Posted by admin on Mar 30, 2015 in |
: Thiosemicarbazobes are the compounds that possess wide range of biological activities. Presently the areas in which thiosemicarbazones receiving more attention is its use against cancer. Reports from the SAR studies confirms that the thiosemicarbazones with heterocyclic moiety shows carcinogenic potency. These are potent ribonucleotide reductase inhibitor. Adamantyl derivatives is also having interesting biological properties and most promising towards anticancer activity. The value of adamantyl group in drug design is multidimensional. A novel series of compounds of thiosemicarbazones were prepared by conjugating adamantyl group and using aromatic substitution. The various substitutions on thiosemicarbazones were reported as anti cancer activity and adamantyl group also show antiproliferative activity against some cell lines, so in present work 20 compounds were prepared on the basis of best results of QSAR studies and they were screened for anticancer activity using cell line studies. The results were compared with standard drug doxorubicin, 3 compounds show more inhibitory action than standard...
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Posted by admin on Mar 30, 2015 in |
A series of novel unsaturated fatty acid based b-hydroxy 1,2,3-triazole hybrids were designed and synthesised in excellent yields by esterification, epoxidation of oleic, ricinoleic and 10-undecenoic acids followed by azidolysis and “click” reaction with different alkynes. All the b-hydroxy 1,2,3-triazole hybrids were characterised by ESI-MS, IR and NMR spectra as well as HRMS analysis and were screened in vitro for their anticancer activity against selected four human cancer cell lines (DU-145, HeLa, MCF-7 and A549) in comparison with doxorubicin, a standard anticancer drug. Among all the triazoles, methyl oleate with-CH2OH as 1,2,3-triazole side chain (1dii) exhibited good anti cancer activity against DU-145, HeLa, MCF-7 and A549 human cancer cell lines with IC50 values 10.73, 13.61, 11.93, and 16.54 μM...
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Posted by admin on Mar 30, 2015 in |
This study investigated the antidiabetic activity of the aqueous extract of the leaves of Ageratum conyzoides. Streptozotocin induced hyperglycemia male adult albino rats were used to study the antidiabetic effect of Ageratum conyzoides aqueous extract (at doses of 100, 200 and 300 mg/kg respectively). The diabetic rats were housed in metabolic cages, for the whole period of the experiment. Body weight was evaluated at the beginning of the experiment and on days 7, 14, and 21 afterward. Water intake, food intake and urine excretion volume were also estimated. At the end of the experiment the rats were sacrificed and serum insulin concentration, total serum proteins and hepatic glycogen content were estimated. Lipid profile (total cholesterol (TC), High density lipoprotein (HDL)-cholesterol, low density lipoprotein (LDL)-cholesterol and triglycerides (TG)) were also assessed. The results showed significant effect of stimulating body weight growth at the doses of 200, 300 mg/kg. The effect of the extract on the food, water intake and water excretion showed a significant decrease in the 200 and 300...
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Posted by admin on Mar 30, 2015 in |
Ailanthus excelsa leaves were evaluated for antimicrobial activity against clinical isolates obtained from patients with eye and skin infections and also for its antioxidant potential. The bacterial isolates obtained were identified to be S. aureus, P. aeruginosa, E. coli and the fungal isolates were identified as Aspergillus niger and Penicillium. The extract showed a maximum zone of inhibition against A. niger followed by P. aeruginosa. But it did not exhibit any inhibitory activity against S. aureus. There was a remarkable inhibitory activity recorded against E. coli and Penicillium. The extracts were found to possess 0.7954 µg/g of total Tannins and 1.41µg/g of total Phenols. The extract also exhibited 12.5% radical scavenging activity in FRAP assay and 8.5% activity in CUPRAC...
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Posted by admin on Mar 30, 2015 in |
Poor water solubility is characterized by low dissolution rate and consequently reduced bioavailability. Formulation of solid dispersion has attracted considerable interest where dispersing a poorly water soluble drug in a water soluble polymer matrix improves the dissolution characteristics and bioavailability of the drug. The aim of the present study was to enhance the dissolution rate and bioavailability of poor water soluble drug Ibuprofen (BCS class II) using solid dispersion techniques. Ibuprofen solid dispersion was prepared by melt dispersion and solvent evaporation method. Drug-carrier physical mixtures were also prepared to compare the dissolution characteristics. Effects of different polymer i.e. Polyvinylpyrrolidone (PVP) k12, Poloxamer 407, PEG 4000 and PEG 6000 were studied for solid dispersion and physical mixture. Solid dispersions were investigated for Drug content, dissolution characteristics, Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) analysis. All the solid dispersions showed better dissolution rate than physical mixtures. Solid dispersion of Ibuprofen containing PEG 6000 in combination with Poloxamer 407 at the ratio of 1:1:1 prepared...
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