目的 评价丹参注射液在体外对人肝微粒体酶CYP2C9、CYP2C19、CYP2D6活性的影响。方法 将丹参注射液与CYP450酶3种亚型(CYP2C9、CYP2C19、CYP2D6)的特异性探针底物甲苯磺丁脲、奥美拉唑、右美沙芬与大鼠肝微粒体进行孵育,采用LC-MS/MS法测定对应3种代谢产物4-羟基甲苯磺丁脲、5-羟基奥美拉唑、右啡烷的浓度,求算出IC₅₀。结果 丹参注射液对CYP2C9、CYP2C19和CYP2D6的IC₅₀值均>50 μg/mL。结论 丹参注射液对人肝微粒体酶CYP2C9、CYP2C19、CYP2D6没有抑制作用。

Objective To investigate the inhibitory effect of Danshen injection on the activities of three human cytochrome P450 enzymes (CYP2C9, CYP2C19, CYP2D6) in vitro. Methods The Danshen injection, three specific probe of cytochrome P450 enzymes (including orinase, omeprazole, and dextromethorphan) and human liver microsome were coincubated. The concentration of the three kinds of metabolites (including 4-hydroxy tolbutamide, 5-hydroxy omeprazole, and dextrorphan) were analyzed by LC-MS/MS assay. The values of IC₅₀ were calculated. Results The IC₅₀ values of Danshen Injection on CYP2C9, CYP2C19, and CYP2D6 were more than 50 μg/mL. Conclusion The Danshen Injection has not significant inhibitory effect on the activities of CYP2C9, CYP2C19, and CYP2D6.