Posted by admin on Jul 31, 2016 in |
The present research aimed to evaluate the binding effect of hydroalcoholic extracts of leaf and Stem bark of Prosopis cineraria (PCL and PCB) with Calf Thymus (CT) DNA. The interaction of the PCL and PCB with Calf Thymus (CT) DNA has been studied using absorption spectra, viscosity measurements and cyclic voltammetry methods. It was observed that the PCL and PCB exhibited hypochromic and bathochromic shifts in the absorption spectra on binding to DNA which is a typical characteristic of DNA intercalation. In viscosity measurements, varying concentration of PCL and PCB causes a significant increase in viscosity of DNA. The variations of the cyclic voltammetric behavior of both extracts PCL and PCB was noted which demonstrate intercalative interaction between the PCL, PCB and the CT-DNA. In conclusion, both PCL and PCB possessed good DNA-binding...
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Posted by admin on Jul 31, 2016 in |
Oxidative stress is a condition due to excessive production of free radicals than the ability of the antioxidant system to counteract them. Antioxidants scavenge and suppress the deleterious effects of free radicals. Both exogenous and endogenous sources of antioxidants are important in pathological conditions. Exogenous antioxidants include dietary sources and even include medicinal plants. These medicinal plants contain phytochemicals which contribute to the beneficial antioxidant activity. Wheat germinated over a period of 9-10 days is generally called wheat grass. The purpose of this work is to determine the phenolic, flavonoids, flavonols and total alkaloids from wheat grass juice. Free radical scavenging activity of wheat grass juice was evaluated by using DPPH , nitric oxide, hydroxyl radical and total antioxidant power by FRAP assay and antilipidperoxidation activity by using mice liver and brain. Wheat grass juice is found to have good antioxidant action in various models due to its polyphenols and...
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Posted by admin on Jul 31, 2016 in |
Ischemic heart disease (IHD) is the major cause of morbid-mortality in most countries. The involvement of inflammation and oxidative stress (OS) in the development of atherosclerosis, ischemic cardiopathy triggering phenomen, has been investigated. The high sensitive C-reactive protein (hs_CRP) was measured in serum by immunoenzymatic method. Serum total homocysteine (Hcy) concentration was measured by fluorescence polarization immunoessay. Plasma levels of substances reacting with thiobarbituric acid (TBARS) were carried out by fluorimetric method (Yagi). Erythrocyte activity of superoxide dismutase (SOD) and plasma total antioxidant status (TAS) were determined by a colorimetric method at 505nm and 600nm, respectively. Erythrocyte activity of catalase (CAT) was measured by colorimetric assay (Goth). Our study showed significant elevation of hs_CRP, TBARS and Hcy levels in patients compared to controls. While we noted significant decrease in TAS levels, SOD and CAT activities in patients compared to the control group. We also noted positive correlations between: hs_CRP-Hcy, hs_CRP-TBARS, Hcy-TBARS, SOD-TAS, CAT-TAS and negative correlations between: hs_CRP-SOD, hs_CRP-CAT, hs_CRP-TAS, TBARS-SOD, TBARS-CAT, TBARS-TAS, Hcy-SOD, Hcy-CAT and Hcy-TAS. This unsuitability,...
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Posted by admin on Jul 31, 2016 in |
The present research has been focused on the development of pharmacophore mapping and docking studies of indole/benzoximidazole-5-carboximidine derivatives as anti-cancer agents that can explore basic pharmacophore responsible for biological activity of structurally diverse compounds and also their binding affinity to the urokinase-type plasminogen activator (uPA). For pharmacophore mapping, a highly predictive pharmacophore based 3D-QSAR model was generated. Molecular docking experiments were carried out by means of the Glide module of the Schrodinger. A cubing receptor grid was centred around the co-crystallized ligand where the active binding site is present. The XP (extra precision) scoring function of GLIDE 6.0 was used. The scoring function of GLIDE docking program is presented in the G-score form which indicates the binding affinity of the designed compound to the receptor. A five point pharmacophore (APRRR) with one acceptor atom, one positively charged group and three aromatic rings as pharmacophore was developed. The generated best pharmacophore hypothesis yielded a statistically significant QSAR model, with a correlation coefficient of R2 = 0.8548 for training set molecules....
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Posted by admin on Jul 31, 2016 in |
Numerous carbazole derivatives were designed by the Chemsketch software followed by 3D optimization. Docking studies were performed using AUTODOCK 4.2.6 software to check their binding interactions with eukaryotic topoisomerase-I, based on the crystal structure of Human Topoisomerse-I-DNA complex (PDB ID: 1A35). Results of docking studies of designed carbazole derivatives were compared on the basis of their minimum binding energy with a well known topoisomerase-I inhibitor i.e. Adriamycin,. Above results were used to find out active compounds and two series of such active compounds i.e. 2-[(4, 5-dihydro-2-substitutedphenyl)imidazol-1-ylamino]-1-(9H-carbazol-9-yl)ethanone (3a-3e) and 2-(9H-carbazol-9-yl)-N’-[{(4-substitutedphenyl)(piperazin-1-yl)} methyl] aceto hydrazide (6a-6e) were synthesized. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR, MASS spectrometry and elemental analysis and also screened for their in vitro anticancer activity against human breast cancer cell line (MCF 7) by sulphorodamine B (SRB) assay method. GI50 was measured by using 10, 20, 40 and 80 µg/ml concentrations of tested compounds along with the standard i.e. Adriamycin. Results revealed that the tested compounds 3a, 3d, 6c, 6d and 6e were...
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