Posted by admin on Feb 28, 2019 in |
Background: Diabetic nephropathy (DN) is a primary cause of end-stage renal disease globally. Activation of mTOR and reduced autophagy has been identified as one of the pathogenic pathways. The presently available drugs have been successful in inhibiting the mTOR signaling, but show low oral bioavailability and suboptimal solubility. Rapamycin is a selective inhibitor of mTOR, shown significant protection against DN. However, its continuous use is associated with side effects. Thus, the search for novel drugs is on great demand. In the present study, in-silico approaches have been adopted to identify potential compounds with optimal oral bioavailability and better solubility properties, with no toxic effect. Materials and method: The receptor protein mTOR with PDB ID: 3FAP was retrieved from the RCSB protein data bank. Total 20 compounds were selected from the list of 113, obtained from LC-MS of Lalchandan. Further, in-silico molecular docking calculation was done by using YASARA software. Drug-likeness and molecular property of best-docked compounds were checked by using Lipinski rule of five and Admet SAR server. Result:...
Read More
Posted by admin on Feb 28, 2019 in |
Abelmoschus esculentus Linn. (Malvaceae) is described in medicine for the treatment of diabetes mellitus. The monech seeds of Abelmoschus esculentus having potential in the development of a drug for diabetes due to their antidiabetic activity. The hypoglycemic effect of the extract was tested in normal, glucose loading and alloxan-induced diabetic rats. Aqueous and ethanolic extracts (250 and 500 mg/kg body weight), were administered orally to male Wistar albino rats. The parameters studied included oral glucose tolerance test in blood, fasting blood glucose, serum insulin, and glycated hemoglobin levels, liver glycogen content, serum lipid profile, and changes in body weights. The extracts produced a dose-dependent fall in fasting blood glucose (FBG). After 15 days of treatment with extracts, the maximum reduction in FBG (35.14%) was observed in diabetic rats treated with ethanolic extract 500 mg/kg dose. Serum lipid levels were reversed towards near normal, and control in the loss of body weight was observed in treated rats as compared to diabetic control. The extract treatment also showed a significant increase...
Read More
Posted by admin on Feb 28, 2019 in |
The liquisolid technique was chosen to enhance the dissolution properties of Candesartan. The study aimed to investigate the complexation of Candesartan with β-cyclodextrin in improving the dissolution profile of Candesartan. Candesartan is a BCS class-II drug. The inclusion complexes were formed by physical mixing (1:1 ratio). Liquisolid compacts were prepared by using, propylene glycol, tween 20 as the nonvolatile liquid vehicles. Avicel pH 102 was used as the carrier and aerosil 200 as a coating material and sodium starch glycolate as the disintegrant respectively. The pre-formulation studies like melting point, flow properties of Candesartan were compiled with IP standards. The FT-IR spectra revealed that there was no interaction between drug and excipient. Liquisolid compact (LS8) was showing the best release. Stability studies showed that there were no significant changes in physical and chemical properties of a tablet of formulation LS8 after 3 months. This research work has produced encouraging results in terms of increasing the in-vitro dissolution of poorly soluble drugs such as Candesartan using liquisolid technology. The technique...
Read More
Posted by admin on Feb 28, 2019 in |
S. marcescens and P. mirabilis are gram-negative bacteria responsible for nosocomial infections. Quorum sensing regulates virulence in S. marcescens and P. mirabilis. Present study documents the potential of E. trigona extracts in inhibiting quorum sensing in both the bacterial species. Extracts of aerial part of the plant were prepared in petroleum ether, chloroform, ethyl acetate, acetone and methanol using soxhlet extraction technique. Petroleum ether extract, chloroform extract, and acetone extract were found to quench quorum in S. marcescens. These extracts were next subjected to column chromatography and assayed for its quorum quenching capacity. Later, thin layer chromatography was used to separate and identify the bioactive fraction responsible for quorum quenching. The fraction exhibiting quorum quenching capacity was subjected to GC-MS analysis. It revealed the presence of fatty acid derivatives in the bioactive fraction. A major part of the bioactive fraction was 9,12-Octadecadienoyl chloride (Z, Z), a derivative of linoleic acid, and, hence linoleic acid was also used for testing its effect on swarm motility of bacteria. Furthermore, the bioactive...
Read More
Posted by admin on Feb 28, 2019 in |
Hyperin, a flavonoid is an active phytochemical constituent gift in numerous plants as well as, Hypericum perforatum, Drosera rotundifolia, Stachys byzantina, Prunella vulgaris, Rumex acetosella, Abelmoschus manihot and Rhododendron arboreum. It’s protecting result on cultured PC12 cells against toxicity induced by hydrogen peroxide and tert-butyl hydroperoxide. Hyperin, isoquercitrin and quercetin isolated from ethyl acetate fraction of the root of A. chiisanensis showed lipopolysaccharide-induced nitrite production in rat peritoneal macrophages. As a crucial bioactive compound, hyperoside (hyperin) has been documented to possess antihyperglycemic, antiviral activity, antinociceptive, medicament, cardioprotective, hepatoprotective, and gastric-mucosal protecting result. The current study evaluates the ulcer healing potential of hyperin against absolute ethanol- (necrotizing agent), aspirin- (non-steroidal medicament drug) and histamine- (gastric secretion stimulator via H2 receptor) iatrogenic ulcers in rats. Hyperin (25 mg/kg and 50 mg/kg) was administered orally to the long fasted rats, one hour before the absolute ethanol/ aspirin/ histamine challenge. The ulcer index, gastroprotective potential, the status of the inhibitor enzymes enzyme (CAT), glutathione peroxidase (GPx) and glutathione reductase (GR) along with reduced...
Read More
