中国药理学通报2013，Vol.29Issue(4)：512-519,8.DOI:10.3969/j.issn.1001-1978.2013.04.016
黄芪颗粒和黄芪注射液对CYP1A2、CYP2D、CYP2C亚酶活性影响的实验研究
Experimental study on effect of Astragalus granules and Astragalus injection on enzymatic activities of CYP1A2, CYP2D and CYP2C
摘要
Abstract
Aim To study the effects of Astragalus granules and Astragalus injection on the enzymatic activities of CYP1A2, CYP2D and CYP2C through the experimental researches in vivo and in vitro.Methods A cocktail vitro reaction system was established.Metabolins of enzymes were detected by the methods of LC/MS/MS.The effect of Astragalus granules and Astragalus injection on the enzymatic activities of CYP1A2, CYP2D6, CYP2C9 and CYP2C19 isoforms were calculated.Rats were randomly divided into the control groups and the experimental groups, each group got gavage administrations of different concentrations of Astragalus granules and Astragalus injection for 10 days.Then the liver microsomes were prepared to proceed the experiment of cocktail to assess the effects in rats of two kinds of drugs on the enzymatic activities of CYP1A2, CYP2D1, CYP2C6 and CYP2C11 isoforms in vivo.Results Enzymatic activities of CYP2D6, CYP2C19 and CYP1A2 isoforms were suppressed significantly by Astragalus granules and Astragalus injection in vitro experiments of cocktail.But they had no effect on the CYP 2 C 9 isoform .In the experiments of gavage administration, enzymatic: activity of CYP1A2 isoform increased significantly by 2.13 ,3.23 and 2.20 times when the doses of Astragalus granules were 32, 160 and 800 mg·kg-1·d-1 and enzymatic activity of CYP1A2 isoform increased significantly by 1.65,2.26 and 2.89 times when the doses of Astragalus injection were 0.16, 0.8 and 4 g·kg-1·d-1 .However, enzymatic activities of CYP2D1, CYP2C6 and CYP2C11 isoforms were not induced by the two kinds of drugs.Conclusions Astragalus granules and Astragalus injection supress enzymatic activities of CYP2D6 and CYP2C19 while increase enzymatic activity of CYP1A2 in rats.关键词
黄芪颗粒/黄芪注射液/CYP1A2/CYP2D/CYP2C/酶活性Key words
Astragalus granules ( AG )/ Astragalus injection (AI)/ CYP1A2/ CYP2D/ CYP2C/ enzymatic activity分类
医药卫生引用本文复制引用
张咏莉,崔玉强,汪向升,李静清,陈江英..黄芪颗粒和黄芪注射液对CYP1A2、CYP2D、CYP2C亚酶活性影响的实验研究[J].中国药理学通报,2013,29(4):512-519,8.基金项目
国家"重大新药创制"科技重大专项(No 2009ZX09304-003,2008ZX09312) （No 2009ZX09304-003,2008ZX09312）
