SM-1对人肝微粒体细胞色素P450亚型酶的抑制作用  

Inhibitory effect of SM-1 on human liver microsomal cytochrome P450 enzyme

作　　者：陈燕芬[1] 陈景秀[1] 孙萌[1] 丁俊垚 程泽能[1] 胡高云[1] 丁劲松[1] 朱曲波[1] CHEN Yan-fen CHEN Jing-xiu SUN Meng DING Jun-yao CHENG Ze-neng HU Gao-yun DING Jin-song ZHU Qu-bo(School of Pharmaceutical Sciences in Central South University,Changsha 410013, China)

机构地区：[1]中南大学湘雅药学院,湖南长沙410013

出　　处：《中国药理学通报》2017年第5期627-629,共3页Chinese Pharmacological Bulletin

基　　金：国家科技部"重大新药创新与发展"重大专项项目(No2012ZX09103101-051);基础研究中国中央大学资助项目(No 7601110179);中南大学研究生自主探索创新基金(No 2016zzts494)

摘　　要：目的观察SM-1对人肝细胞色素P450酶系统中7种亚型酶活性的影响。方法在体外将一定浓度的底物或SM-1与人肝微粒体孵育30 min,分为对照组(底物)和实验组(底物和SM-1),以非那西丁、安非他酮、紫杉醇、甲苯磺丁脲、奥美拉唑、右美沙芬、睾酮为CYP探针底物,应用HPLC法检测各探针底物代谢量,计算抑制率,评价SM-1对人肝微粒体CYP1A2、2B6、2C8、2C9、2C19、2D6、3A4酶的抑制活性。结果 SM-1对CYP1A2、2B6、2C8、2C9、2C19、2D6、3A4的抑制率分别是0.05%、3.37%、0.08%、2.07%、4.20%、-0.15%和10.84%。结论 SM-1对CYP3A4可能有抑制作用,临床用药时应注意因CYP酶抑制引起的药物相互作用。Aim To investigate the effect of SM-1 on seven main cytochrome P450（CYP450）in human liver microsomes.Methods Substrate or SM-1 was incubated with human liver microsomes for 30 min in vitro, and divided into control group and experimental group.The effects of SM-1 on the main phase I metabolic enzymes in human liver microsomes was detected by HPLC.Phenacetin, bupropion, paclitaxel, tolbutamide, omeprazole, dextromethorphan, testosterone were investigated as probe drugs.Results Inhibition rate of SM-1 on the classical substrate of human liver microsomal CYP was 0.05%,3.37%,0.08%,2.07%,4.20%,-0.15% and 10.84%, respectively.Conclusions SM-1 may have inhibitory effect on CYP3A4.Attention should be paid to the interaction of clinical drug induced by CYP enzyme inhibition.

关 键 词：SM-1 细胞色素P450 底物 抑制率 肝微粒体 亚型酶 

分 类 号：R322.47[医药卫生—人体解剖和组织胚胎学] R345.99[医药卫生—基础医学]