银杏叶提取物对细胞色素P450酶CYP1A2实验研究  

Eexrerimental study on the effect of Ginkgo biloba extract on cytochrome P450 isozymes CYP1A2

作　　者：赵立子[1] 马锦芳[1] 邓颖[1] 关溯[1] 陈杰[1] 黄民[1] 

机构地区：[1]中山大学临床药理研究所,广东广州510080

出　　处：《中国临床药理学杂志》2005年第2期122-125,共4页The Chinese Journal of Clinical Pharmacology

基　　金：广州市重大项目--创新药物药理毒理评价研究技术平台资助项目(2003Z2-E4071)

摘　　要：目的　研究银杏叶提取物对大鼠细胞色素P450酶CYP1A2活性的影响。方法　银杏叶提取物10, 100mg·kg-1 2个剂量,分别经1, 5, 10天灌胃处理大鼠,以未经处理者为对照组,测定CYP1A2的酶活性。同剂量灌胃处理10天后,再单次灌胃盐酸普萘洛尔10mg·kg-1,测定普萘洛尔和N-去异丙基普萘洛尔在大鼠体内的血药浓度。结果　银杏叶提取物处理后,大鼠肝微粒体的CYP1A2酶活性显著升高,且能显著降低普萘洛尔在大鼠体内的AUC和Cmax,使N-去异丙基普萘洛尔的AUC和Cmax显著升高。结论　银杏叶提取物能显著诱导大鼠CYP1A2的酶活性,并显著影响普萘洛尔及其代谢物在大鼠体内的血药浓度。故银杏叶提取物可能影响与之同时服用、经CYP1A2代谢的药物临床疗效。Objective To investigate the effect of Ginkgo biloba extract (GBE) on cytochrome P450 isozymes CYP1A2 activity in rat. Methods CYP1A2 dependent reaction was monitored in rats treated intragastric gavage with GBE 10 and 100 mg·kg -1 daily for 1, 5 and 10 days. The changes of plasma concentration of propranolol and N-desisopropylpropranolol were measured after single dose of propranolol hydrochloride. Results CYP1A2 activity in rat liver increased significantly after treatment with GBE. AUC and C max of propranolol decreased significantly, and that of N-desisopropylpropranolol increased significantly. Conclusion GBE induced CYP1A2 significantly and modified the plasma concentration of propranolol and N-desisopropylpropranolol, so GBE may modify the efficacy of drugs which metabolized by CYP1A2 taken simultaneously.

关 键 词：银杏叶提取物 细胞色素P450 盐酸普萘洛尔 液相色谱-质谱 

分 类 号：R969.2[医药卫生—药理学] R972.6[医药卫生—药学]