Posted by admin on Mar 31, 2016 in |
A series of novel cholesteryl lactate-fatty acid conjugates (4a-i) were prepared by esterification of cholesterol with lactic acid, followed by coupling hydroxyl group of cholesteryl lactate with –COOH group of fatty acids including, saturated fatty acids of varying carbon chain of C10-C18, unsaturated fatty acids like 10-undecenoic, oleic ((9Z)-octadec-9-enoic), ricinoleic ((9Z,12R)-12-hydroxyoctadec-9-enoic) and 11-bromoundecanoic acid. Cholesteryl lactate-fatty acid conjugates were characterized by spectroscopic techniques like FT-IR, 1H-NMR, 13C-NMR, ESI-MS and HRMS. All the synthesized compounds were tested for their antimicrobial activity against a panel of seven bacterial strains like Staphylococcus aureus MTCC 96, Bacillus subtilis MTCC 121, Micrococcus luteus MTCC 2470, Klebsiella planticola MTCC 530, Escherichia coli MTCC 739, Pseudomonas aeruginosa MTCC 2453 and fungal strain like Candida albicans. Among them, the compounds with unsaturation (4f and 4h), and functional groups like bromine and hydroxyl group (4g and 4i) showed good antibacterial activity. But, promising activity was observed against Staphylococcus aureus MTCC 96 strain ranging from 7.8-15.6 µg/ml. These compounds (4f-i) are also exhibited good to moderate antifungal activity against...
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Posted by admin on Mar 31, 2016 in |
Crataeva tapia L. (Family- Capparaceae) is an important medicinal tree, commonly called as ‘Varuna’. The plant has been reported to possess several medicinal properties. Propagation of Crataeva tapia L. is mostly by seeds, but germination percentage is very low mainly due to presence of hard seed coat. Conservation and propagation of species using biotechnological tools like plant tissue culture are relevant when natural propagation is hampered. Plant cell culture systems have potential for commercial exploitation of secondary metabolites. These secondary metabolites can then be analyzed using chromatographic techniques. In the present study, a simple, precise, rapid and selective High Performance Thin Layer Chromatography (HPTLC) method was developed and validated for detection and quantification of phytochemical marker β-sitosterol in leaf, bark, leaf callus and stem callus of Crataeva tapia L. as per ICH guidelines....
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Posted by admin on Mar 31, 2016 in |
Metformin HCl (MH), is an oral anti-diabetic drug with less bioavailability, and a BCS class III, short plasma half-life as well as narrow absorption window. The objective of this research work is to obtain better delivery of MH to the upper part of GIT by increasing the mean residence time (MRT) in the stomach. For this, Gastroretentive swellable and floating sustained release tablets were prepared to prolong the gastric emptying that provides maximum drug at the site of absorption. Different formulations were prepared by wet granulation with the help of hydrophilic polymers like different grades of hyroxypropyl methyl cellulose (HPMC), xanthan gum (XG), sodium alginate (SA), carbopol 940; hydrophobic polymer like ethyl cellulose (EC); swelling agent like crospovidone (CP) and gas generating agent sodium bicarbonate (SBC). The formulations were evaluated for pre and post-compression characteristics; the formulation F5 gave the optimum result along with >24 hrs floating time and an in vitro release profile very near to desire release. Release kinetic studies showed that all batches followed Super case...
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Posted by admin on Mar 31, 2016 in |
Objective: Following World Health Organization tropical disease research mandate, there is definitive need for search of new lead molecules for development of drug against human lymphatic filariasis. Thiazolidineone derivatives has shown versatile therapeutic potential. The present study has been undertaken to explore the possible antifilarial effect of such synthetic compounds against filarial parasite, Brugia malayi. Methods: A series of 12 thiazolidineone derivatives, following synthesis and characterization, were screened for antifilarial potential in vitro against microfilarial stage of Brugia malayi; those showed significant effect were tested against adult parasites also. The pharmacological response in terms of loss of parasitic motility was assessed under microscope. Further dose dependent response and potential lethality onto host cells for such effective drugs were carried out. Result: Out of the tested compounds, four such compounds showed significant activity and those were tested against the adult worms; one of these compounds showed marked effect. The corresponding IC50 and LD50 values were deduced for each of these four effective compounds. Most of them showed a good therapeutic...
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Posted by admin on Mar 31, 2016 in |
Four crude extracts viz, methanol extract of fruit and n-hexane, dichloromethane, methanol extracts of the leaf of R. tetraphylla were investigated for in vitro antioxidant activity at different concentrations (5, 50 and 100 μg). Antioxidant ability is expressed as equivalents of ascorbic acid and was calculated using standard graph. The results indicated that the leaf n-hexane and methanol extracts was found to be significantly active at 5μg when compared with BHA, and at 50 μg concentration the methanol leaf extract found be very high. The fruit methanol extract was found to be active and the activity increased with increase in dose, but not as that of BHA. The experimental results show that the activity exhibited by the solvent extracts is dose...
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