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胡椒碱和胡椒基丁醚对大鼠肝脏药物代谢酶系统影响的差异

Differences in the effects of piperine and piperonyl butoxide on hepatic drug-metabolizing enzyme system in rats.

作者信息

Dalvi R R, Dalvi P S

机构信息

Toxicology Laboratory School of Veterinary Medicine, Tuskegee University, Alabama 36088.

出版信息

Drug Chem Toxicol. 1991;14(1-2):219-29. doi: 10.3109/01480549109017878.

Abstract

An i.p. administration of rats with piperine (100 mg/kg) and piperonyl butoxide (400 mg/kg) produced a significant decrease in hepatic cytochrome P-450, and activities of benzphetamine N-demethylase, aminopyrine N-demethylase and aniline hydroxylase 1 hr after the treatment. Twenty-four hr later, these parameters along with cytochrome b5 and NADPH-cytochrome c reductase remained depressed only in piperine-treated rats. In contrast, piperonyl butoxide caused a significant induction of these parameters with the exception of cytochrome b5 and aminopyrine N-demethylase, which were up by 36 and 33% over their respective controls but not significantly. These results point up that effect of piperine on hepatic mixed-function oxidases is monophasic while that of piperonyl butoxide is biphasic.

摘要

给大鼠腹腔注射胡椒碱(100毫克/千克)和胡椒基丁醚(400毫克/千克)后1小时,肝细胞色素P-450、苄非他明N-脱甲基酶、氨基比林N-脱甲基酶和苯胺羟化酶的活性显著降低。24小时后,仅在胡椒碱处理的大鼠中,这些参数以及细胞色素b5和NADPH-细胞色素c还原酶仍处于抑制状态。相比之下,胡椒基丁醚除细胞色素b5和氨基比林N-脱甲基酶外,对这些参数有显著诱导作用,细胞色素b5和氨基比林N-脱甲基酶分别比各自对照组升高36%和33%,但无统计学意义。这些结果表明,胡椒碱对肝混合功能氧化酶的作用是单相的,而胡椒基丁醚的作用是双相的。

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