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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 study the inhibitory effect of Xuesaitong injection in vitro on the activity of CYP3A in rat liver microsomes. Methods: The testosterone CYP3A enzyme substrate and different volumes of Xuesaitong injection were added into rat liver microsomal in vitro system to measure the formation of 6β-hydroxytestosterone in testosterone by high performance liquid chromatography CYP3A enzyme activity. Ketoconazole is a positive control. Results: The IC 50 and K 1 values of Xuesaitong injection for CYP3A enzyme were 0.87% and 0.43% of that of Xuesaitong injection respectively in the in vitro incubation system of rat liver microsomes. Conclusion: Xuesaitong injection can inhibit the activity of CYP3A in rat liver microsomes in vitro, which is in accordance with the mixed inhibition model.