Abstract:The objective of the present work was the synthesis of 1-[5-acetyl-4 (4-substituted phenyl)-2, 6-dimethyl-1,4-dihydroxypyridine-3-yl]-ethan-1-one and evaluation of in vivo hepatoprotective activity. Based on this a new series of compound had been planned to synthesize by reacting acetyl acetone with various aromatic aldehydes in the presence of ammonium acetate. The synthesized compounds were characterized by IR, NMR, and Mass spectroscopy. The in-vivo Hepatoprotective activity was carried out by using albino rats. The results displayed that the elevated levels of SGOT, SGPT, ALP and Serum bilirubin were mainly due to CCl 4 intoxication, reduced significantly (*P < 0.05) in rats, after treatment with synthesized compounds. Treatment with a synthesized compound at a dose of 250 mg/kg b.w. decreased the SGOT, SGPT, ALP, Serum bilirubin levels by 6.23% ns (non significantly), 28.96%, 8.81%, and 11.11% ns (non significantly) respectively, while a higher dose of 500 mg/kg b. wt. was more effective, causing a reduction of 25.02%, 47.65%, 24.09% and 27.35%. Silymarin was used as standard drug showed a reduction of 55.09%, 68.98%, 57.46% and 35.04% receiving CCl 4 alone. So depending upon the experimental data it was confirmed that the biochemical parameters of the group treated with compounds were significantly lower than the CCl 4 treated group. Moreover the treatment with the synthesized compounds significantly reduced the previously raised levels of AST, ALT, ALP and bilirubin in hepatotoxic rats. Histopathological investigation displayed that at both doses (250 mg/kg b.w. and 500 mg/kg b.w.) the synthesized compounds were possessed moderate to good hepatoprotective activity, but at 500 mg/kg b.w. executed excellent hepatoprotective activity against CCl4 induced damaged hepatocytes.
The main aim and objective of my present research work was to determine the various important mucoadhesive parameters such as mucoadhesive force, force of adhesion and bonding strength etc. Mucoadhesive properties of natural polymers were evaluated by formulating gels using Carbopol 940 P as a gelling agent. Mucoadhesive parameters of the prepared Carbopol 940 P gels containing natural polymers were determined by ex vivo followed by modified physical balance using excised cock intestinal mucosa. From the recent experimental data it was displayed that the mucoadhesive strength, force of adhesion and bonding strength of gel containing low methoxy pectin (1 % w/v) was found higher than other tested gels. The gel containing Moringa oleifera gum (1 % w/v) exhibited less mucoadhesion than other tested gels. The order of mucoadhesion of these plant-derived polymers was found as: low methoxy pectin > jackfruit seed starch > cashew gum/okra gum gum > pumpkin pectin > linseed mucilage > sago starch > gum Arabic > xanthan gum > fenugreek seed mucilage/black palm seed polysaccharide > Moringa oleifera gum.
Keywords: Mucoadhesion, Mucoadhesive strength, gelling agent, intestinal mucosa, and plant derived polymers etc.
The main aim and objective of the present research work was the isolation of some novel bioflavanoids from methanolic extract of peels of sweet lime (MEE-PSWL) and evaluation of in vitro anticancer activity followed by molecular docking against target protein topoisomerase II. The extraction was done by reflux condensation method and preliminary phytochemical screening of MEE-PSWL was carried out for the evaluation of bioactive molecules, the bioflavanoids present in MEE-PSWL was confirmed by spectral analysis such as ESI-MS-MS and FTIR. Molecular docking of isolated compounds was carried out against target protein Topoisomerase II with PDB id 1ZXM by Auto dock program and the best dock pose was selected based on the interaction study analysis. In vitro anticancer activity MEE-PSWL was evaluated by SRB assay toward human colon adenocarcinoma cell line SW620 and the test was carried out at different concentrations. A preliminary screening displayed that the MEE-PSWL was able to inhibit the proliferation of more than 60% of human colon adenocarcinoma SW620 cells. The maximum growth of inhibition was found to be at 125µg/ml (IC50 4.5µg/ml) and the standard drug doxorubicin was found to inhibit the maximum proliferation at concentration 75µg/ml (IC50 3µg/ml).
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