甘草次酸在人细胞色素CYP450中体外代谢研究(英文)

被引：31

作者：

刘丽

肖娟

彭志红

陈勇

机构：

[1] 湖北大学中药生物技术省重点实验室

来源：

药学学报 | 2011年 / 01期

关键词：

甘草次酸; 代谢; 人肝微粒体; 细胞色素P450;

D O I：

暂无

中图分类号：

R969 [临床药理学];

学科分类号：

100706 [药理学];

摘要：

甘草根是中医临床常用解毒草药,其活性成分甘草次酸主要是通过肝脏代谢。本文研究了人肝微粒体以及人源性CYP450s对甘草次酸的体外代谢影响,以及甘草次酸对几种CYP450酶活性的影响。实验结果表明,甘草次酸体外主要代谢酶为CYP3A4。体外药代动力学参数Km,Vmax和CLint分别为18.6μmol.L-1,4.4 nmol.mg-1(protein).min-1和0.237 mL.mg-1(protein).min-1。体外抑制试验显示,50μmol.L-1甘草次酸可以抑制CYP2C19、CYP2C9、CYP3A4酶的活性,其抑制率可高达50%以上。

引用

页码：81 / 87

页数：7

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