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Therapeutic Methods and Therapies TCIM
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1.
Br J Nutr ; 125(4): 377-388, 2021 02 28.
Article in English | MEDLINE | ID: mdl-32713360

ABSTRACT

In the present investigation, the supercritical carbon dioxide (SC-CO2) extracts of small cardamom (SC) and yellow mustard (YM) seeds have been investigated for their efficacies in combating type 2 diabetes in streptozotocin-induced Wistar albino rats. Fasting blood glucose (FBG) levels in the rats were monitored on days 8, 15 and 21. On day 15, FBG level reduced appreciably by 31·49 % in rats treated with SC seed extract and by 32·28 % in rats treated with YM seed extract, comparable to metformin (30·70 %) and BGR-34 (a commercial polyherbal drug) (31·81 %) administered rats. Either extract exhibited desirable effects on hepatic glucose-6-phosphatase, glucose-6-phosphate dehydrogenase (G6PD) and catalase activities in controlling diabetes. A molecular docking exercise was conducted to identify specific compounds in the extracts which possessed augmenting effect on G6PD. The results revealed that all the bioactive compounds in the extracts have binding affinities with the enzyme and contributed to the antidiabetic efficacies of the extracts as G6PD augmenters. The effects of the extracts on insulin sensitivity and glucose uptake were investigated using non-invasive modelling by iHOMA2 software. This in vitro approach indicated that extract administration resulted in increased both insulin sensitivity of the liver and glucose uptake in the gut. The findings of the present study attest these SC-CO2 extracts of the spices as safe alternatives of metformin and BGR-34 in combating type 2 diabetes and could be safely subjected to clinical studies. These extracts could also be employed in designing proactive food supplements in mitigating the metabolic disorder.


Subject(s)
Carbon Dioxide/chemistry , Chemical Fractionation/methods , Elettaria/chemistry , Hypoglycemic Agents/therapeutic use , Mustard Plant/chemistry , Seeds/chemistry , Animals , Diabetes Mellitus, Experimental/drug therapy , Gene Expression Regulation/drug effects , Glucose-6-Phosphatase/genetics , Glucose-6-Phosphatase/metabolism , Glucosephosphate Dehydrogenase/genetics , Glucosephosphate Dehydrogenase/metabolism , Hypoglycemic Agents/chemistry , Metformin/therapeutic use , Models, Biological , Molecular Docking Simulation , Plant Extracts/chemistry , Plant Extracts/pharmacology , Rats , Rats, Wistar , Software
2.
J Nutr Sci ; 8: e32, 2019.
Article in English | MEDLINE | ID: mdl-31595188

ABSTRACT

Melatonin-rich and 1,8-cineole-rich extracts have been successfully obtained from yellow mustard (YM) and small cardamom (SC) seeds, respectively, employing green technology of supercritical CO2 (SC-CO2) extraction. Chemical profiling confirmed the presence of melatonin and 1,8-cineole and co-extractants in the respective extracts. Electron paramagnetic resonance spectroscopy attested strong antioxidant activities of the extracts foregoing pan-assay interference compounds involved in spectroscopic analysis. These extracts also exhibited synergistic efficacies greater than unity confirming antioxidant synergy among the co-extracted bioactives therein. To ascertain hypocholesterolaemic efficacies, these extracts were co-administered orally with Triton X (at the pre-optimised dose of 175 mg/kg body weight (BW)) to Wistar albino rats at doses of 550, 175 and 55 mg/kg BW. Serum total cholesterol levels in the rats were monitored on days 3, 7, 15 and 21. On day 21, total cholesterol level reduced appreciably by 49·44 % in rats treated with YM seed extract and by 48·95 % in rats treated with SC seed extract, comparable with atorvastatin-administered rats (51·09 %). Either extract demonstrated inhibitory effects on hepatic 3-hydroxy-3-methyl-glutaryl-CoA (HMG-CoA) reductase activity. A molecular docking exercise identified specific compounds in the extracts which possessed binding affinities comparable with therapeutically used HMG-CoA reductase inhibitors. In silico and in vivo studies concertedly concluded that the consortium of bioactive components in the extracts cannot be considered as invalid metabolic panaceas and therefore these 'green' extracts could be safely subjected to clinical studies as preventive biotherapeutics for hypercholesterolaemia. These extracts could be consumed per se as hypocholesterolaemic supplements or could be ingredients of new spice-based therapeutic foods.


Subject(s)
Carbon Dioxide/chemistry , Cholesterol/blood , Dietary Supplements , Elettaria/chemistry , Mustard Plant/chemistry , Seeds/chemistry , Spices/analysis , Animals , Anticholesteremic Agents/analysis , Anticholesteremic Agents/pharmacology , Antioxidants/analysis , Antioxidants/pharmacology , Chromatography, Supercritical Fluid , Dose-Response Relationship, Drug , Drug Synergism , Hydroxymethylglutaryl-CoA Reductase Inhibitors/analysis , Hydroxymethylglutaryl-CoA Reductase Inhibitors/pharmacology , Hypercholesterolemia/drug therapy , Male , Molecular Docking Simulation , Octoxynol/analysis , Octoxynol/pharmacology , Plant Extracts/analysis , Plant Extracts/pharmacology , Rats , Rats, Wistar , Toxicity Tests, Acute
3.
J Mol Recognit ; 29(5): 223-31, 2016 May.
Article in English | MEDLINE | ID: mdl-26748819

ABSTRACT

Phytocystatins belong to the family of cysteine proteinases inhibitors. They are ubiquitously found in plants and carry out various significant physiological functions. These plant derived inhibitors are gaining wide consideration as potential candidate in engineering transgenic crops and in drug designing. Hence it is crucial to identify these inhibitors from various plant sources. In the present study a phytocystatin has been isolated and purified by a simple two-step procedure using ammonium sulfate saturation and gel filtration chromatography on Sephacryl S-100HR from Brassica alba seeds (yellow mustard seeds).The protein was purified to homogeneity with 60.3% yield and 180-fold of purification. The molecular mass of the mustard seed cystatin was estimated to be nearly 26,000 Da by sodium dodecyl sulfate polyacrylamide gel electrophoresis as well as by gel filtration chromatography. The stokes radius and diffusion coefficient of the mustard cystatin were found to be 23A° and 9.4 × 10(-7) cm(2) s(-1) respectively. The isolated phytocystatin was found to be stable in the pH range of 6-8 and is thermostable up to 60 °C. Kinetic analysis revealed that the phytocystatin exhibited non-competitive type of inhibition and inhibited papain more efficiently (K(i) = 3 × 10(-7) M) than ficin (K(i) = 6.6 × 10(-7) M) and bromelain (K(i) = 7.7 × 10(-7) M respectively). CD spectral analysis shows that it possesses 17.11% alpha helical content.


Subject(s)
Cystatins/isolation & purification , Cystatins/pharmacology , Cysteine Proteinase Inhibitors/isolation & purification , Cysteine Proteinase Inhibitors/pharmacology , Sinapis/metabolism , Bromelains/antagonists & inhibitors , Chromatography, Gel , Circular Dichroism , Cystatins/chemistry , Cysteine Proteinase Inhibitors/chemistry , Ficain/antagonists & inhibitors , Molecular Weight , Papain/antagonists & inhibitors , Plant Proteins/chemistry , Plant Proteins/isolation & purification , Plant Proteins/pharmacology , Protein Structure, Secondary , Seeds/metabolism
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