目的 評(píng)價(jià)丹參注射液在體外對(duì)人肝微粒體酶CYP2C9、CYP2C19、CYP2D6活性的影響。方法 將丹參注射液與CYP450酶3種亞型(CYP2C9、CYP2C19、CYP2D6)的特異性探針底物甲苯磺丁脲、奧美拉唑、右美沙芬與大鼠肝微粒體進(jìn)行孵育,采用LC-MS/MS法測(cè)定對(duì)應(yīng)3種代謝產(chǎn)物4-羥基甲苯磺丁脲、5-羥基奧美拉唑、右啡烷的濃度,求算出IC₅₀。結(jié)果 丹參注射液對(duì)CYP2C9、CYP2C19和CYP2D6的IC₅₀值均>50 μg/mL。結(jié)論 丹參注射液對(duì)人肝微粒體酶CYP2C9、CYP2C19、CYP2D6沒有抑制作用。

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.