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   2019| July-September  | Volume 15 | Issue 64  
    Online since August 23, 2019

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Anti-diabetic activities of Dactylorhiza hatagirea leaf extract in 3T3-L1 cell line model
Murad Alsawalha, Abeer Mohammed Al-Subaei, Reem Yousuf Al-Jindan, Srinivasa Rao Bolla, Dwaipayan Sen, Janardhana Papayya Balakrishna, Padma Kanchi Ravi, Shiva Shankar Reddy Gollapalli, Vishnu Priya Veeraraghavan, Aruthra Arumugam Pillai, Joel Palpath Joseph, Mohammed Salahuddin, Surapaneni Krishna Mohan
July-September 2019, 15(64):212-217
Background: Diabetes is an endocrine disorder that results in altered carbohydrate, protein, and lipid metabolism. Several synthetic drugs used to treat diabetes have adverse effects on prolonged usage. This has given the impetus to the search for alternative medicines with no or less side effects. The plants of Orchidaceae family have displayed antimicrobial, anti-inflammatory, antioxidant, anticancer, and antidiabetic activity. However, their antidiabetic properties are yet to be explored. Materials and Methods: The in vitro antidiabetic properties of Dactylorhiza hatagirea leaf extract were studied by biochemical assays such as α-amylase and α-glucosidase inhibition assays and in vitro cellular assays such as glucose uptake assay and glucose transporter type 4 (GLUT4) expression studies in 3T3-L1 cell line. Results: The methanolic extract of D. hatagirea, at varying concentrations (25 μg-400 μg/mL), did not exhibit cytotoxicity against 3T3-L1 cell line after 24 h of incubation. Methanolic extract of D. hatagirea leaves showed significant inhibition of α-Amylase and α-Glucosidase enzymes. After 24 h of exposure of 3T3-L1 cells to 100 μg/mL of D. hatagirea leaf extract and 100 μM of metformin, the relative expression rates of GLUT4 receptor were elevated when compared with untreated cells. The results also revealed that the amount of 2-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl) Amino)-2-Deoxyglucose taken up by 3T3-L1 cells treated with D. hatagirea leaf extract and metformin is higher than that of untreated cells. Conclusion: Our results suggest that methanolic extract of D. hatagirea leaves has potential antidiabetic activity and could be a plausible resource for antidiabetic agents.
  3,180 217 -
Primary skin irritation and dermal sensitization assay: In vivo evaluation of the essential oil from Piper sarmentosum Roxb.
Nor Zafirah Abu Bakar, Hidayatulfathi Othman, Nor Fadilah Rajab, Siti Balkis Budin, Ahmad Fuad Shamsuddin, Nor Azwani Mohamed Nor
July-September 2019, 15(64):352-358
Background: Piper sarmentosum Roxb. is a traditional medicine which can also be consumed as a vegetable. Despite the availability of a variety of toxicological data on extracts of this plant, to our knowledge, until now, no dermal toxicological tests have been conducted. The aim of the present study was, therefore, to carry out in vivo assays to verify the safety of application of P. sarmentosum extract gel on the skin. Materials and Methods: The essential oils were extracted from the dried leaves of P. sarmentosum by hydrodistillation and then formulated into a gel. An in vivo skin irritation test of the P. sarmentosum extract gel was then conducted on albino rabbits, and an in vivo sensitization test was carried out on albino guinea pigs. Results: For both abraded and non-abraded sites, the calculated primary irritation index value for P. sarmentosum was 2.55, indicating that topical use of a gel with P. sarmentosum (1.55%) is nonirritative. However, a dermal sensitization assay revealed mild sensitization effects in 1 out of 10 guinea pigs in response to the application. Histological analysis revealed a slight thickening of the stratum corneum epidermis layer in the guinea pigs' skin. Conclusion: Together, these results indicate that the gel with P. sarmentosum is safe for application on the skin, but may lead to sensitization upon repeated application.
  2,996 273 -
Identification and quantification of fucoxanthin in selected carotenoid-producing marine microalgae and evaluation for their chemotherapeutic potential
Muthukumaran Peraman, Saraswathy Nachimuthu
July-September 2019, 15(64):243-249
Background: Although there are about 18,500 compounds have been isolated and reported from marine resources, the prominence of drug discovery research on marine microalgae is still very less while comparing to other natural resources. Hence, this investigation was designed, especially on some carotenoid-producing marine microalgae to evaluate their chemotherapeutic efficacies including antibacterial, antifungal, antioxidant, hemolytic, and anthelmintic activities. Objective: The objective of this research is to evaluate the suitability of the selected marine microalgae for biological activities and to perform the identification and quantification of fucoxanthin in their methanol extracts using high-performance liquid chromatography (HPLC)–diode-array detector technique. Materials and Methods: The methanolic extracts of all 10 marine microalgae were screened for antibacterial, antifungal, antioxidant, hemolytic, and anthelmintic activities. The fucoxanthin was identified and quantified by thin-layer chromatography and HPLC techniques, respectively. Results: Among the test microalgae, Isochrysis galbana (IG) showed the presence of the highest concentration of fucoxanthin (5.93 mg/g dry weight) and also exhibited notable antioxidant activities (86%) at 80 mg/mL. In antimicrobial activities, Dunaliella salina (DS) demonstrated the promising antimicrobial activities (minimum inhibitory concentration [MIC]: 40 mg/mL) against Gram-negative bacteria and fungi while Thalassiosira species showed activity (MIC: 40 mg/mL) against Staphylococcus aureus and fungi. It was also noted that all test extracts were resistant to Escherichia coli. In anthelmintic activity against Pheretima posthuma, there are two microalgae, namely IG and Chaetoceros gracilis, exhibited considerable anthelmintic potential (with P < 0.01). Conclusion: From this study, it was concluded that DS and IG could serve as a promising source for further investigation to discover new antimicrobial leads and also demonstrated the positive correlation with the carotenoid content.
  2,541 366 -
Potential Cyclooxygenase (COX-2) enzyme inhibitors from Myrica nagi-from in-silico to in-vitro investigation
HP Prashanth Kumar, Prachurjya Panda, Prashantha Karunakar, Kotikalapudi Shiksha, Laxmi Singh, Nijalingappa Ramesh, Talambedu Usha, Sushil Kumar Middha
July-September 2019, 15(64):280-287
Introduction: Myrica nagi Thunb. (family Myricaceae) are actinorhizal plants showing symbiotic interaction with Frankia. Inhibition of cyclooxygenase-2 (COX-2) enzyme is known to be significant in preventing inflammation and in therapeutics. Objectives: Our principal focus was to identify COX-2 enzyme inhibitors, safer and natural anti-inflammatory compounds from M. nagi. Protein–ligand interaction has a significant role in structure-based drug design. Materials and Methods: Sixty-eight phytochemicals were therefore screened and evaluated for their binding energies with COX-2. These phytoconstituents were screened and analyzed for drug Likeliness along with Lipinski's rule of five. The X-ray crystallographic structure of the target COX-2 (protein data bank [PDB] ID: 4PH9), obtained from PDB, was docked with PubChem structures of phytochemicals using AutoDock 4.2 that uses Lamarckian genetic algorithm. Further, myricetin was subjected to in vitro anti-inflammatory assay using RAW-264.7 cell lines and inhibitory concentration (IC50) value was also determined. Results: The myricetin, myricitrin, and corchoionoside-C inhibited COX-2 with − 6.52, −4.94, and − 4.94 Kcal/mol binding energies, respectively, comparable to ibuprofen. Eventually, bioactivity score and absorption distribution metabolism excretion-toxicity properties showed considerable biological activities as G protein-coupled receptor, nuclear receptor, protease inhibitor, and enzyme inhibitors for myricetin, myricitrin, and corchoionoside-C phytochemicals. Molecular docking revealed hydrophobic interactions followed by four, nine, and four numbers of hydrogen bonds between myricetin, myricitrin, and corchoionoside-C, respectively, within the binding site of COX-2. Flavonol myricetin showed 112 μg/mL as IC50 value when it was subjected to in vitro cytotoxicity assay. These results clearly demonstrated that myricetin, myricitrin, and corchoionoside-C could act as highly potential COX-2 inhibitors. Therefore, in silico and in vitro studies revealed that of three best phytochemicals, myricetin could be promising candidate.
  2,314 211 -
Anti-adipogenic effect of Terminalia chebula fruit aqueous extract in 3T3-L1 preadipocytes
Anuj Kumar Borah, Pooja Rani Kuri, Archana Singh, Sougata Saha
July-September 2019, 15(64):197-204
Background: Phytoextracts, due to its complex nature of formulations yet little or no side effects, have been pursued as alternative medicine for the treatment of complex metabolic disorders such as obesity. One of the appealing strategies to achieve this is the modulation of adipocyte development and function with the treatment of phytoextracts. The current study explored the activity of Terminalia chebula fruit, a component of Ayurveda formulation “Triphala” on these aspects of adipogenesis. Materials and Methods: The effect of T. chebula aqueous fruit extract (CAFE) on the process of adipocyte development and function was investigated. To test the effect of CAFE on adipocyte development, 3T3-L1 preadipocytes were differentiated in the presence and absence of CAFE followed by estimation of lipid content and expression of adipogenic genes. To test its effect on adipocyte function, mature 3T3-L1 adipocytes were treated with the extract followed by estimation of lipolysis. Results: Treatment of 3T3-L1 preadipocytes with this extract had efficiently inhibited differentiation and lipid accumulation in these cells. Gene expression of key adipogenic regulators, peroxisome proliferative-activated receptor γ and C/CAAT enhancer-binding protein α, was suppressed due to the treatment with CAFE. Preadipocytes exposed to CAFE also showed suppressed expression of important adipogenic effector genes such as perilipin 1 and fatty acid synthase. Treatment of differentiated adipocytes with CAFE did not affect total lipid contents of the cells. However, CAFE treatment reduced lipolysis to a small extent. Conclusion: CAFE is an anti-adipogenic and anti-lipolytic agent which inhibits adipocyte differentiation by downregulating expression of key adipogenic genes.
  1,982 216 -
Nanoencapsulation of Tinospora cordifolia (Willd.) using poly (D, L-lactide) nanoparticles: Yield optimization by response surface methodology and in silico modeling with insulin receptor tyrosine kinase
A Ragavee, Selvaraj Asha Devi
July-September 2019, 15(64):218-227
Background: Tinospora cordifolia (TC) is a widely used shrub in Ayurveda system of medicine. The main chemical constituent reported from this shrub is alkaloid with nitrogen heterocycles such as tropane alkaloids, thiazole, piperidines, and pyridine derivatives; nonisoprene indole alkaloids; and pseudoalkaloids with antidiabetic effects. Materials and Methods: The nanoparticles (NPs) were synthesized via solvent evaporation method using a biodegradable poly(D,L-lactide) (PLA) polymer. The NPs were then characterized using spectroscopic methods, X-ray diffraction, and scanning electron microscopy. Release profile and entrapment efficiency of the NPs are studied. Further, the synthesized NPs were evaluated for the inhibitory activity to find the antidiabetic potential and compared with docking analysis. Results: In this study, the TC extract was loaded to PLA NPs by the solvent evaporation method. The synthesis of NPs is sonicated at 40% amplitude at 30 s to get 48% of yield. The loading efficiency was found to be 76.21% for 5 mg and 58.10% for 10 mg. Release profile was observed with controlled release up to 8 h and 70% of TC was released after 40 h. Release kinetic showed good correlation with Higuchi kinetics. The maximum inhibitory percentage of TC-loaded PLA NPs was found to be 92.59 ± 0.854 and shows potential activity for diabetes. The interaction of the compounds with the receptor, fentanyl, and cholic acid showed that the highest binding energies of −6.09 and −6.4 have the potential to activate the insulin receptor. Conclusion: The result proves that TC stem extract possesses a therapeutic effect on diabetes and it is noticeable that acarbose interaction with insulin receptor shows minimum binding affinity when compared to the compounds from mass spectrum shows the highest binding affinity which acts as an insulin activator and responsible for the inhibitory action of α-glucosidase.
  1,864 154 -
Morinda Citrifolia (Noni) fruit protects the exocrine pancreatic dysfunction against L-arginine induced acute pancreatitis in rats
Veena Gadicherla, Siva Reddy Challa, Mandava V Basaveswara Rao, Pavan Kumar Kunda, Ramakrishna Prudhvi
July-September 2019, 15(64):328-334
Background and Objective: Morinda citrifolia (MC) commonly known as Noni is being used for many ailments and is considered as wellness drink. It is traditionally used for anti-inflammatory, anti-aging, and immunostimulant properties. The present study has been initiated to investigate the protective effects of MC fruit extract (MCFE) on L-arginine-induced acute pancreatitis (AP) in rats. Materials and Methods: Male Sprague-Dawley rats were randomly divided into groups of control, disease control, positive control, and treatment groups. AP is induced by the administration of a single dose of L-arginine (2 × 2.5 g/kg, intraperitoneally, 1 h apart). Positive control received melatonin (10 mg/kg); treatment groups received 200 mg/kg and 400 mg/kg MCFE 6 days before administration of L-arginine. After 12 h of induction, the serum samples were analyzed for biomarker enzymes such as amylase, lipase, C-reactive protein, superoxide dismutase, glutathione, catalase, tissue nitrate, lactate dehydrogenase, and myeloperoxidase. Histopathological studies and deoxyribonucleic acid (DNA) fragmentation assay were performed from the isolated pancreatic tissue. Results: MCFE administration showed a dose-dependent significant (P < 0.001) protective effect by improving the levels of antioxidant enzymes and reducing the elevated levels of amylase and lipase. The acinar cell damage was limited in histopathological findings and an intact DNA when compared to disease control. Conclusion: MCFE administration showed a protective effect against AP in rats, and it may be due to the attenuation of oxidative stress. Further investigation for the exact molecular mechanism is needed.
  1,812 144 -
Cell cycle arrest and apoptosis in human liver cancer cell line and A549 cell lines by Turbiconol– A novel sterol isolated from Turbinaria conoides
Kala K Jacob, KJ Prashob Peter, S Muraleedharan Nair, N Chandramohanakumar
July-September 2019, 15(64):189-196
Background: Turbinaria conoides, a brown seaweed, is a rich source of oxygenated fucosterols which are capable of suppressing the proliferation of cancer cells. Their specific therapeutically significant biological activity is directly related to the unique structural features of the molecule. This study specifically focuses on extracting unconventional sterol molecules (side chain extension) from this seaweed which can be used as a lead molecule to evolve therapeutical agents. Materials and Methods: To isolate unconventional sterol molecule, for structural elucidation and bioactivity study, sufficient amount of T. conoides was collected from Mandapam, an unique biodiverse environment along the Southeast coast of India. State-of-the-art methods available for the purification and characterization of molecule (High-resolution fast-atom bombardment mass spectrometry, ultraviolet-visible spectroscopy, attenuated total reflection–fourier transform infra-red, One-dimensional nuclear magnetic resonance, and two-dimensional nuclear magnetic resonance) were put in. In vitro bioassays (3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium bromide, double staining, and flowcytometry) were carried out against A549 and human liver cancer cell line (HepG2) malignant cells to assess the cytostatic potential. Data were statistically validated. Results: A unique unconventional sterol molecule (Turbiconol) with ethyl and methyl group at C-27 was isolated. This molecule induced apoptosis in A549 and HepG2. However, cell cycle assessment revealed G0/G1 cell cycle arrest in Hep G2 and G2/M checkpoint was responsible for the suppression of A549 cell line. Conclusion: A novel unconventional compound, turbiconol, is reported in this study. In vitro results highlight the potential of this molecule in developing therapeutical combination which can be used for novel treatment methods.
  1,651 136 -
The antioxidant paradox
Ashok Kumar Tiwari
July-September 2019, 15(64):173-175
  1,607 120 -
Evaluation of the effectiveness of Acmella uliginosa (Sw.) Cass. flower methanolic extract in pain amelioration and memory impairment in the experimental rat models: Search for an alternative remedy over opioid painkillers
Subhashis Paul, Debabrata Modak, Somit Dutta, Tapas Kumar Chaudhuri, Soumen Bhattacharjee
July-September 2019, 15(64):335-345
Background: The flower of Acmella uliginosa (AU) (Sw.) Cass., a naturally grown herb in India, is consumed as a natural painkiller for its notable analgesic properties. Objective: The objective of the study was to establish the role of AU flower methanolic extract in antinociception and its neuromodulatory activities to assess any disadvantage of the drug akin to opioids. Materials and Methods: In experimental rats, plant flower extracts were fed at a dose of 100 mg and 200 mg/kg body weight (BW) for 14 days. Analgesic activity was evaluated through formalin-induced paw licking test. T-maze, novel object recognition (NOR), and rotarod tests were done to assess the role of the extract in memory alteration and neuromotor coordination, respectively. Acetylcholinesterase (AChE), reduced glutathione (GSH), and superoxide dismutase (SOD) activity from the brain homogenates were done to assess the induced oxidative stress. Results: The plant proved to be a promising analgesic when fed orally up to 200 mg/kg BW dose. No acute toxicity was seen up to 1000 mg/kg. In the T-maze test, extract-fed animals showed a reduction in food searching time. In NOR test, the discrimination index between new and familiar objects was high in extract-fed animals compared to standard group. In rotarod test, the extract did not alter the neuromotor coordination. AChE, GSH, and SOD activities were normal in extract-treated animals. Conclusion: Memory alteration and oxidative stress are two major drawbacks associated with opioid drugs. Our results indicate that the AU flower methanolic extract qualifies as a potent painkiller and overcomes the disadvantages of opioid analgesics.
  1,544 119 -
Impact of microwaves on the extraction yield of phenolics, flavonoids, and triterpenoids from centella leaves: An approach toward digitized robust botanical extraction
Kamal Kumar Sen, Kavi Bhushan Singh Chouhan, Roshni Tandey, Rajendra Mehta, Vivekananda Mandal
July-September 2019, 15(64):267-273
Introduction: A novel green approach of microwave-based extraction of botanicals for improved yield of bioactives has been investigated. In this regard, leaves of Centella asiatica which has a rich history of ethomedicinal use were chosen. Objective: The aim of this study is to develop a robust optimized microwave-based extraction protocol for improved yield of phenolics, flavonoids, and triterpenoids principles. Materials and Methods: Microwave power and extraction time were critically optimized along with the effect of moisture content through sample pretreatment. Effect of optimized operating conditions on the biological integrity of the extract and on the extraction of other nutraceutical principles was also evaluated. Results were compared to traditional extraction methods. Results: The final optimum extraction conditions were 50% microwave power, 6-min irradiation time, and 54% moisture content for maximum yield of phenolics and triterpenoids, whereas for flavonoids, optimum microwave power was 40% with other conditions remaining same. The proposed method was found to be three-fold better than 36 h of Soxhlet extraction and produced 200 times lesser carbon load than Soxhlet. Improved yield of other nutraceutical principles with better anti-oxidant activity was recorded for the proposed method. Conclusion: Switching to such greener technology is now the need of the hour. This research is a sincere effort to showcase the potential of green chemistry in the herbal drug industry.
  1,472 163 -
Anti-proliferative and apoptotic effects of Rheum emodi on human breast adenocarcinoma, MCF-7 Cells, and antimicrobial effectiveness against selected bacterial strains
Juhi Rais, Asif Jafri, Shabana Bano, Neelam Shivnath, Madhu Tripathi, Md Arshad
July-September 2019, 15(64):237-242
Background: Breast cancer is the most common gynecological malignancy and one of the leading causes of death in women worldwide. Since antiquity to date, the saga of usage of plants as medicines has been the mainstay among the people. In Ayurvedic and Unani systems of medicine, Rheum emodi (RE) commonly known as Revand chini or Rhubarb is an important medicinal plant. It is a perennial herb belonging to family Polygonaceae and has antimicrobial, anticarcinogenic, and anti-inflammatory properties. The rhizomes of RE have anthraquinone derivatives such as emodin, aloe-emodin, rhein, emodin glycoside, and chrysophanol glycosides. Objective: In this study, we have investigated the anti-cancerous potentials of RE ethanolic extract on human breast adenocarcinoma cells MCF-7 and its antimicrobial effect against selected pathogenic bacterial strains. Materials and Methods: The apoptotic and anti-proliferative potentials of RE on human breast adenocarcinoma cells MCF-7 were observed through cell viability (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide [MTT]), reactive oxygen species (ROS) generation, nuclear fragmentation, and mitochondrial membrane potential (MMP) analysis. Antimicrobial activity of RE was screened through well-diffusion assay. Results: The results show that RE significantly inhibits the proliferation and induces apoptosis in MCF-7 cells of breast adenocarcinoma in a dose-dependent manner. The MTT cellular viability assay and morphological study reveal that RE significantly induces morphological alterations in MCF-7 cells in a dose-dependent manner and thus inhibits cell proliferation. The cytotoxic effect of RE through the induction of apoptosis is evident by the disruption of MMP, nuclear fragmentation, and ROS accumulation. In addition, we have found that RE is potent enough to decrease the microbial activity of selective bacterial strains. Conclusion: The findings demonstrated that RE promotes significant apoptosis in breast adenocarcinoma MCF-7 cells. Therefore, RE may be a potent candidate that aids for adjuvant cancer treatment though further studies are needed to elucidate the comprehensive mechanistic pathways.
  1,443 135 -
Caesalpinia pulcherrima arrests cell cycle and triggers reactive oxygen species-induced mitochondrial-mediated apoptosis and necroptosis via modulating estrogen and estrogen receptors
Nikhil S Sakle, Deepak Lokwani, Santosh Namdeo Mokale
July-September 2019, 15(64):288-297
Background: Caesalpinia pulcherrima belonging to the family Fabaceae is used in India as a traditional medicine for a variety of ailments. Globally, traditional medicines are presently being used for the treatment of cancer. Objective: The present study was aimed at investigating the chemomodulatory potential of C. pulcherrima flowers in breast cancer and explaining its possible mechanism. Materials and Methods: The cytotoxic potential of ethyl acetate fraction of C. pulcherrima (EAFCP) flower was tested in MCF-12A (normal breast), MCF-7 (estrogen receptor [ER] positive), and MDA-MB-453 (human epidermal growth factor receptor 2 positive) human breast cancer cells by sulforhodamine B assay. Chemomodulatory potential was evaluated in vivo against N-methyl-N-nitrosourea (MNU)-induced mammary carcinoma in female Sprague Dawley® rats. The mechanism for anticancer potential was screened by in vitro studies involving Annexin V-FITC assay (apoptosis), cell cycle patterns, intracellular reactive oxygen species, and mitochondrial membrane potential measurement (FACS based) followed by docking study on estrogen receptor-alpha (ER-α). Results: The fractions showed perceptible cell growth inhibition potency (IC50<50 μg/ml) in MCF-7 breast cancer cells. In MNU-treated animals, antioxidant enzymes and histological examination showed statistically significant (P < 0.001) changes. Treatment of MCF-7 cells with EAFCP reduced cell growth rate by a mechanism associated with both apoptotic and necrotic cell death. Molecular docking study further showed that rutin and catechin have a comparable binding affinity for the ER-α. Conclusion: In this study, we confirmed that EAFCP was most effective in reducing cell viability, scavenging physiological oxidant species, and causing mitochondria-mediated apoptosis and necroptosis in MCF-7 cell by selectively modulating the functions of ER-α.
  1,462 111 -
In silico molecular docking and comparative in-vitro analysis of ethyl 3, 4, 5-trihydroxybenzoate and its derivative isolated from Hippophae rhamnoides leaves as free radical scavenger and anti-inflammatory compound
PK Pandey, Bahar Ahmed, Haider A Khan, M Bala, Jagdish Prasad
July-September 2019, 15(64):313-319
Background: Excessive production of reactive oxygen species (ROS) associated with oxidative stress induce tissue injury that might trigger the inflammatory process. Superoxide dismutase (SOD) and cyclooxygenase 2 (COX-2) play a significant role in the inflammation prompt after the overproduction of ROS. Polyphenols compound play an important role in alleviating problem associated with oxidative stress. Hippophae rhamnoides leaves extract contain major bioactive polyphenol compound Ethyl 3,4,5-trihydroxybenzoate (gallic acid ethyl ester [GAE]), Gallic acid (GA) and need to be investigate for its anti-oxidant and anti-inflammatory properties. Objective: The objective of this study is to determine the antioxidant and anti-inflammatory potential of GAE and GA derivatives isolated from H. rhamnoides leaves, in vitro and in silico approach target on COX-2 and SOD receptor. Materials and Methods: The isolated compounds GAE, GA, and derivatives 4-O methyl gallic acid (4-OMGA), pyrogallol (PG) were docked using Schrodinger's (LLC, Cambridge, USA) tools. Further in vitro antioxidant activity was determined using the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radical anion scavenging activity. The anti-inflammatory activity was evaluated using COX-2 inhibitory assay in lipopolysaccharide-stimulated RAW 264.7 cell line. Results: In silico result showed notable binding affinity of GAE with the SOD and COX-2 receptors followed by GA > PG > 4-OMGA. Experimentally, GAE confirmed promising antioxidant potential (DPPH; half-maximal inhibitory concentration 20.3 ± 2.65), SOD anion at 50 μM as well anti-inflammatory activity by inhibiting the COX-2 activity in RAW 264.7 cell line. Conclusion: The result demonstrated the potential biological activities of GAE, GA, and derivatives. In silico finding may act as precious tools to further unlock these potential therapeutic agents against oxidative stress.
  1,422 144 -
Osteogenic activity of resveratrol in human fetal osteoblast cells
Aarti Abhishek Shah, Karthik Gourishetti, Yogendra Nayak
July-September 2019, 15(64):250-255
Background: Resveratrol (RSV) is a polyphenolic phytomolecule naturally present in the skin of grapes fruit. It is reported to be phytoestrogen because of its estrogenic potentials, hence it can be explored to the treatment of osteoporosis. There was no conclusive evidence for the estrogenic potential of RSV in osteoporosis. In this study, RSV is evaluated for its effects on human osteoblast cells. Objective: The main objective of the study was to evaluate RSV on the proliferation and differentiation of immortalized human fetal osteoblastic cells 1.19 (hFOB). Materials and Methods: The osteoblastic cell proliferation and differentiation potentials of RSV were tested by cell viability assay, alkaline phosphatase (ALP) activity, total protein content, and alizarin staining for the mineralization assays. Results: The cell viability assay indicated that RSV was found to be safe at a wider concentration range and the EC50 was 72.05 μM. The therapeutic concentrations as 500 nM and 1 μM were selected for the further assays. RSV at 500-nM and 1-μM concentrations treatment on immortalized human fetal osteoblastic cells 1.19 (hFOB) did not show a significant effect on ALP activity. The total cellular proteins in hFOB increased in a dose-dependent manner on RSV treatment (P ≤ 0.05). The significant staining and the color intensity of the calcium crystals by Alizarin staining assay indicate a stimulatory effect on the mineralization phase of bone formation. Conclusion: In mature osteoblasts, ALP activity is expressed in early stage, whereas mineralized nodules are formed in the late stage of differentiation. Therefore, the present study suggests that RSV stimulates the process of bone formation through activation of late differentiation phase and may have positive effects on osteoblastic differentiation potential.
  1,426 127 -
Effect of ethanolic extract of Excoecaria agallocha leaves on the cytotoxic activity and cell cycle arrest of human breast cancer cell lines – MCF-7
Palagati Rohith Kumar Reddy, Priya Durairaj, Palaniyandi Thiruvanavukkarasu, Rajeswary Hari
July-September 2019, 15(64):346-351
Background: At present, Mangrove plants have gained importance in drug discovery due to the presence of many phytomolecules of medicinal importance. Excoecaria agallocha is widely distributed medicinal mangrove which has been traditionally used to treat sores, ulcers, and leprosy. Objective: The aim of the present study is to analyze the cytotoxic potential of Exoecaria agallocha leaves in terms of its antiproliferative activity, apoptosis induction, and cell cycle arrest in the breast cancer MCF-7 cell lines. Materials and Methods: The ant proliferative nature of the EEEA extract was determined by direct microscopic observation as well as 3-(4, 5-dimethyl-2-thiazolyl)-2, 5-diphenyl-tetrazolium bromide (MTT) assay by employing the different concentrations of the plant extract, and the IC50 values were calculated. Apoptosis-inducing potential was determined by double staining with acridine orange/ethidium bromide staining method and further confirmed by annexin V staining. Flow cytometry was performed with IC50 concentration of EEEA drug treated MCF-7 cells to determine arresting stage in the cell cycle progression. Results: There was a significant cytotoxic activity exhibited by the ethanolic extract of E. agallocha leaves (EEEA) in the direct microscopic as well as MTT assay with IC50 value of 56.5 μg/ml. Well prominent fluorescent microscopic images of morphological changes in the double staining method indicate the apoptotic potential of the extract which was further confirmed by annexin V staining. Suppression of cell cycle progression at subG1 and G1/G2 phases were also evidenced in the flow cytometry analysis. Conclusion: From the above results, it may be concluded that the ethanolic leaf extract of E. agallocha (EEEA)-induced apoptosis mediated cytotoxic and antiproliferative activity in the breast cancer MCF-7 cell lines which can be developed into a new drug for treating breast cancer.
  1,376 150 -
Pterodon emarginatus hydroalcoholic extract: Antioxidant and photoprotective activities, noncytotoxic effect, and perspective of obtaining formulations with photochemoprotective activity
Wannessa Lenyse Rocha de Carvalho, Larissa Ceres Moreira, Marize Campos Valadares, Danielle Guimaraes A. Diniz, Maria Teresa Freitas Bara
July-September 2019, 15(64):176-182
Background: Pterodon emarginatus fruits have phenolic compounds that may be related to photoprotective and antioxidant activities. Objective: This study aims to investigate the antioxidant and photoprotective activities and cytotoxicity effect of hydroalcoholic extract of P. emarginatus (HEP) and obtain formulations with photochemoprotective activity containing HEP in Lanette®, Polawax®, or Focus Gel®. Materials and Methods: Phenolic compounds, antioxidant activity, cytotoxic effect, and in vitro sun protection factor (SPF) were determined in HEP. Lanette®, Polawax®, or Focus Gel® containing HEP or synthetic sunscreen (Eusolex 2292®) or both Eusolex 2292® and HEP were prepared. The in vitro SPF of the formulations was determined to investigate the association of protection between HEP and synthetic sunscreen. Preliminary stability of formulations was evaluated. Results: Phenolic acids and flavonoids were detected by thin-layer chromatography. HEP showed antioxidant activity by 2,2-diphenyl-1-picrylhydrazyl, with EC50 of 19.3 μg/mL, and by ferric reducing antioxidant power methods, in which 1 g of the extract reduces 14,880 μM/L of ferrous sulfate. In cytotoxicity assays, an IC50 of 767.3 μg/mL was obtained, suggesting that the HEP is not cytotoxic. The SPF for HEP was 8 ± 0.31 and it was noted an additive effect to SPF for synthetic sunscreen used, in the three formulations, when associated to HEP, resulting in an improvement of about 24% (Focus Gel®), 65% (Lanette®), and 66% (Polawax®). Only on Lanette®-based formulation, no significant changes of the analyzed parameters were observed during the preliminary stability. Conclusion: It can be suggested that HEP, due to its antioxidant and photoprotective activities, leads to the photochemoprotective effect on the formulations.
  1,355 141 -
Liquid chromatography–mass spectrometry/mass spectrometry method development for the determination of carbaryl residue in honey
S Venu, K Santhi, Ashish Rawson, R Paranthaman, K Sureshkumar
July-September 2019, 15(64):205-211
Background: Honey, the natural sweetener, obtained from Apis mellifera (honey bees) possesses many medicinal properties. Intensive use of carbamate insecticide in agricultural land not only contaminates the crop but also affects the honey and honey matrices. Hence, this study focused on the analysis of insecticide in honey. Objective: Liquid chromatography–mass spectrometry/mass spectrometry (LC-MS/MS) method development for the determination of Carbaryl insecticide in honey and Comparisons of different extraction techniques to determine the efficiency of extraction process. Materials and Methods: The LC-MS/MS method was developed by optimizing the multiple reaction monitoring (MRM) parameters. Further, the comparison study was done for the optimized extraction techniques such as quick, easy, cheap, effective, rugged, and safe (QuEChERS) method and ultrasound solid phase extraction (SPE) in the developed method. The validation was studied for the developed method as well as the extraction techniques to confirm the robustness of the developed method. Results: The validation study showed good accuracy for the developed method for the concentration from 2 to 9 ppb of the working solution. Limit of detection for the developed method was 0.08 and 0.05 ppb for the fragments 145.1 m/z and 127.1 m/z, respectively. Moreover, limit of quantification for the fragment 145.1 m/z was 0.24 ppb and for 127.1 m/z was 0.16 ppb. The average accuracies for the developed method of both the fragments (145.1 m/z and 127.1 m/z) were 98.51% and 98.15%, respectively. Recovery percentage for optimized QuEChERS ranged from 107% to 112% and for the ultrasound-SPE and from 107% to 118% of the honey samples which were spiked with three different concentrations of analyte. Conclusion: From the validation, it was confirmed that the developed method was robust and simple and provides better sensitivity and intensity and low consumption of chemicals. Thus, the developed method can be used for the routine analysis of carbaryl in honey.
  1,333 124 -
Naphthazarins as cytotoxic agents isolated from Arnebia euchroma
Nidhi Sharma, Ashu Gulati, Dharmesh Kumar, Yogendra Padwad
July-September 2019, 15(64):366-370
Background: Currently, many compounds of different medicinal plants are under investigation for curing various types of cancers. In extension with this ongoing research, Arnebia euchroma is taken for the study of cytotoxic compounds present in its roots. The sensitivity of human cervical cancer (SiHa), human epidermoid carcinoma (KB), and human colorectal cancer 116 (HCT116) cell lines toward C1 and C2 isolated from A. euchroma roots was evaluated. Materials and Methods: The root extract of A. euchroma was subjected to extraction, chromatographic separation to afford two naphthazarin esters C1 and C2 as well as two white-colored compounds. The structures of purified compounds were determined by electrospray ionization mass spectrometry and nuclear magnetic resonance analysis. Results: Both C1 and C2 showed potent cytotoxicity against SiHa, KB, HCT116 cells at different concentrations. Conclusion: C1 and C2 exhibited strong cytotoxicity with IC50= 0.02 μM and 0.09 μM against SiHa cells and with IC50= 0.11 μM HCT116 cells than the vinblastine standard, respectively.
  1,305 136 -
Optimization of ultrasound-assisted extraction of L-ascorbic acid from Adansonia digitata (Linn.) and evaluation of its antityrosinase activity
Hussein Zeitoun, Sabine Lone, Dominique Salameh, Roger Lteif
July-September 2019, 15(64):183-188
Background: Adansonia digitata (Linn.) is a widely distributed tree and its edible fruit pulp is well known to have L-ascorbic acid (AA) in high amounts. AA is essential for collagen biosynthesis and has been reported to have antioxidant and skin-lightening properties. Objectives: The aim of this study was to optimize the extraction of AA from the fruit pulp of A. digitata by ultrasound-assisted extraction and to evaluate the antityrosinase activity of the extract. Materials and Methods: A rotatable central composite design was used to investigate the effect of process variables by surface response methodology. The effect of key parameters of extraction temperature (30°C–40°C), extraction time (12–28 min), and ratio solvent to material (7–13 mL/g) was investigated on AA content. Then, mushroom tyrosinase was used to evaluate the antityrosinase activity of the extract. Results: The optimal conditions were obtained with a temperature of 43.4°C, in 23.5 min with a ratio solvent to material of 15.04 mL/g. Under these conditions, AA content from A. digitata (167.4 ± 5.724 mg AA per 100 g dry weight) was determined. Antityrosinase activity of A. digitata extract containing AA was 31.36% ± 1.65%. After degradation of AA, tyrosinase activity decreases to 24.21% ± 1.43%. Conclusion: AA contained in A. digitata extract show to increases significantly the inhibition of enzymatic tyrosinase activity. This extract may have a potential impact on skin depigmentation for the treatment of hyperpigmentation disorders.
  1,313 119 -
Pila globosa snail extract inhibits osteoclast differentiation via downregulation of nuclear factor κB and nuclear factor of activated T-Cells c1 signaling pathways
Shanmuganathan Pandiarajan, Shila Samuel, Tholcopiyan Loganathan, Shyam Sundar Jaganathan, Thiagarajan Krishnamurthi, Radhakrishnan Sarangapani, Vinod Kumar Anandan, Ramasubramanian Venkatachalam
July-September 2019, 15(64):298-306
Background: Osteoporosis, a skeletal disease, that leads to increased fracture risk, features an enhanced osteoclast formation and bone resorption. Identification of agents that modulate aberrant osteoclast formation and function is important for the treatment of osteoporosis. Objective: The current study describes for the first time that Pila globosa snail extract inhibits osteoclastogenesis in vitro and thus suppresses bone loss in ovariectomy-induced rat model. Materials and Methods: Ovariectomized (Ovx) rats were treated with P. globosa snail extract and compared with sham, Ovx, and Ovx treated with zoledronate groups. Serum levels of C-terminal crosslinking telopeptides of type-1 collagen (CTX-1), TRAP5b, and antioxidant markers were determined. mRNA expressions of cathepsin K (CTSK), TRAP, calcitonin receptor (CTR), and matrix metalloproteinase 9 (MMP-9) were also assessed. Immunoblots of nuclear factor of activated T-cells c1 (NFATc1), c-Fos, TNF receptor-associated factor 6, c-Jun, and nuclear factor κB (NFκB) proteins were analyzed. Results and Discussion: P. globosa snail extract induced a decrease in the activation of NFκB, c-Fos, and NFATc1, which resulted in the downregulation of target genes, CTSK, TRAP, CTR, and MMP-9. P. globosa snail extract decreased the serum markers of bone resorption, C-terminal telopeptides of type-1 collagen (CTX-1), and tartrate-resistant acid phosphatase 5b (TRAP5b), reflecting the reduced number and activity of osteoclasts. Moreover, the results also suggested that the protective effect of P. globosa snail extract against osteoporosis is associated with the reduction of oxidative stress as evidenced by decreased malondialdehyde and increased serum antioxidant markers, superoxide dismutase, catalase, and glutathione. Conclusion: The upshot of the study suggests that the P. globosa snail extract represents a potential treatment option against osteolytic bone disease.
  1,325 96 -
Anticancer effect of different extracts of Cynanchum acutum L. seeds on cancer cell lines
Ahmed Mohamed Mohamed Youssef, Zeinab Ahmed Said El-Swaify, Yousef Mohammed Al-Saraireh, Saed Mohammed Al-Dalain
July-September 2019, 15(64):261-266
Background: Cynanchum acutum L. is a perennial medicinal herb, used for several traditional medicine purposes in Egypt and around the world. Objective: The anticancer effects of ether, chloroform subfraction, and aqueous extracts of C. acutum seeds were investigated. Materials and Methods: C. acutum seeds were extracted by ether, chloroform, and aqueous. Then, all extracts were subjected to gas chromatography/mass spectrometry (GC/MS) to determine alkaloids and other bioactive compounds. Furthermore, anticancer effects on malignant cell lines as well as normal cells were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Results: GC/MS analysis of the different extracts of C. acutum seeds revealed different compounds of alkane hydrocarbons, fatty acids, sterols, terpenoids, flavonoids, and alkaloids. The significant components of unsaturated fatty acids were linoleic acid (56.71%) in the ether extract and oleic acid (6.59%) in the chloroform extract, whereas the major saturated fatty acid was palmitic acid (3.51%) in the ether extract. Furthermore, the anticancer effects of the three extracts of the plant seeds on all tested cancer cell lines were minor. However, the higher anticancer effects were observed on lung (A549) and breast (MCF-7) cancers by water and ether extracts, respectively, as compared to positive control. Furthermore, both extracts showed low cytotoxicity toward normal cell line (WI-38) comparing to a positive control. Conclusion: Aqueous and ether extracts of C. acutum L. seeds could be considered as potential chemotherapeutic agents in lung and breast cancer treatments, respectively, with reduced systemic adverse effects.
  1,283 119 -
Efficacy of Trigonella foenum-graecum seed extract on ovariectomy-induced hyperlipidemia, oxidative stress, and histopathological changes in rats
Takkella Nagamma, Anjaneyulu Konuri, Rajalekshmi Maheshwari, EG Padmanabha Udupa, Yogendra Nayak
July-September 2019, 15(64):274-279
Objectives: This study was to standardize Trigonella foenum-graecum (fenugreek, TFG) seed extract by high-performance thin-layer chromatography (HPTLC) and to test its efficacy in ovariectomy-induced hyperlipidemia in rats. Materials and Methods: Hydroalcoholic extract of TFG-seed was standardized by HPTLC using diosgenin as standard. Female rats were selected and bilateral-ovariectomy was performed. Rats in Group-1 and Group-2 were healthy control and Ovariectomized (OVX) respectively. After 14-days of ovariectomy, Group 3 and Group 4 rats were administered TFG-extract (200 mg/kg/day) and 17β-estradiol (100 μg/kg/day), respectively, for 30 days. Serum lipid profile and liver oxidative markers were determined to compare between the groups. Results: The phytoestrogen, diosgenin, was found to be 0.83% w/w in the TFG-seed extract. The OVX rats exhibited a significant increase (P < 0.001) in serum cholesterol, triglycerides, low-density lipoprotein, and decreased high-density lipoprotein compared to control rats. The significant increase in thiobarbituric acid reactive substances and decreased glutathione was the indication of oxidative stress in the liver of OVX rats. Treatment with TFG extract significantly reverted these parameters in OVX rats which was comparable to that of standard 17β-estradiol. Conclusion: The favorable effect of TFG extract on ovariectomy-induced hyperlipidemia could be because of diosgenin along with other flavonoids and phenols in it. Thus, TFG has the benefits in menopause-induced hyperlipidemia and oxidative stress.
  1,194 126 -
Decalepis hamiltonii and its bioactive compounds protects isoproterenol-induced myocardial oxidative stress in rats
Anupama Sindhaghatta Kariyappa, Sowbhagya Ramachandregowda, Santosh Anand, Bhagyalakshmi Dundaiah, Mamatha Madhugiri Gopinath, Ravikiran Tekupalli
July-September 2019, 15(64):320-327
Background: Decalepis hamiltonii (Dh), a climbing shrub belonging to the family Apocynaceae, is consumed for its health-promoting properties. Objective: The present study was designed to evaluate the cardioprotective potential of Dh extract and its bioactive compounds on region-specific responses against isoproterenol (ISO)-induced myocardial injury in male Wistar rats. Materials and Methods: Rats were orally supplemented with ellagic acid (50 mg/kg body weight [BW]), 4-hydroxy isophthalic acid (30 mg/kg BW), and Dh extract (100 mg/kg BW) for 30 days, and they were subsequently administered (intraperitoneally) with ISO (150 mg/kg BW) for the last 2 days. Results: ISO-treated rats showed a significant increase in serum lipid profile, markers of cardiac damage, and decreased antioxidant status. Supplemented groups showed improved lipid profile, reduced serum marker enzymes, and enhanced antioxidant status in ISO-administered rats. Histopathological studies further confirmed the protective effect of Dh extract against ISO-induced myocardial infarction (MI). Conclusion: Our results demonstrated that Dh extract and its compounds efficiently ameliorated ISO-induced MI in rats.
  1,156 136 -
High-performance thin-layer chromatography marker-based standardization of Piperine, Asiaticoside, and Withanolide-A in the developed polyherbal formulation and in vitro evaluation of acetylcholinesterase inhibition
Vasudev Pai, KS Chandrashekar, Polu Picheshwara Rao, Manganahalli Manjunath Setty
July-September 2019, 15(64):256-260
Background: Preparation of highly standardized polyherbal formulation with its chief active chemical constituents supported by therapeutic efficacy in vitro is a valuable approach in the field of pharmaceutical sciences. Objective: The present work aims to develop the high-performance thin-layer chromatography (HPTLC) marker-based standardization of polyherbal formulation using Piperine, Asiaticoside, and Withanolide-A and in vitro acetylcholinesterase inhibition activity. Materials and Methods: For successful standardization, the HPTLC quantification of Piperine, Asiaticoside, and Withanolide-A was carried out. Suitable solvent systems were optimized to achieve the better resolution of the marker compounds, extracts, and sample formulation. The reproducibility of the methods was also confirmed by repeating the procedure twice. The identity of the bands in the sample formulation was confirmed by comparing the Rf value with those of their respective reference standards. In vitro acetylcholinesterase inhibition assay was done on the different crude extracts as well as tablet formulation. Results: HPTLC quantification of formulation for Piperine content showed 1.97% content w/w, whereas Piper longum extract showed 2.44% w/w. Similarly, Asiaticoside showed 0.71% in formulation and in Centella asiatica extract, it was 1.33% w/w. Contrary to the above, Withanolide-A content was 2.12% w/w in formulation and in Withania somnifera extract, it was only 0.81% w/w. In vitro acetylcholinesterase inhibition assay exhibited significant inhibition with IC50 value of 70 μg for tablet formulation. Conclusion: The presence of Piperine, Asiaticoside, and Withanolide-A in formulation was identified by rapid HPTLC quantification method. The method is very precise, reproducible, and accurate. The developed method can be used to quantify the marker compounds in the formulations available in the market. The formulation also evaluated for its acetylcholinesterase inhibition assay and showed significant activity. Hence, it could be used in the treatment of memory-related disorders such as Alzheimer's disease.
  1,107 145 -
Volatile and phenolic compounds in freshwater diatom Nitzschia palea as a potential oxidative damage protective and anti-inflammatory source
BL Sudarshan, PK Maheshwar, P Shanmukha Priya, KR Sanjay
July-September 2019, 15(64):228-236
Background: Nitzschia palea is a freshwater diatom species (Bacillariophyceae), is easy to cultivate, and is a primary producer of organic matters in aquatic environments. Materials and Methods: In this study, proximate composition in axenic culture of N. palea was determined, phenolic content and volatile compounds were determined for methanol and ethyl acetate extracts. Both the extracts were evaluated for eight different in vitro antioxidant and free radical scavenging activities. Macromolecular damage prevention properties were determined by electrophoretic methods, and antihemolytic activity was validated by lactate dehydrogenase assay, atomic force microscope, and scanning electron microscope image analysis. Results: Both the extracts showed antioxidant, macromolecular damage prevention, and antihemolytic properties. Among the two extracts, ethyl acetate extract showed high activity compared to methanol extract. Based on this result, ethyl acetate extract was evaluated for in vitro anti-inflammatory properties using RAW 264.7 cells. The extract showed IC50 value of 50.73 μg/mL and inhibition of inflammatory cytokines such as nitric oxide, tumor necrosis factor-alpha, and prostaglandin E2. The observed activity was correlated with identified important metabolites such as butyl isobutyl phthalate, pristane, and squalene of methanol extracts. Similar co-relation was observed for 7,9-di-tert-butyl-1-oxaspiro (4,5) deca-6,9-diene-2,8-dione, methyl palmitate, hentriacontane, and dibutyl phthalate were of ethyl acetate extract. Conclusion: The study concludes that N. palea has potentiality to isolate pharmacologically active metabolites using advanced chromatographic techniques, which can be useful in combating oxidative stress-related inflammatory diseases.
  1,123 128 -
Catha edulis-induced skeletal muscle toxicity in experimental rats via regulation of rhabdomyolysis biomarkers
Syam Mohan, Emad Shaheen, Yasmin O El-Amir, Hussein A Khadashi, Saida S Ncibi, Abdullah Farasani, Siddig Ibrahim Abdelwahab
July-September 2019, 15(64):359-365
Background: Recently, there are clinical reports on the potential of Catha edulis (khat) to induce muscular toxicity. C. edulis (khat) is an evergreen shrub and a well-known controversial plant due to the content of natural stimulant, cathine and cathinone. Objective: The main objective of the study is to evaluate the possible effect of C. edulis leaves extract to induce rhabdomyolysis in vivo. Materials and Methods: Sprague Dawley rats were grouped and treated with khat extract at two different doses (250 and 500 mg/kg), while atorvastatin was used as positive control for 28 days. Body weight was measured throughout the study period. Overnight urine was collected from each rat at the 28th day for myoglobin (Myo) analysis. Terminal blood samples were collected from sacrificed animals for the measurement of serum biomarkers and clinical chemistry. The standard clinical pathology assays aspartate aminotransferase (AST), alanine aminotransferase (ALT), and serum creatinine (CR) were monitored. Skeletal muscle, cardiac muscle, and kidney were collected for histopathological examination. Results: Animals received 250 mg/kg khat extract had shown mild-to-no gait disorders, while at higher dose extract (500 mg/kg) had reduced the body weight of rats with marked increase of gait disorders compared to control. CR, AST, and ALT were elevated in high-dose administration and in rats received ethanol. The tested biomarkers such as heart-type fatty acid-binding protein (HFABP) 3, Troponin I Type 1 slow skeletal (TNNI1), and Myo were significantly increased in khat high dose and statin treatment, but not in low-dose extract and alcohol. The increase in HFABP and TNN1 results were well reflected in histopathological findings of skeletal myofiber degeneration and in the hemorrhages and pyknosis of nucleus observed in the cardiac muscle. Conclusion: These results provide evidence that khat chewing contributes to the development of muscle toxicity and probable rhabdomyolysis. The current subject thus warrants detailed studies which could emphasize on the cardiac complications and muscular toxicity mechanisms.
  1,135 115 -
Tetrahydronaphthalene lignan glucoside from Crataeva nurvala: Apoptotic induction, antimigration, and in silico analysis
Nandan Sarkar, Puneet Kacker, Hina Amin, Priyanka Narad, Anindya Goswami, Sabari Ghosal
July-September 2019, 15(64):307-312
Background: Crataeva nurvala is an important plant having wide application in Ayurveda and Siddha. It is extensively used in formulations for patients suffering from benign prostatic hyperplasia. Objective: Isolation, characterization, and evaluation of cytotoxic activity of bioactive fraction of C. nurvala and identification of molecular target prediction by suitable method. Materials and Methods: Gravity column chromatography followed by HPLC of the bioactive n-butanol fraction afforded compound 1. Besides cell proliferation, apoptotic index and cell migration were studied to determine the efficacy of the compound against cancer cells. Results: The cell cycle analysis revealed that the compound 1 showing apoptosis inducing property through G2/M arrest and mitotic inhibition. Besides, clonogenic assay and wound healing assay demonstrated that the compound could decrease the ability of colony formation and cell migration in a significant way. However, limited availability of the compound impelled us to undertake in silico studies to predictprobable protein targets. This resulted in the identification of IGF1R with highest docking score of −10.0 in preference to four other protein targets (EGFR, AKT1, AKT2, and BCL2) of receptor tyrosine kinase domain (RTKs). As insulin receptor R (Insulin receptor) of tyrosine kinase domain maintains high resemblance with IGF1R, molecular docking was also conducted on the same target. The insignificant docking score suggested specificity of the compound toward IGF1R. Conclusion: The study concluded that; (+)-lyoniresino1-2a-0-β-D-glucopyranoside is a promising apoptosis inducing agent. Molecular modeling of the compound against five crucial protein targets of RTKs suggested that IGF1R could be the probable protein target for the compound.
  1,038 116 -