SYNTHESIS AND ASSESSMENT OF HEPATOPROTECITVE ACTIVITY OF SOME NEW 2-ARYL TETRAHYDROQUINOLINE AND SPIROOXYINDOLYL TETRAHYDROQUINOLINE DERIVATIVES
Keywords:
Tetrahydroquinolines, Imino diels-Alder reaction, Antimony (III) sulfate, Hepatoprotecitve, Silymarin, Liver, Carbon tetrachlorideAbstract
Objective: To evaluate the hepatoprotecitve potential of some newly synthesized tetrahydroquinoline derivatives against carbon tetrachloride induced hepatic damage in wister rats.
Methods: A series of 2-aryl, 4-N vinyl pyrrolido/caprolacto and spirooxy indolyl tetrahydroquinolines were synthesized by imino Diels-Alder reaction using Antimony (III) sulfate as catalyst. The titled compounds were characterized by IR, 1HNMR spectroscopy and screened for hepatoprotecitve activity. Hepatopotoxicity was induced in male Wister rats by intrperitoneal injection of CCl4. Wister rats weighing 150-200g were randomly assigned in to various groups of six animals each. Group I – Normal control received only 1% Tween in distilled water, Group II – Served as negative control received CCl4 in liquid paraffin 1 ml/kg p. o. at every 72 h for 10 days. Group III – X were intoxicated with CCl4 1 ml/kg p. o. before the administration of Silymarin 100 mg/kg p. o. and suspension of synthetic derivatives in polyethylene glycol-400 at the dose of 25 mg/kg p. o. for 10 days. Different hepatic biochemical parameters viz. SGOT, SGPT, SALP, Total and direct bilirubin were evaluated before and after treatment to investigate the hepatoprotecitve activity.
Results: It was observed that in CCl4 intoxicated group; total and direct bilirubin, SGOT, SGPT, SALP levels were significantly increased as compared to control group. Administration of synthesized tetrahydroquinoline derivatives at the dose of 25 mg/kg p. o. reduced these pathological damages caused by CCl4 intoxication compared to normal and Silymarin treated groups.
Conclusion: The present study revealed that synthesized tetrahydroquinoline derivatives, showed hepatoprotecitve potential against CCl4 induced hepatotoxicity in wister rats, thus offering a novel synthetic formulation as a hepatoprotecitve drug.
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