5种中药成份体外对羧酸酯酶活性及影响与研究.pdfVIP

5 种中药成份体外对羧酸酯酶活性的影响研究 1 1 1 2 1 1 张程亮 ，李喜平 ，徐艳娇 ，向道春 ，冯承阳 ，刘东 (1. 华中科技大学同济医学院附属同济医院药学部，湖北武汉 430030 ； 2. 武汉市中心医院药学部，湖北武汉430014) 摘要目的：初步考察5 种中药成份黄芩苷、穿心莲内酯、橙皮苷、茶多酚及黄豆 苷元在体外对羧酸酯酶 1 （CES1 ）和羧酸酯酶 2 （CES2 ）活性的影响。方法： 采用 CES1、CES2 特异性探针咪达普利和伊立替康（CPT-11 ）及其代谢产物咪 达普利拉和SN-38，在大鼠肝微粒体孵育体系中初步考察上述5 种中药成份抑制 两种CESs 活性强度。结果：上述5 种中药成份在100 μM 浓度下对CES1、CES2 活性均无显著抑制作用（P 0.05 ）。结论：黄芩苷、穿心莲内酯、橙皮苷、茶 多酚及黄豆苷元在体外不影响CESs 活性，体内实验有待进一步开展。 关键词：中药单体；羧酸酯酶；咪达普利；伊立替康 Effect of 5 Chinese Herbal Medicinal Ingredients on the Acitivity of Carboxylesterase 1 and 2 in vitro 1 1 1 2 1 Zhang Chengliang , Li Xiping , Xu Yanjiao , Xiang Daochun , Feng Chenyang , Liu Dong1 (1.Department of Pharmacy, Tongji Hospital, Tongji Medical college, Huazhong University of Science and Technology, Wuhan 430030, Hubei; 2. Department of Pharmacy, the Central Hospital of Wuhan, Wuhan 430030, Hubei) ABSTRACT Objective: To evaluate the inhibitory effect of 5 Chinese herbal medicinal ingredients, baicalin, andrographolide, hesperidin, polyphenols, and daidzein, on carboxylesterase 1 (CES 1) and carboxylesterase 2 (CES2). Methods:Based on our previous methods determiningthe metabolites’ concentration of imidapril and CPT-11, imidaprilat and SN-38 in rat liver microsomes incubation system, which were index for the activity of CES1 and CES2respectively, we investigated the potential effect of above drugs on CES1 and CES2. Results:Compared with the control group, the activity of CES1 and CES2 were not significantly influenced by the above 5 Chinese herbal medicinal ingredients (P 0.05). Conclusion: Baicalin, andrographolide, hesperidin, polyphenols and daidzei