灯盏细辛注射液对大鼠肝微粒体CYP3A的抑制作用  

Inhibition of Dengzhanxixin injection on rat liver microsomal CYP3A

作　　者：韩永龙[1,2,3] 余奇[1] 孟祥乐[1] 李丹[1] 卞卡[2] 郭澄[1] 

机构地区：[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

出　　处：《中国临床药理学与治疗学》2009年第8期891-895,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：上海市药学会上海医院药学科研基金(2008-YY-0227)资助

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。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 estimate 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 incubation 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.

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 

分 类 号：R965.2[医药卫生—药理学]