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[摘要]
目的 研究瓜蒌皮注射液对人肝细胞色素P450(CYP450)酶4种亚型CYP1A2、CYP2B6、CYP2C9和CYP2D6的体外抑制作用。方法 瓜蒌皮注射液8个不同浓度(2%、1%、0.2%、0.05%、0.01%、0.005%、0.002%、0.000 5%)的工作液分别与4种CYP450酶亚型的探针底物混合,即非那西丁(CYP1A2)、安非他酮(CYP2B6)、双氯芬酸(CYP2C9)、右美沙芬(CYP2D6),用维拉帕米作为内标,在人肝微粒体中孵育,采用高效液相色谱法检测4种探针底物的剩余浓度,计算半数抑制浓度(IC50)。结果 瓜蒌皮注射液对CYP1A2、CYP2B6、CYP2C9和CYP2D6的IC50值均大于临床常用量。结论 正常用量下,瓜蒌皮注射液对人CYP450酶的4亚型无明显影响。
[Key word]
[Abstract]
Objective To study inhibitory effects of Gualoupi Injection on 4 subtypes of human liver cytochrome P450s (CYP1A2, CYP2B6, CYP2C9, and CYP2D6). Methods Eight different doses of Gualoupi Injection (2%, 1%, 0.2%, 0.05%, 0.01%, 0.005%, 0.002%, and 0.000 5%) were incubated with human liver microsomes in 4 kinds of specific probe substrates, including phenacetin (CYP1A2), amfebutamone (CYP2B6), diclofenac (CYP2C9), and dextromethorphan (CYP2D6). Verapamil was used as internal reference to calculate other specific probe substrates. HPLC-UV method was used to analyze the residual concentration of specific probe substrates and calculate the IC50 values. Results IC50 values of Gualoupi Injection with CYP1A2, CYP2B6, CYP2C9, and CYP2D6 were higher than the therapeutic dose. Conclusion Gualoupi Injection might not has significant effect on 4 subtypes of human CYP450s within curing dose.
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[基金项目]
常州市科技计划项目(1130)