瓜蒌皮注射液对人肝微粒体CYP450酶4种亚型的影响  

Effects of Gualoupi Injection on 4 subtypes of human liver CYP450

作　　者：邹凯杰 石壬伟 袁传顺[2] 陆再华 罗立波 ZOU Kai-jie;SHI Ren-wei;YUAN Chuan-shun;LU Zai-hua;LUO Li-bo(Department of Pharmacy,The No.7 People＇s Hospital of Changzhou,Changzhou 213000,China;Science and Education Division,The No.7 People＇s Hospital of Changzhou,Changzhou 213000,China;Department of Cardiology,The No.7 People＇s Hospital ofChangzhou,Changzhou 213000,China)

机构地区：[1]常州市第七人民医院药剂科,江苏常州213000 [2]常州市第七人民医院科教科,江苏常州213000 [3]常州市第七人民医院心内科,江苏常州213000

出　　处：《现代药物与临床》2018年第11期2769-2775,共7页Drugs & Clinic

基　　金：常州市科技计划项目(1130)

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(IC_(50))。结果瓜蒌皮注射液对CYP1A2、CYP2B6、CYP2C9和CYP2D6的IC_(50)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。Objective To study inhibitory effects of Gualoupi Injection on 4 subtypes of human liver cytochrome P450 s（CYP1 A2, CYP2 B6, CYP2 C9, and CYP2 D6）. 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（CYP1 A2）, amfebutamone（CYP2 B6）, diclofenac（CYP2 C9）, and dextromethorphan（CYP2 D6）. 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 IC_（50） values. Results IC_（50） values of Gualoupi Injection with CYP1 A2, CYP2 B6, CYP2 C9, and CYP2 D6 were higher than the therapeutic dose. Conclusion Gualoupi Injection might not has significant effect on 4 subtypes of human CYP450 s within curing dose.

关 键 词：瓜蒌皮注射液 细胞色素P450 人肝微粒体 半数抑制浓度 

分 类 号：R966[医药卫生—药理学]