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目的:初步考察5种中药成分黄芩苷、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种中药成分抑制两种CESs活性强度。结果:上述5种中药成分在100μmol·L-1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。
OBJECTIVE: To investigate the effects of five traditional Chinese medicines baicalin, andrographolide, hesperidin, tea polyphenol and daidzein on the activities of carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) in vitro. Methods: The CES1 and CES2 specific probes were used to probe the effects of imidacloprid and irinotecan (CPT-11) and their metabolites imidaprilat and SN-38 on the rat liver microsomal incubation system Chinese medicine ingredients inhibit the activity of two CESs. Results: The five Chinese herbal ingredients showed no significant inhibitory effect on the activity of CES1 and CES2 at a concentration of 100μmol·L-1 (P <0.05). Conclusion: Baicalin, andrographolide, hesperidin, tea polyphenols and daidzein do not affect the activity of CESs in vitro. The in vivo experiments need to be further carried out.