Posted by admin on Aug 31, 2020 in |
Novel coronavirus (nCovid-19) is a recent emerging, dangerous pathogen that has shaken the whole world. Present therapeutic strategies to deals with this infectious disease are only supportive. The discovery of a new drug within a short period of time is a great task. Structure predictions of several proteins associated with SARS-CoV-2, the virus that causes COVID-19, was made possible by Genomics. Docking is a computational method used in present days to identify a hit molecule by measuring the binding ability of molecular drugs within the binding pocket of the macromolecular target. In this study, we have selected five ligand molecules which are currently used as antiviral agents. The drugs selected are, namely, Acyclovir, Ganciclovir, Penciclovir, Valaciclovir, and deoxyguanosine. The protein with PDB id 6LU7 was retrieved from the protein data bank for the docking procedure. The 2D plot of interactions was obtained using discovery studio visualizer software, and energy calculations were done by summing up van der Waals, electrostatic, and Hydrogen bonding interactions. Acyclovir and its derivatives are found...
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Posted by admin on Aug 31, 2020 in |
Coumarin and its analogs have a wide range of attention in the treatment of hormone-dependent breast cancer by blocking the formation of estrogen through the inhibition of estrogen receptor. However, the Schiff bases are an important class of compounds with structural similarities of natural biological substances and also due to their presence of imine (-N=CH-), which have an impact on a biological system. Considering the above all facts, the present research work is aimed to design the series of building blocks of coumarin Schiff base moiety as target candidates for estrogen receptor. The designed molecules ensured their reliability through the in-silico drug designing model and subjected to a preliminary study by screening their violation of Lipinski rule of five, if any, predicted for their ADMET profile study by using online available tools. Later an attempt was made to synthesize the proposed compounds, and structural elucidation was done by IR, NMR, and Mass spectroscopy. Besides to this, an in-vitro cytotoxicity study by using human breast cancer cell lines also carried...
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Posted by admin on Aug 31, 2020 in |
Simple, sensitive, and accurate spectrophotometry method one each for estimation of five drugs viz., chloroquine phosphate (CHP), granisetron hydrochloride (GRA), rizatriptan benzoate (RIZ), zoledronic acid (ZOL) and zolmitriptan (ZOT), have been developed. The method depends upon oxidation of each drug by excess N-Bromo succinimide (NS), and subsequent determination of UN reacted NBS by Rhodamine-B dye at λmax 557 nm. Beers law is obeyed between 2-14 µg mL-1 (for CHP); 52-14 µg mL-1 (for GRA); 1-7 µg mL-1 (for RIZ); 1-7 µg mL-1 (for ZOL) & 2-14 µg mL-1 (for ZOT). This method has been applied for the determination of drugs in their pure form as well as in tablet formulations. All the methods have been validated as per ICH...
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Posted by admin on Aug 31, 2020 in |
Alzheimer’s disease is the most common neurodegenerative disease, which initially causes oxidative stresses and leads to neuronal death. It characterized by notable memory loss, cognitive impairment, and personality disorders accompanied by diffuse structural abnormalities in the brain of the aged population. The present work focused on anticholinesterase inhibiting activity Smilax zeylanica and Smilax china against neurodegenerative disorder such as Alzheimer’s diseases on animal model respectively, as proof of preliminary anticholinesterase profile. In this paper, we studied various extracts prepared from roots of Smilax zeylanica and Smilax china for their AChE -inhibitory activity using animals. The ethanolic and various extracts from the plant roots of smilax zeylanica and smilax china were screened for their acetylcholinesterase inhibitory activity by using animals and Ellman’s method. These extracts of smilax china and smilax zeylanica exhibited inhibitory activities were observed (Cortex and Hippocampus) at a concentration of 150 mg/kg, it can be used for further study to treat the neurodegenerative disorders like Alzheimer’s disease...
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Posted by admin on Aug 31, 2020 in |
A simple, sensitive, and rapid Liquid Chromatography-Mass Spectroscopy method was developed and validated for the quantification of Isoproterenol in human plasma using Dobutamine as an internal standard. The method utilized simple liquid-liquid extraction using a mixture of diethyl ether and dichloromethane for the sample preparation involved prior to LCMS analysis. The analytes were chromatographed on Prontosil ODS C18 Column with isocratic elution using methanol, Acetonitrile and Tri ethyl-amine in the ratio of 60:25:15 (v/v) at pH 6.3 as the mobile phase at a flow rate of 0.9 mL/min and the UV detector response of the column eluents were recorded at a wavelength of 248 nm. Quantification was performed in multiple-reaction-monitoring mode with the ion transitions m/z 212.19 → 135.21 for Isoproterenol, m/z 302.19 → 107.05 for Dobutamine. Good linearity was obtained in the range of 0.50–300 ng/mL (r2 = 0.999). The method was fully validated with accuracy, precision, matrix effects, recovery and stability. The results of the stability study confirm that the method was found to be stable. The...
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