Posted by admin on Apr 30, 2015 in |
Warfarin and coumarin containing drugs act on Vitamin K epoxide reductase to show its anti-coagulant activity. In this study, three different series of 5- hydroxy coumarin containing phenyl, furan and pyran substituents at third position were designed. Molecular docking studies were performed to determine binding modes and affinities of ligand molecule towards Vitamin K epoxide reductase. In docking studies pair wise linear potential (PLP score) was used as a scoring function and systematic search method to find out bio active conformer. Ligand 2B, 2C, 2D, 2E, 3C, 3D has shown more negative binding energies, which reflects its affinity towards a vitamin K epoxide reductase. Ligand 1A, 1E, 3D has shown maximum hydrogen bond interactions as compared to warfarin. Tyr178, Thr72, Met111, Glu115amino acid residues were involved in the ligand-protein interactions. Hydroxy, methoxy, ethoxy and methyl substitutions has played major roles in the ligand-protein interaction. Therefore, 3-substituted -5-hydroxy coumarins could be served as good drug candidates for anticoagulant activity and additional experimental studies are warranted to locate their importance as...
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Posted by admin on Apr 3, 2015 in |
Honey possesses a wide range of medicinal properties due to presence of phytochemicals including flavonoids and phenolic acids. Free radicals and process of angiogenesis are one of the major contributors to cancer development and the use of phytoconstituents as reactive oxygen species scavengers and as an antiangiogenic moiety has clinical potential and may be having less negative side effects than the existing drugs. This study has explored the phyto-constituents as well as anti-angiogenic and anti-oxidant activity of Indian honey (Kashmir honey and dhanwantari honey) in comparison with manuka honey. The total phenolic content was measured by folin ciocalteau method and antioxidant activity was estimated by DPPH scavenging assay. Anti-angiogenic activity of honey samples were evaluated by chorioallantoic membrane (CAM) assay. Drabkin’s assay was performed in order to check the hemoglobin content of the chorioallantoic membrane sections. Presence of flavonoids and tannins were observed in all honey samples. Higher total phenolic content was found in kashmir honey (6662.67 mg GAE /100 gm honey) than manuka honey (6078.67 mg GAE /100...
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Posted by admin on Mar 30, 2015 in |
In the present study, a new series of 2, 4, 5- trisubstituted imidazoles derivatives were synthesized taking different aldehydes as substitutions. The preliminary characterization of synthesized compounds identified by physical constants determination and TLC. The chemical structures were confirmed by means of IR, 1H-NMR and Mass spectral data. The synthesized compounds were screened for their anti-microbial and antifungal activity using standard methods. Both gram positive and gram negative organisms such as E.coli, B.subtilis, S.aureus, A. niger, C.albicans were used. The compounds screened for their antibacterial and antifungal activities A1, A2, A4 have shown promising antibacterial and antifungal activity against as compared to standard drugs Ciprofloxacin and Griseofulvin. The compounds were also screened for their antidepressant activities using forced swimming test in mice in which A1, A2 and A6 are found to be most significant while compounds A4 and A5 showed moderate activity as compared to standard drug Fluoxetin. The compound A4, 4-(4, 5-diphenyl-1H-imidazole-2-yl) phenol exhibited excellent...
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Posted by admin on Mar 30, 2015 in |
Medicinal plants have been used since prehistoric period for the cure of various diseases. Hence the herbal medicines occupy distinct position right from the primitive period to present day. Calotropis procera, a wild growing plant of family Asclepiadaceae, is well known for its medicinal properties. Different parts of this plant have been reported to exhibit anti-inflammatory, analgesic, and antioxidant properties. Calotropis gigantea found in dry waste places, therapeutically used as Anti-cancer, intermittent fever, paralysed part of body painful joints, swelling, heals wounds (leaves). The present study was undertaken to analyse the various active phytochemical constituents and to study detailed anatomical features of two species of Calotropis (family: Asclepediaceae) i.e., C.procera, C.gigantea. A qualitative analysis was performed for detection of alkaloids, glycosides, terpenoids, steroids and flavanoids. HPLC (High Performance Liquid Chromatography) was used in identifying the qualitative and quantitative analysis of active principle index of two species of Calotropis present in the area of present study. Anatomical features of various plant parts were found useful for correct easy identification of...
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Posted by admin on Mar 30, 2015 in |
In eukaryotes, DNA is packaged into chromatin structures, whose basic unit is the nucleosome. A principle component of chromatin that plays an important role in the regulation of DNA is the modification of histones. Since histones are post-translationally modified, there inludes a large number of different histone post-translational modifications. These histone modifications create a repressive environment for gene expression, which in case of histone acetylation, are controlled by competing activities of two families of enzymes, histone acetyltransferases (HAT’s) and histone deacetylases (HDACs). HDAC11 is a class IV protein of the HDAC family. The present aim of this study is to develop a model of HDAC11 by using bioinformatics applications. The design of the model is based on thorough evaluation of the HDAC-11 query sequence, Q96DB2, which was retrieved from UniProtKB. The physiochemical and primary analysis were computed using ExPASy Protparam tool. Functional characterization was computed using RaptorX, HMMTOP and Softberry Server’s CYS_REC tool (Cysteine Recognition Server) which predicted the secondary structure composition, presence of transmembrane proteins and the presence...
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