Posted by admin on Jul 1, 2014 in |
Non-nucleoside reverse transcriptase inhibitors (NNRTI) are a group of small hydrophobic compounds with diverse structure that specifically inhibit HIV-1 reverse transcriptase (RT) by allosteric bind to change its conformation. NNRTIs interact with HIV-1 RT by binding to a single site on the p66 subunit of the p66/p51 heterodimeric enzyme, termed the NNRTI-binding pocket (NNRTI-BP), binding interaction results in both short-range and long-range distortions of RT structure. In this article, we chose T-70(Rilipivirine) as a base structure for virtually identification of more/similar efficient drug like leads then T-70 using five different PDB structures (4KFB, 4IG3, 4IF3, 4GIQ, 3BGR) of RT fromPDB database ‘RCSB’ versus chemical compounds database ‘ZINC’ using Schrodinger and Discovery Studio software. Using molecular constraint search with similarity coefficient ‘Tanimoto’, 67500 ligands were extracted and docking analysis resulted in few better efficient in docking properties and in other computational medicinal parameters have reported, and they may further undergo through high end extensive virtual investigation and...
Read More
Posted by admin on Jul 1, 2014 in |
Cordia dichotoma L. family Boraginaceae is a medium sized tree, is taken as food. The immature fruits are pickled and are also used as vegetable. The various extracts and fractions of Cordia dichotoma were screened for their free radical scavenging properties using 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical and comparing it with butylated hydroxyl toluene (BHT) as standard antioxidant. The methanolic extract of seeds of Cordia dichotoma Linn and its fraction containing Taxifolin showed promising (P<0.001) DPPH free radical scavenging activity at a concentration of 100...
Read More
Posted by admin on Jul 1, 2014 in |
The role of liquid membrane hypothesis has been studied in the mechanism of action of Ertapenem. In the present study transport of selected permeants (glucose, p-amino benzoic acid and ions like magnesium, ammonium, phosphate, calcium, sodium, potassium and chloride) through liquid membrane generated by Ertapenem in series with supporting membrane has been studied. The results indicate that the liquid membrane generated by Ertapenem inhibit the transport of various essential bio-molecules and permeants into the cell. The data indicate that modification in permeability of different permeants in the presence of the liquid membrane is likely to play significant role in the biological actions of Ertapenem. It seems that the formation of liquid membrane by Ertapenem may also contribute for the bactericidal activity of the drug, in addition to its conventionally established mechanism i.e. inhibition of cell wall...
Read More
Posted by admin on Jul 1, 2014 in |
Among numerous species of plants growing in the wild in India, Garike, orDruva or taxonomically the Cynodon dactylon sp. occupies its unique place in the traditions, religions and cultures of different societies. In the present study, Phytochemical screening of methanolic, petroleum ether, ethanolic and aqueous extracts of Cynodon dactylon revealed the presence of 17 different phytoconstituents. Quantitative analysis ofmethanolic extract revealed the concentration of various bioactive constituents.Antimicrobial activity of both Ethanolic and Methanolic extracts of Cynodon dactylon showed good inhibitory effect for all the tested Bacterial and Fungal strains including E. coli, B. subtilis, S. typhimurium, M. luteus, K. pneumoniae, S. aureus, P. vulgaris, P. aeruginosa, C. albicans, A. flavus, A. fumigatus, P. notatum, Sporothrix schenckii, Stachybotrys chartarum and C. neoformans by Agar well method. TLC for all the extracts showed bands in U.V for the presence of Flavonoids, Alkaloids, Phenols and Glycosoids. HPLC analysis of methanolic extract gave peaks at retention time 2.779, 4.115 and 9.840.LC-MS of methanolic extract of Cynodon dactylon showed the presence of eight compounds....
Read More
Posted by admin on Jul 1, 2014 in |
Background: Familial Hypercholesterolemia (FH) is an autosomal dominant disorder caused by mutation in the LDL receptor gene and characterized by raised LDL-C, tendon xanthomata and premature atherosclerosis. Existing therapies for FH such as statins and LDL apheresis do not offer adequate lipid control in most patients, which has led to the search for more definite alternatives. Two new drugs have been approved by the US FDA in the recent past for FH, namely mipomersen, an anti-sense oligo-nucleotide and lomitapide, a microsomal triglyceride transfer protein. Methods: We did a literature search across PubMed to retrieve articles related to efficacy and safety of mipomersen and lomitapide. Results:Mipomersen has been found to have reasonable efficacy in clinical trials over and above that seen with concomitant statin therapy in FH. Lomitapide has also shown evidence of adequate LDL-C reduction in clinical trials though the number of studies performed with lomitapide is relatively fewer. The subcutaneous route of administration for mipomersen may affect compliance especially with long term treatment. The most common adverse reactions...
Read More
