Posted by admin on Mar 1, 2016 in |
3D-QSAR models of Comparative of Molecular Field Analysis (CoMFA) and Comparative of Molecular Similarity Indices Analysis (CoMSIA) of 44 potent p56lck inhibitors were performed. The conventional ligand-based 3D-QSAR studies were performed for a series of Benzothiazole derivatives as p56lck inhibitors. The model gave q2 values of 0.710 and 0.642, r2 values of 0.966 and 0.956 for CoMFA and CoMSIA, respectively. The predictive ability of the models was validated using the external test set of 10 compounds that were not included in the training set of 34 molecules. These results provided better understanding of the relationship between the structural features of p56lck inhibitors and its activities, which should be applicable to design and find new potential p56lck...
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Posted by admin on Mar 1, 2016 in |
Ethanolic extract of the roots of Chonemorpha fragrans, a traditionally used antidibetic plant was evaluated for its antihyperglycemic and antihyperlipidemic effect using streptozotocin-nicotinamide induced diabetic rat model. Oral glucose tolerance test with 2g/kg of glucose and normoglycemic studies were performed which showed a dose dependant decrease in sugar levels. The acute oral toxicity studies demonstrated the safety of the dose up to 2000mg/kg body weight. The diabetic rats were treated with ethanolic root extracts, at a dose of 200mg/kg and 400mg/kg based on the acute toxicity study. Standard groups were treated with Glibenclamide at a dose of 0.6mg/kg. Treatment was continued for 21 days and the weights of the rats and serum glucose levels were measured on 1st,7th,14th and 21stday. Other biochemical parameters like lipid profile, HbA1c, ALT, AST, serum creatinine, urea and total proteins were evaluated on the last day of the study. The results of the study have shown a significant difference between the initial and final fasting blood glucose levels of C. fragrans and glibenclamide treated...
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Posted by admin on Mar 1, 2016 in |
3D-QSAR models of Comparative of Molecular Field Analysis (CoMFA) and Comparative of Molecular Similarity Indices Analysis (CoMSIA) of 44 potent p56lck inhibitors were performed. The conventional ligand-based 3D-QSAR studies were performed for a series of Benzothiazole derivatives as p56lck inhibitors. The model gave q2 values of 0.710 and 0.642, r2 values of 0.966 and 0.956 for CoMFA and CoMSIA, respectively. The predictive ability of the models was validated using the external test set of 10 compounds that were not included in the training set of 34 molecules. These results provided better understanding of the relationship between the structural features of p56lck inhibitors and its activities, which should be applicable to design and find new potential p56lck...
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Posted by admin on Mar 1, 2016 in |
The poor bioavailability of ophthalmic solutions caused by dilution and drainage from the eye can be overcome by using in situ forming ophthalmic drug delivery system prepared from polymer that exhibit reversible liquid–gel phase transition. The objective of the study was to develop optimized formulation of in situ ophthalmic gel of Epinastine hydrochloride, an antihistaminic drug, using a pH triggered polymer, Carbopol as a gelling polymer and HPMC E-50LV (hydroxyl propyl methyl cellulose) as release retardant. The 32 full factorial design was employed to optimize the formulation considering Carbopol and HPMC as independent variables. The formulations were assessed for appearance, gelling ability, sterility, pH, drug content, viscosity, release through cellophane membrane & corneal membrane of goat, ocular irritation study & stability study as per ICH guidelines. Formulations F3 and F7 were found to be the good formulations from the nine formulations developed by 32 factorial design. The study revealed that the in situ system of epinastine hydrochloride sustained the effect of drug to 12 hours. The formulations F3 and...
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Posted by admin on Mar 1, 2016 in |
Emergence of Mycobacteria that are resistant to common antibiotics necessitate development of novel antibacterial drugs. The complexity of mycobacterial cell envelope plays an important role in its defense against antimicrobial activity of human immune system. The cell wall of Mycobacteria constitutes a set of carbohydrate-containing molecules. Glycosyltransferases, the glycan processing enzymes play a significant role in assembling these moieties. Targeting these enzymes could therefore interfere with the virulence of the pathogen thus leading to non-proliferation or its death. The significant role of these enzymes makes them novel targets for drug action. Natural products are important sources of pharmacologically relevant compounds. The present study has been undertaken to evaluate the inhibition potential of selected phytochemicals against glycosyltransferases of Mycobacterium. Fourteen antimicrobial phytochemicals were selected from the NCBI Pubchem Database. These phytochemicals were further screened using Lipinski’s rule of five. Molecular docking was performed to identify new potential inhibitors against Mycobacterial glycosyltransferases using Discovery studio 4.0 with these compounds. These sets of phytochemicals were further screened for toxicity using ADMET descriptors....
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