灯盏细辛注射液对大鼠肝微粒体CYP3A的抑制作用

中国临床药理学与治疗学 ›› 2009, Vol. 14 ›› Issue (8): 891-895.

灯盏细辛注射液对大鼠肝微粒体CYP3A的抑制作用

韩永龙^1,2,3, 余奇¹, 孟祥乐¹, 李丹¹, 卞卡², 郭澄¹

¹上海交通大学附属第六人民医院药剂科, 上海 200233;
²上海中医药大学穆拉德中药现代化研究中心, 上海 201203;
³大庆油田总医院临床药学科, 大庆 163001, 黑龙江

收稿日期:2009-06-24 修回日期:2009-07-14 出版日期:2009-08-26 发布日期:2020-10-30
通讯作者: 郭澄, 男, 博士, 教授, 主任药师, 博士研究生导师, 主要从事中药学与临床药理学研究。Tel:021-64369181-8098 E-mail:gboss@sina .com
作者简介:韩永龙, 男, 在读博士研究生, 副主任药师, 主要从事中药药物代谢及药代动力学研究。Tel:021-64369181-8789 E-mail:yonglongh@sina.com
基金资助:
上海市药学会上海医院药学科研基金(2008-YY-0227) 资助

Inhibition of Dengzhanxixin injection on rat liver microsomal CYP3A

HAN Yong-long^1,2,3, YU Qi¹, MENG Xiang-le¹, LI Dan¹, BIAN Ka², GUO Cheng¹

¹The Sixth People's Hospital Affiliated of Shanghai Jiao Tong University, Shanghai 200233, China;
²Murad Research Institute for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China;
³Department of Clinical Pharmacy, Daqing Oilfield General Hospital, Daqing 163001, Heilongjiang, China

Received:2009-06-24 Revised:2009-07-14 Online:2009-08-26 Published:2020-10-30

摘要/Abstract

摘要： 目的: :研究灯盏细辛注射液对大鼠肝微粒体CYP3A 酶活性的抑制作用。方法: :在体外大鼠肝微粒体孵育体系中加入底物睾酮和不同体积的灯盏细辛注射液, 用高效液相色谱法测定睾酮的羟化代谢产物 6β-羟基睾酮的生成量反映 CYP3A酶的活性。酮康唑用作阳性对照药。结果: :在体外孵育体系中, 灯盏细辛注射液对大鼠肝微粒体CYP3A 酶活性有抑制作用, IC50 和 Ki 值分别为0.40%和 0.24%(V/V) 。结论: :体外给药灯盏细辛注射液对大鼠肝微粒体 CYP3A 酶活性有抑制作用, 符合混合型抑制模型

关键词: 灯盏细辛注射液, 鼠肝微粒体, CYP3A酶, 抑制作用, 药物相互作用

Abstract: AIM: To investigate the inhibition of Dengzhanxixin injection on rat liver microsome CYP3A in vitro .METHODS: The rat liver microsomes were incubated with different doses of Dengzhanxixin injection at the present of testosterone, a specific substrate of CYP3A, whose metabolite (6β-hydroxytestosterone) in incubation systems was measuered by HPLC to esti-mate the effect of Dengzhanxixin injection on the activity of CYP3A in rat liver microsome .Ketoconazole was used as a positive control. RESULTS: In in vitro in-cubation systems, Dengzhanxixin injection has inhibition on rat liver microsomal CYP3A, the IC50 value and Ki value are 0.40%and 0.24%(V/V) , respectively . CONCLUSION: Dengzhanxixin injection which can depress CYP3A activity, is a mixed inhibitor to CYP3A.

Key words: Dengzhanxixin injection, rat liver microsome, CYP3A, inhibition, drug-drug interaction

中图分类号:

R965.2

韩永龙, 余奇, 孟祥乐, 李丹, 卞卡, 郭澄. 灯盏细辛注射液对大鼠肝微粒体CYP3A的抑制作用[J]. 中国临床药理学与治疗学, 2009, 14(8): 891-895.

HAN Yong-long, YU Qi, MENG Xiang-le, LI Dan, BIAN Ka, GUO Cheng. Inhibition of Dengzhanxixin injection on rat liver microsomal CYP3A[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2009, 14(8): 891-895.

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