半枝莲粗提物对人肝脏细胞色素P450酶的影响.pdfVIP

中南药学2008年2月第6卷第1期 Central South Pharmacy．February 2008，Vo1．6 No．1 半枝莲粗提物对人肝脏细胞色素P450酶的影响 李卓 ，李幸曼。，王海云 ，李燕华 (1．广东省佛山市三水区人民医院，广‘东佛山 510055；2．广卅I医学院附属第 一 人民医院龙洞分院，广州 510520) 摘要：目的 研究半枝莲水相和乙醇相提取物对人细胞色素P450主要酶活性的影响，为半枝莲的开发和合理地临 床应用提供参考。方法 以咪哒唑仑、甲苯磺丁脲、咖啡因、氯唑沙完、异喹呱和试卤灵为探针药，用高效液相色 谱法分别测定不同提取溶质的半枝莲粗提物对人细胞色素P450主要酶活性的影响。结果 ①半枝莲粗提物对 CYP3A4、CYP2C9、CYP1A2、CYP1A1酶的活性呈现出剂量依赖性抑制作用。②半枝莲水相粗提物比乙醇相粗提 物对CYP1A1和CYP1A2酶的体外抑制作用强。结论 半枝莲水相提取物和乙醇相提取物是CYP3A4、CYP2C9、 CYP1A2、CYP1A1体外抑制剂。 关键词：半枝莲；细胞色素P450酶；高效液相色谱 中图分类号：R968 文献标识码：A 文章编号：1672 2981(2008)Ol一0053 03 Effect 0f crude extract of Scutellarla barbata D．Don on the activities of cytochrome P4 5 0 in human Liver microsomes LI Zhuo ，LI Xin—ming ，WANG Hal yun ，LI Yan hua (1．People s Hospital of Sanshui District。Foshan Guangdong 510055；2．The First iated Hospital of Guangzhou Medical College，Longdong Division，Guang zhou 510520) Abstract：Objective To investigate the effect of water and ethano1 extracts of Scutellarla barbata D．Don on the activi— ties of cytochrome P45O n human I iver microsomes．Methods Midazolam，E0R，caffeine，tolbutamide，chlorzoxa— zone。and debrisoquine were incubated as probes with or without Scutellariae barbatae respectively tO determine the effect of water extract and ethano1 extract of Scutellaria barbata on cytochrome P450 activities including CYP3A4． CYP1A1，CYP1A2，CYP2C9，CYP2E1．and CYP2D6 in human 1iver microsomes．Results ① Both water and etha no1 extracts of Scutellarla barbara D．Don inhibited the activities of CYPs(CYP3A4。CYP2C9。CYP1A2，and CYPIA1)in a concentration dependent manner．② Significant differences between the water and ethanol extracts of Scutellarla barbata D．Don were observed in CYP1A2 and CYP1A2．The water extract had stronger potentia1 ability tO inhibit the activities of the two enzymes than the