceutical utility. Calotropis gigantea is one of the important latex producing plants belonging to asclepediaceae family with wide ethnopharmacological applications and is rich in proteolytic enzymes. Present study investigates hemostatic, milk clotting and blood stain removal potential of C. gigantea latex proteases. Materials and Methods: The protease activity of crude enzyme (CE), obtained by centrifugation followed by ammonium sulphate precipitation and dialysis, was assayed using casein as the substrate. Effect of pH, temperature and specific inhibitors on protease activity was determined. Native PAGE and in gel protease activity of CE was performed. Hemostatic (Fibrinogen polymerization, fibrinogen agarose plate and blood clot lysis assays), milk clotting and blood stain removal efficacies of CE were determined. Results: CE exhibited high caseinolytic activity. Enzyme activity was optimum at 37-50ºC and pH 8.0. Fibrinogen polymerization assay showed concentration dependent increase in turbidity indicating thrombin like activity which was further confirmed by fibrinogen agarose plate assays. Clot lysis assay indicated 92.41% thrombolysis by CE in 90 min. CE also revealed significantly high ratio of milk clotting to protease activity (Milk Clotting Index, MCI = 827.59 ± 1.52). Complete destaining of blood stained fabric was observed when incubated with 1% detergent incorporated with 0.1mg/ml CE. The study highlights and validates the compound application potential of latex cysteine proteases from C. gigantea.
  2 3,087 62
In Vivo skin hydration and anti-erythema effects of Aloe vera, Aloe ferox and Aloe marlothii gel materials after single and multiple applications
Lizelle T Fox, Jeanetta du Plessis, Minja Gerber, Sterna van Zyl, Banie Boneschans, Josias H Hamman
May 2014, 10(38):392-403
DOI:10.4103/0973-1296.133291  PMID:24991119
Objective: To investigate the skin hydrating and anti-erythema activity of gel materials from Aloe marlothii A. Berger and A. ferox Mill. in comparison to that of Aloe barbadensis Miller (Aloe vera) in healthy human volunteers. Materials and Methods: Aqueous solutions of the polisaccharidic fractions of the selected aloe leaf gel materials were applied to the volar forearm skin of female subjects. The hydration effect of the aloe gel materials were measured with a Corneometer ® CM 825, Visioscan ® VC 98 and Cutometer ® dual MPA 580 after single and multiple applications. The Mexameter ® MX 18 was used to determine the anti-erythema effects of the aloe material solutions on irritated skin areas. Results: The A. vera and A. marlothii gel materials hydrated the skin after a single application, whereas the A. ferox gel material showed dehydration effects compared to the placebo. After multiple applications all the aloe materials exhibited dehydration effects on the skin. Mexameter ® readings showed that A. vera and A. ferox have anti-erythema activity similar to that of the positive control group (i.e. hydrocortisone gel) after 6 days of treatment. Conclusion: The polysaccharide component of the gel materials from selected aloe species has a dehydrating effect on the skin after multiple applications. Both A. vera and A. ferox gel materials showed potential to reduce erythema on the skin similar to that of hydrocortisone gel.
  1 5,530 99
Cytotoxicity of gypsogenic acid isolated from Gypsophila trichotoma
Ilina Krasteva, Maya Yotova, Deyan Yosifov, Niko Benbassat, Kristina Jenett-Siems, Spiro Konstantinov
May 2014, 10(38):430-433
DOI:10.4103/0973-1296.133299  PMID:24991123
Background: Gypsophila trichotoma Wend. (Caryophyllaceae) is a medicinal plant which is protected in Bulgaria by the Biodiversity Law. Previous studies have showed the presence of triterpene saponins, sterols, flavonoids, triterpens, etc. Objective: Gypsogenic acid, isolated from Gypsophila trichotoma roots, was evaluated for cytotoxic activity. Materials and Methods: The structure of the compound was elucidated by spectral methods. The cell survival fraction was determined by the MTT dye reduction assay, performed with some modifications. Results: Gypsogenic acid was tested in a panel of human tumor cell lines and was found to inhibit the proliferation of malignant cells. It was active against leukemic cells with lymphoid (SKW-3 and BV-173) or myeloid phenotype (HL-60, K-562, and LAMA-84), as well as against the EJ bladder carcinoma cell line. Bcr-Abl expressing myeloid cells (LAMA-84 and especially K-562) displayed lower sensitivity. HL-60/Dox cells were less sensitive to gypsogenic acid than the parent cell line, which shows that gypsogenic acid is probably a substrate of MRP-1.
  1 1,746 52
Germplasm preservation in vitro of Polygonum multiflorum Thunb
He-Ping Huang, Jian Wang, Lu-Qi Huang, Shan-Lin Gao, Peng Huang, Dian-Lei Wang
April-June 2014, 10(38):179-184
DOI:10.4103/0973-1296.131032  PMID:24914285
Background: The root of Polygonum multiflorum Thunb. is a common traditional Chinese medicine. In recent years, the wild resources of P. multiflorum have been seriously broken, and the cultivated varieties have been degrading. The germplasm resources of P. multiflorum need protection and preservation. So far, no in vitro germplasm preservation of P. multiflorum has been reported. Objective: To explore a method for the in vitro germplasm preservation of P. multiflorum. Materials and Methods: A large number of buds from seed explants were induced by tissue culture. The single buds were used as experimental materials to study the effects of plant growth regulator, temperature, and osmotic pressure on the preservation time, growth recovery, and genetic stability. Results: When the buds were inoculated onto Murashige and Skoog (MS) basal media containing 4% w/v sucrose, 2% w/v mannitol, and 1% w/v sorbitol, supplemented with paclobutrazol (PP 333 ) 1.0 mg/l, abscisic acid (ABA) 5.0 mg/l, and daminozide (B9) 30.0 mg/l in an illuminated chamber under a 16 h photoperiod of 1500 lx light intensity at 15°C for 10 months, the survival rate was over 70% with good growth recovery and genetic stability. Conclusion: The results of this study can be used for medium-term in vitro germplasm preservation of P. multiflorum, and meeting actual needs of research and production.
  1 2,063 49
Aqueous extract from taxus baccata inhibits adenosine deaminase activity significantly in cancerous and noncancerous human gastric and colon tissues
Zahide Esra Durak, Suleyman Buber, Erdinc Devrim, Hilmi Kocaoglu, Ilker Durak
May 2014, 10(38):214-216
DOI:10.4103/0973-1296.133232  PMID:24991094
Objective: To investigate possible effects of aqueous taxus baccata extract on adenosine deaminase (ADA) activity in cancerous and noncancerous human tissues and to clarify mechanism(s) of its anticancer potential. Materials and Methods: Cancerous and noncancerous human gastric and colon tissues were used in the study. The extracts were prepared in distilled water. Before and after treatment with the extracts, ADA activities in the tissue homogenates were measured. Results: ADA activity was found to be higher in gastric tissue compared with colon tissue, but no differences were found between ADA activities of cancerous and noncancerous tissues for both as well. In the plant extract studies, it was found that taxus extract significantly inhibited ADA activity both in cancerous and noncancerous gastric and colon tissues. Conclusion: Our results suggest that aqueous extract from taxus baccata inhibits ADA activities in both gastric and colon tissues significantly. It is suggested that in addition to other proposed mechanisms, accumulated adenosine due to the inhibition of ADA enzyme might also play part in the anticancer properties of taxus species.
  1 2,952 132
Neuroprotective effects of 4,5-dimethoxypyrocatechol isolated from Cynanchum paniculatum on HT22 cells
Jin Bae Weon, Bohyoung Lee, Bo-Ra Yun, Jiwoo Lee, Choong Je Ma
April-June 2014, 10(38):161-164
DOI:10.4103/0973-1296.131028  PMID:24914282
Background: Cynanchum paniculatum, belongs to the family Asclepiadaceae and is used to treat various diseases, such as invigorate blood, alleviate edema and to relieve pain and toxicity for a long time. Materials and Methods: 4,5-Dimethoxypyrocatechol was isolated from the 80% methanol extract of C. paniculatum and its neuroprotective effect was evaluated by MTT assay. Results: 4,5-Dimethoxypyrocatechol had neuroprotective effect on the glutamate-induced cellular oxidative death in HT22 cells. Conclusion: Furthermore, we found that reactive oxygen species (ROS) accumulation and calcium concentration by oxidative stress were reduced by 4,5-dimethoxypyrocatechol in HT22 cells.
  1 2,043 38
Screening of siddha medicinal plants for its in-vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity
Madhuri Kadiyala, Sivasankaran Ponnusankar, Kannan Elango
May 2014, 10(38):294-298
DOI:10.4103/0973-1296.133281  PMID:24991106
Background: The plants selected for the study were traditionally used in siddha system of medicine in neurological disorders. Aim: The aim of the following study isto screen the plant species for both acetylcholinesterase (AchE) and butyrylcholinesterase (BuchE) inhibition by in-vitro Ellman's method and a thin layer chromatography bioautographic assay for newer drug candidates for the treatment of Alzheimer's disease. Materials and Methods: Ellman's colorimetric method was performed in a 96 well micro plate for cholinesterases inhibition using galantamine as standard drug. Results: Present studies confirmed that out of all the tested extracts Hemidesmus indicus R.Br (HI) showed considerable IC 50 values for AchE (28.40 ± 0.92 μg/mL) and BuchE (43.47 ± 0.64 μg/mL) inhibition which indicates that HI extract has considerable specificity toward AchE and BuchE compared with all the tested extracts and the activity was followed by Vernonia anthelmintica (VA) Willd and Saussurea lappa Clarke (SL). The bioautograms also confirmed the activity potent extracts. Conclusion: Besides various bioactivities HI, VA and SL exhibited considerable cholinesterases inhibition making it to consider these species for further investigation of new compounds.
  1 2,581 60
Optimization of Ultrasound-assisted extraction of polyphenols, tannins and epigallocatechin gallate from barks of Stryphnodendron adstringens (Mart.) Coville bark extracts
Jordana N. Sousa, Nathalia B. Pedroso, Leonardo L. Borges, Gerlon A., Jose R. Paula, Edemilson C. Conceicao
May 2014, 10(38):318-323
DOI:10.4103/0973-1296.133287  PMID:24991110
Background: Stryphnodendron adstringens (Mar.) Coville is a native plant from Brazil, rich in phenolic compounds and used on popular medicine as a wound healing agent, in the treatment of gastric lesions and as antimicrobial. Materials and Methods: Ultrassound-assisted extraction (UAE) was applied to extraction of epigallocatechin gallate (EGCG), total polyphenols (TP) and total tannins (TT) content from barks of Stryphnodendron adstringens (Mar.) Coville. Several operating parameters, namely extraction time (min), liquid to solid ratio (mg/mL), ethanolic strength (%, v/v), were optimized using response surface methodology (RSM) with a Box-Behnken design. Results: By using the desirability function approach, the optimum UAE conditions to obtain desirable extraction yields for all these metabolites simultaneously were found at the extraction time of 30 min, solid to liquid ratio of 4 mg/mL and ethanolic strength of 65. Under these conditions, the epigallocatechin gallate, total polyphenols and total tannins content were 0.31; 22.95 and 11.95 % (w/w), respectively. Conclusion: The results indicated that knowledge gained from this study should be helpful to further exploit and apply this resource and also showed the feasibility of ultrasound-assisted extraction for obtaining GEGC, TP and TT from barks of S. adstrigens.
  1 2,542 60
Isolation and identification of cytotoxic compounds from the rhizomes of Paris quadrifolia L.
Jerzy Gajdus, Zbigniew Kaczynski, Anna Kawiak, Ewa Lojkowska, Justyna Stefanowicz-Hajduk, J. Renata Ochocka, Piotr Stepnowski
May 2014, 10(38):324-333
DOI:10.4103/0973-1296.133289  PMID:24991111
Background: Paris quadrifolia L. is a medicinal plant which contains steroidal saponins. The present study reports isolation and structural identification of six pennogenyl saponins obtained from P. quadrifolia rhizomes. The four spirostan saponins were obtained from P. quadrifolia for the first time. The cytotoxic effects of the sub-fractions and six compounds isolated from the plant extract were evaluated on tumour cells. Materials and Methods: Ethanol extract from the rhizomes of P. quadrifolia were partinioned using column chromatography. The saponins were isolated from the obtained sub-fractions by isocratic RP HPLC and their structures were determined by means of 1D and 2D NMR spectroscopy and MALDI TOF MS. The cytotoxic effects of the sub-fractions and the isolated compounds were tested against human promyelocytic leukaemia cells (HL-60), human cervical adenocarcinoma cells (HeLa) and human breast cancer cells (MCF-7) using the [(3-(4,5-dimethylthiazol-2-yl)]-2,5-diphenyltetrazolium bromide (MTT) assay. Results: Six pennogenyl saponins were isolated from P. quadrifolia rhizomes: pennogenin 3-O-β-D-glucopyranoside (1), pennogenin 3-O-α-L-rhamnopyranosyl-(1→ 4)-β-D-glucopyranoside (2), pennogenin 3-O-α-L-rhamnopyranosyl-(1→ 2)-β-D-glucopyranoside (3), pennogenin 3-O-α-L-rhamnopyranosyl-(1→ 4)-α-L-rhamnopyranosyl-(1→ 4)-β-D-glucopyranoside (4), pennogenin 3-O-α-L-rhamnopyranosyl-(1→ 4)-[α-L-rhamnopyranosyl-(1→ 2)]-β-D-glucopyranoside (5), pennogenin 3-O-α-L-rhamnopyranosyl-(1→ 4)-α-L-rhamnopyranosyl-(1→ 4)-[α-L-rhamnopyranosyl-(1→ 2)]-β-D-glucopyranoside (6). Pennogenyl saponins 5 and 6 exhibited cytotoxic activity against HL-60, HeLa and MCF-7 tumour cells with IC 50 values of 1.0 ± 0.04 μg/ml, 1.8 ± 0.072 μg/ml and 2.4 ± 0.096 μg/ml respectively, and 2.0 ± 0.08 μg/ml, 2.5 ± 0.125 μg/ml and 3.2 ± 0.128 μg/ml respectively. Conclusion: Compounds 1 -4 were isolated from this species for the first time.
  1 3,032 57
Inhibition of LDL oxidation and oxidized LDL-induced foam cell formation in RAW 264.7 cells show anti-atherogenic properties of a foliar methanol extract of Scoparia dulcis
Sinjitha S. Nambiar, Nandini Prasad Shetty, Praveena Bhatt, Bhagyalakshmi Neelwarne
May 2014, 10(38):240-248
DOI:10.4103/0973-1296.133241  PMID:24991098
Background: Oxidation of low density lipoproteins and their further uptake by macrophages is known to result in the formation of foam cells, which are critical in the initiation of atherosclerosis through activation of inflammatory signalling cascades. Thus, powerful dietary antioxidants are receiving attention for the reversal of such pathological states. Materials and Methods: Extracts of Scoparia dulcis have been used as tea and health drinks with various health promoting effects. In the present study, we examined the reactive oxygen scavenging potential as well as anti-inflammatory and anti-atherogenic efficacies, using leaf extracts obtained after successive extraction with various solvents. Results: A methanol extract showed potent antioxidant activity with an IC 50 value of 570 μg/ml, caused hydrogen peroxide scavenging (28.9 µg/ml) and anti-inflammatory effects by improving human erythrocyte membrane stabilisation (about 86%). The methanol extract also efficiently inhibited lipid peroxidation and oxidation of low density lipoproteins, thus preventing foam cell formation in cultured RAW 264.7 cells. Furthermore, phytochemical screening of the extracts showed high accumulation of flavonoids. Conclusions: The foliar methanol extract of Scoparia dulcis has a strong anti-atherogenic potential and this property could be attributed maybe due to presence of flavonoids since HPLC analysis showed high concentrations of myricetin and rutin in the methanol extract.
  1 11,052 210
Efficiency and selectivity of triterpene acid extraction from decoctions and tinctures prepared from apple peels
Antonio C. Siani, Marcos J. Nakamura, Daniel S. dos Santos, Jose L. Mazzei, Adriana C. do Nascimento, Ligia M.M. Valente
May 2014, 10(38):225-231
DOI:10.4103/0973-1296.133236  PMID:24991096
Background: This study assessed the extraction efficiency of ursolic (UA) and oleanolic acids (OA), as well as the total phenols in aqueous and hydroethanolic extracts of dry apple peels at room temperature. Materials and Methods: After running preliminary assays on decoctions and tinctures (ethanol: water 7:3 v/v), the extracts from dried apple (cv. Fuji) peels were obtained by static maceration over varied intervals (2 to 180 days). The UA and OA content in the extracts was quantified by High Performance Liquid Chromatography with Diode Array Detection (HPLC-DAD) with a reversed phase column and isocratic elution (CH 3 CN/H 2 O/H 3 PO 4 ) against calibration curves (R 2 > 0.9995). The total phenol content in the extracts was evaluated spectrophotometrically at 760 nm using the Folin-Ciocalteau method referencing gallic acid. Results: UA and OA in the hydroethanolic extracts ranged from 3.63-6.12 mg/g and 2.12-3.30 mg/g, corresponding to 1.72-3.07 and 1.00-1.66 mg/g in the raw material, respectively. Higher values of triterpene acid content corresponded to maceration periods of 10 or 30 days. The residual phenol and polyphenol content ranged from 6.97 to 11.6 mg/g. The UA and OA yields, as well as the total phenol content, versus the maceration time were plotted in Control Charts within confidence intervals (95%) and were unaffected during the assayed period. Conclusion: Apple peel tinctures from 10% solids obtained at room temperature exhibited the highest content of triterpene acids when employing a maceration period of 10 to 30 days. Extracts prepared using this procedure contained an average of 7.33 mg/g of total triterpene acids and 10.6 mg/g phenolic compounds. These results establish supporting data for apple peel tinctures and their derived phytopharmaceuticals that are standardized on the ursolic-oleanolic acid content.
  1 2,419 79
The evolution of pharmacognosy in Iran, challenges, and developments
Soodabeh Saeidnia
May 2014, 10(38):441-442
DOI:10.4103/0973-1296.133298  PMID:24991125
  - 1,349 46
Phytochemical and anti-staphylococcal biofilm assessment of Dracaena draco L. Spp. draco resin
V. Di Stefano, R. Pitonzo, D. Schillaci
May 2014, 10(38):434-440
DOI:10.4103/0973-1296.133300  PMID:24991124
Background: Dracaena draco L. ssp. draco is known as the "dragon's blood tree" and it is endemic from the Canary Islands and Morocco. Objective: Carry out phytochemical investigation of acetonic extracts of red resin obtained from the trunk of D. draco, to obtain to the isolation of the most abundant resin constituents, belonging to the class of flavonoids: flavans, along with homoisoflavans and homoisoflavanones. Materials and Methods: The structures of the isolated compounds were established by Nuclear Magnetic Resonance (NMR) and mass spectrometry data and comparison with literature data. The acetonic extract was evaluated for its anti-staphylococcal properties against two reference strains. Results: The acetonic extracts resulted inactive at the maximum tested concentration of 1000 μg/ml against free living forms of tested staphylococci, but they showed a very interesting activity in the prevention of a biofilm formation at a concentration equal to 200 μg/ml against S. aureus ATCC 25923.
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Dietary supplementation of chloroquine with nigella sativa seed and oil extracts in the treatment of malaria induced in mice with plasmodium berghei
Promise Madu Emeka, Lorina Ineta Badger-Emeka, Chiamaka Maryann Eneh, Tahir Mahmood Khan
May 2014, 10(38):357-362
DOI:10.4103/0973-1296.133282  PMID:24991115
Background: The aim of the study was to investigate the effects of dietary combination of Nigella sativa seed and oil extracts with chloroquine (CQ), and how these combinations enhance CQ efficacy in mice infected with Plasmodium berghei and their survival rates. Materials and Methods: Chloroquine sensitive P. berghei, NK65 strain was used for the study. This was passaged intraperitoneally into albino mice with a 0.2ml standard inoculum consisting of 10 6 parasitized erythrocyte suspension in phosphate buffer solution (PBS). Parasitaemia was ascertained by microscopical examination of blood films under oil immersion at X100 magnification. Results: Nigella sativa seed in feed (NSSF), NSSF + CQ on day 4, produced 86.1% and 86.0% suppression respectively, while Nigella sativa oil extract in feed (NSOF) and in combination with CQ had 86.0% and 99.9% suppression respectively. The degree of suppression with the combination was significantly higher compared to CQ alone (P < 0.001) (36.1%). Complete parasitaemia clearance was obtained on the 20 th and 15 th day of treatment for NSSF, NSSF + CQ respectively, while that for NSOF and NSOF + CQ was on days 26 and 12 respectively. For CQ parasite clearance was 12 days with treatment. Also, the combinastion of 10 mg/kg Nigella sativa oil treatment injected intraperitoneally with oral CQ produced very significant parasite suppression (P < 0.0001) (93%). Survival rate in NSSF and NSOF and in combination with CQ groups was 100 and 60.0% for CQ alone. Conclusion : sThis study shows that the use of Nigella sativa seed and oil extract as dietary supplements in combination with CQ has a potential in enhancing the efficacy of CQ and could be of benefit in management of malaria.
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Two novel antifungals, acornine 1 and acornine 2, from the bark of mangrove plant Aegiceras corniculatum (Linn.) Blanco from Sundarban Estuary
Vinod K. Gupta, Kalishankar Mukherjee, Amit Roy
May 2014, 10(38):342-349
DOI:10.4103/0973-1296.133293  PMID:24991113
Background: Microbes have been implicated in a wide variety of human diseases many of which are of life-threatening nature. New antimicrobials are urgently needed not only for combating these organisms but also to counter the menace of the harmful microbes developing resistance against drugs at alarming rates. Mangrove plants are rich sources of secondary metabolites having many beneficial biological activities including antimicrobial ones. True to this fact, this report describes identification, isolation and partial characterization of two novel antifungal compounds from Aegiceras corniculatum, a mangrove plant from Indian Sundarban estuary. Materials and Methods: Two compounds, named as Acornine 1 and Acornine 2, having antifungal activities were isolated from the bark of A. corniculatum, a mangrove plant, by using standard techniques. The compounds were characterized using routine microbiological and physicochemical methods. Results: Partial structural characterization of the two compounds indicated they are oleanane triterpenoids with linked sugar moieties. While both the compounds exhibited growth inhibition in tested Gram positive bacteria, Acornine 2 in particular demonstrated strong antifungal activities against several pathogenic fungi tested. Results also indicated that various environmental factors may govern the secondary metabolite profiles of the same mangrove plants growing in different geographical areas. Conclusion: Tissue extracts of Aegiceras corniculatum, a mangrove plant from Indian Sundarban estuary, exhibited the presence of remarkable antifungal activities. The isolated compounds responsible for such activities, named as Acornine 1 and Acornine 2, appear to have potential in food processing and health care industry. They need to be studied further.
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Simultaneous determination of 11 bioactive compounds in Jaeumganghwa-tang by high performance liquid chromatography-diode array detection
Bo-Ra Yun, Jin Bae Weon, Jiwoo Lee, Min Rye Eom, Choong Je Ma
May 2014, 10(38):256-263
DOI:10.4103/0973-1296.133267  PMID:24991100
Background: Jaeumganghwa-tang (JEGH) is a traditional Korean herbal medicine for the treatment of chronic bronchitis, nephritis and diabetes mellitus. Objective: A high performance liquid chromatography-diode array detector (HPLC-DAD) method was developed for simultaneous determination of 11 major compounds such as 5- hydroxymethylfurfural, mangiferin, paeoniflorin, nodakenin, naringin, hesperidin, decursinol, berberine, glycyrrhizin, atractylenolide III and decursin, in JEGH. Materials and Methods: The separation was conducted on Shishedo C 18 column with gradient elution of 0.1% trifluoroacetic acid-acetonitrile. Detection of wavelength was set at 205, 250, 280 and 330 nm. Results: The developed analysis showed a good linearity (R2 >0.9997). The range of limit of detection and limit of quantification were observed from 0.04 to 0.43 and from 0.11 to 1.30, respectively. The intra- and inter-day test relative standard deviations (RSD) were less than 3% and the accuracy was 95.98-108.44%. The recoveries were between 92.75% and 109.19% and RSD range of recoveries was measured from 0.52% to 2.78%. Conclusion: This HPLC-DAD method can be successfully applied for simultaneous determination of 11 major compounds in JEGH samples.
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An attempt to stabilize tanshinone IIA solid dispersion by the use of ternary systems with nano-CaCO 3 and poloxamer 188
Hong-mei Yan, Zhen-hai Zhang, Yan-rong Jiang, Dong-mei Ding, E. Sun, Xiao-bin Jia
May 2014, 10(38):311-317
DOI:10.4103/0973-1296.133286  PMID:24991109
Background: Tanshinone IIA (TSIIA) on solid dispersions (SDs) has thermodynamical instability of amorphous drug. Ternary solid dispersions (tSDs) can extend the stability of the amorphous form of drug. Poloxamer 188 was used as a SD carrier. Nano-CaCO 3 played an important role in adsorption of biomolecules and is being developed for a host of biotechnological applications. Objective: The aim of the present study was to investigate the dissolution behavior and accelerated stability of TSIIA on solid dispersions (SDs) by the use of ternary systems with nano-CaCO 3 and poloxamer 188. Materials and Methods: The TSIIA tSDs were prepared by a spray-drying method. First, the effect of combination of poloxamer 188 and nano-CaCO 3 on TSIIA dissolution was studied. Subsequently, a set of complementary techniques (DSC, XRPD, SEM and FTIR) was used to monitor the physical changes of TSIIA in the SDs. Finally, stability test was carried out under the conditions 40°C/75% RH for 6 months. Results: The characterization of tSDs by differential scanning calorimetry analysis (DSC) and X-ray powder diffraction (XRPD) showed that TSIIA was present in its amorphous form. Fourier transforms infrared spectroscopy (FTIR) suggested the presence of interactions between TSIIA and carriers in tSDs. Improvement in the dissolution rate was observed for all SDs. The stability study conducted on SDs with nano-CaCO 3 showed stable drug content and dissolution behavior, over the period of 6 months as compared with freshly prepared SDs. Conclusion: SDs preparation with nano-CaCO 3 and poloxamer 188 may be a promising approach to enhance the dissolution and stability of TSIIA.
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Efficacy of Acorus calamus on collagen maturation on full thickness cutaneous wounds in rats
Thangavel Ponrasu, Karuppanan Natarajan Madhukumar, Moorthy Ganeshkumar, Kuttalam Iyappan, Vilvanathan Sangeethapriya, Vinaya Subramani Gayathri, Lonchin Suguna
May 2014, 10(38):299-305
DOI:10.4103/0973-1296.133283  PMID:24991107
Background: The rhizomes of Acorus calamus and their essential oil are widely used in the flavoring industry and production of alcoholic beverages in Europe. Recent reports have confirmed the presence of several pharmacological components in the rhizomes of A. calamus. Objective: The objective of this study was to find out the efficacy of topical administration of ethanolic extract of A. calamus on dermal wound healing in rats. Wound healing is a natural process occurring in living organisms, which results in a complete or partial remodeling of injured tissue and ultimately progresses to the formation of a fibrous scar. Several natural products have been reported to augment the wound healing process. Materials and Methods: An ethanolic extract of A. calamus was prepared and its wound-healing efficacy was studied. An excision wound was made on the back of the rat and 200 μL (40 mg/kg body weight) of the A. calamus extract was applied topically once daily for the treated wounds. The control wounds were treated with 200 μL of phosphate buffered saline. Results: The granulation tissues formed were removed at 4, 8 and 12 days and biochemical parameters such as deoxyribonucleic acid, total protein, total collagen, hexosamine and uronic acids were measured. The amount of type I/III collagen formed in control and treated wound tissues was evaluated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The epithelialization time, tensile strength and histological examination of the wounds were also studied. Biochemical analyses of the granulation tissues revealed a significant increase in collagen, hexosamine and uronic acid when compared with the control. The tensile strength of extract treated wounds was found to increase by 112%. A significant reduction in lipid peroxide levels suggested that A. calamus possesses antioxidant components. Conclusions: The results strongly confirm the beneficial effects of A. calamus in augmenting the wound healing process.
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Study on the in vivo toxic mechanism of xixin based on trace elements determination by inductively coupled plasma-mass spectrometry
Bao Yong-Rui, Yang Xin-Xin, Wang Shuai, Meng Xian-Sheng, Zhu Rui-Qing, Xia Yue-Ming, Cai Lin
April-June 2014, 10(38):141-146
DOI:10.4103/0973-1296.131025  PMID:24914279
Background: Xixin has been widely used as a traditional Chinese medicine for headache, toothache and inflammatory diseases. Clinical investigation indicated that adverse drug reactions occurred with an overdose of xixin, but the toxic mechanism of xixin in vivo based on trace elements has not been researched yet. Objective: To explore the in vivo toxic mechanism of xixin induced by trace elements. Materials and Methods: The contents of trace elements in the serum and liver of mice were determined by inductively coupled plasma-mass spectrometry (ICP-MS) after obtaining xixin extracts. Principal component analysis (PCA) and cluster analysis (CA) were performed between the trace elements' content and dosage using the software GeneSpring 12.1 to analyze the main toxic elements in vivo. Results: Trace elements' contents were obviously raised after xixin extracts were taken as a dosage of 150 mg/mL and 50 mg/mL, respectively. Na, Ca, Cu and Cd in serum and Ca and Zn in liver were the main trace elements inducing the toxic reaction of xixin. Conclusion: Xixin possesses the potential function of indirectly upregulating trace elements in vivo. This study, for the first time, elucidated the in vivo toxic mechanism of xixin based on trace elements. This method could also be utilized in the research of corresponding aspects.
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Pretreatment with Assafoetida exerts dose-dependent dual effects on rat hearts
Mansour Esmailidehaj, Mohadeseh Kakoo, Mohammad Ebrahim Rezvani, Mohammad Hossein Mosaddeghmehrjardi
April-June 2014, 10(38):147-153
DOI:10.4103/0973-1296.131026  PMID:24914280
Context: Although many studies displayed the favorable effects of Assafoetida, some of them reported that high doses of Assafoetida could lead to harmful effects. Aims: In this study, the effect of pretreatment with Assafoetida investigated on ischemic-reperfusion injury in isolated rat heart model. Materials and Methods: Thirty two male Wistar rats were divided into 4 groups of eight. Group 1 as the control (Con) group and three other groups as the treatment groups that given Assafoetida by gavage at levels of 25, 50 and 100 mg/kg, once a day for four weeks (T25, T50 and T100 groups). Then their hearts were subjected to 30 min global ischemia and 90 min reperfusion under langendorff apparatus. Results: The data shown that hemodynamic parameters including left ventricular developed pressure (LVDP) and maximum and minimum of pressure changes (±dp/dt) were increased in T25 and decreased in T50 and T100 groups during reperfusion in comparison with Con group. There was not any significant difference in the incidence of irreversible ventricular fibrillation between T25 and Con group, while it was increased in T50 and T100 groups significantly. There was not any significant difference in infarct size between all groups. Conclusion: These data indicate that pretreatment of rats with Assafoetida have cardioprotective effects in low doses and cardiotoxic effects in higher doses. Therefore, it needs more investigation in the future.
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The extracts of Japanese willow tree species are effective forapoptotic desperation or differentiation of acute myeloid leukemia cells
Kounosuke Fujita, Yuji Nomura, Masahiko Sawajiri, Pravat K Mohapatra, Hany A El-Shemy, Nguyen T Nguyen, Masashi Hosokawa, Kazuo Miyashita, Teruo Maeda, Hirofumi Saneoka, Shohei Fujita, Takayuki Fujita
April-June 2014, 10(38):125-131
DOI:10.4103/0973-1296.131023  PMID:24914277
Background: The antileukemic activity of hot water extract of plant parts of some Japanese willow tree species grown at different levels of nitrogen were examined. Materials and Methods: Water extracts of willow leaves were prepared for this studies in different level of nitrogen nutrition. Results: The extracts obtained from the leaves and stem exhibited anti-leukemic activities prominently. The crude hot water extracts of the young growing parts including apex, matured leaves and stem, killed the blasts of acute myeloid leukemia (AML) cells, (HL60 and NB4) after 48h incubation, however, such desperation was far less in the root extract. Similar to the plant parts, response of extracts obtained from different willow species was not identical; the proportion of dead cells relative to whole cells of the culture medium ranged from 21% to 93% among the species. Leaf extracts obtained from the responsive willow species decreased the live cell percentage and increased the dead cell percentage at higher level of nitrogen nutrition. The mode of desperation of leaf extract treated AML cells in such species appeared to be cell apoptosis as shown by binding with fluorescein isothiocyanate (FITC) -labeled Annexin V. Conclusion: Differentiation of alive AML cells continued unabated and apoptosis was poor when extract of an unresponsive species added to the culture medium.
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Study on interaction between plasmid DNA and berberine derivatives with aliphatic chain by fluorescence analysis
Yang Yong, He Kai, Zhang Bao-Shun, LI Xue-Gang
April-June 2014, 10(38):97-100
DOI:10.4103/0973-1296.131017  PMID:24914272
In this study, the fluorescence analysis was used to reveal the interaction between berberine derivatives and plasmid DNA. The results showed that berberine (C0) and its 8-alkyl derivatives can enhance the fluorescent intensity of plasmid DNA. Compared with 8-dodecyl- (C12) and 8-hexadecyl- (C16) berberine, 8-alkylberberine with shorter alkyl group, such as 8-ethyl (C2), 8-butyl (C4), 8-hexyl (C6), and 8-octyl (C8) berberine derivatives showed higher fluorescence increasing effect. Among all compounds, C4 showed highest fluorescence increasing effect. All compounds tested obviously enhanced fluorescent intensity at the concentration of 6.25 × 10−5 mol/L. These results suggested that berberine and its derivatives can be selectively inserted to the grooves running down the plasmid DNA helix, thus, lead to the increase of fluorescence intensity of the reaction system. Also, adding proper length of aliphatic chain to berberine could promote the interaction between DNA and berberine derivatives. The results of this study may lay some useful foundation for the development of berberine-based medicine agents.
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Analysis of the metabolites of mesaconitine in rat blood using ultrafast liquid chromatography and electrospray ionization mass spectrometry
Peng Tan, Xin Chen, Ruirui He, Yonggang Liu
April-June 2014, 10(38):101-105
DOI:10.4103/0973-1296.131019  PMID:24914273
Background: Mesaconitine is the main active component of genus aconitum plants that are widely used in clinics in China. However, little has been known about the metabolic pathway of mesaconitine. Objective: To explore the metabolites and propose the pathway of mesaconitine. Materials and Methods: In the present study, mesaconitine (4 mg kg−1 ) was orally administered to male rats. Then, blood samples collected were pretreated using solid-phase extraction technique with C18 cartridges, and analyzed using LC/MS/MS method with electrospray ionization. Both positive ion mode and collision induced dissociation (CID) were used to elucidate the structures of the major metabolites of mesaconitine. Results: Ten compounds were identified, among which seven were new metabolites, and the metabolic pathway was proposed. The protonated molecular ions of seven new metabolites were at m/z 648, 618, 616, 602, 572, 468, and 542, multistage fragment ions with neutral loss of 28 u (CO), 60 u (CH 3 COOH), 18 u (H 2 O), and 32 u (CH 3 OH). These new metabolites detected firstly in vivo, were named 10-hydroxyl-mesaconitine, hypaconitine, dehydrated mesaconitine 16-O-demethylmesaconitine, 16-O-demethylhypaconitine, and 16-O-demethyl-dehydrated hypaconitine, respectively. Furthermore, the breaking sequence of methoxyl was obtained using quantum chemistry. Conclusion: The study proved that the method of solid-phase extraction technique coupled with MS and quantum chemistry can be applied to the analysis of metabolites in plasma quickly and conveniently.
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