血塞通注射液对鼠肝CYP3A体外抑制作用研究

Inhibition Potential of Xuesaitong Injection on Rat Liver Microsomal CYP3A In Vitro

目的:研究血塞通注射液对大鼠肝微粒体CYP3A酶活性的体外抑制作用。方法:在大鼠肝微粒体体外孵育体系中加入CYP3A酶的底物睾酮和不同体积的血塞通注射液,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。酮康唑为阳性对照药。结果:在大鼠肝微粒体体外孵育体系中,血塞通注射液对CYP3A酶的IC_(50)和K_1值分别为血塞通注射液原液的0.87%和0.43%。结论:血塞通注射液在体外对大鼠肝微粒体CYP3A酶活性有抑制作用,符合混合型抑制模型。

Objective： To investigate the inhibition potential of Xuesaitong injection （XSTI） on rat liver microsome CYP3A in vitro. Method： The rat liver microsomes were incubated with different volumes of XSTI 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 XSTI on the activity of CYP3A in rat liver mierosome. Ketoconazole was used as a positive control. Result： In in vitro incubation systems, the IC50 value and Ki value of XSTI on rat liver mierosome CYP3A were 0.87% and 0.43% （v/v） respectively. Conclusion： XSTI can depress rat liver microsome CYP3A activity in vitro, is a mixed inhibitor to CYP3A.