银杏叶片对人药物代谢酶CYP1A2与NAT_2活性的影响  

Effect of Ginkgo Biloba Tablets on Activity of Cytochrome P_(450)1A2 and N-acetyltransferase 2 in Human

作　　者：卢新建 张鉴[2] 初建设 翟蕾 

机构地区：[1]山东省淄博市齐鲁石化中心医院药剂科,255400 [2]山东省立医院临床药理中心,济南250021

出　　处：《医药导报》2009年第12期1540-1542,共3页Herald of Medicine

摘　　要：目的探讨银杏叶片对人肝脏药物代谢酶CYP1A2和N-乙酰基转移酶(NAT2)活性的影响,预测银杏叶片与常用药物的相互作用,指导临床合理用药。方法以咖啡因作为药物代谢酶CYP1A2、NAT2的探针药物,以反相高效液相梯度洗脱法测定30例受试者服用银杏叶前后尿液内咖啡因5种主要代谢物的相对含量,采用代谢物的比值分别评价人肝脏药物代谢酶CYP1A2、NAT2活性的变化。结果受试者服药前CYP1A2、NAT2平均活性分别为2.976±1.428,0.447±0.172;服用银杏叶片28 d后CYP1A2、NAT2平均活性分别为3.021±1.318,0.391±0.147;服药前后CYP1A2的活性差异无显著性,NAT2的活性差异有显著性。结论银杏叶片对人药物代谢酶CYP1A2活性无明显影响,但是对NAT2的活性有明显影响;银杏叶片可能不会影响其他经CYP1A2酶代谢的药物临床疗效,但是可以影响与之合用经NAT代谢的药物临床疗效。Objective To investigate the effect of ginkgo biloba tablets on activiy of cytochrome P450 1A2 （CYP1A2） and N-acetyltransferase 2 （ NAT2 ） in human and to forecast the drug-drug interaction and instruct clinic rational administration of it. Methods Caffeine was used as a metabolic probe for CYP1A2 、 NAT2, before and after administration of ginkgo biloba tablets. Five major metabolites of caffeine in the urine of 30 volunteers were determined by RP-HPLC method and then evaluated to detect the activity change of CYP1A2 and NAT2 by the ratio of metabolites. Results It was found that the average activity of CYP1A2、NAT2 were 2. 976 ± 1. 428, 0. 447 ± 0. 172 and 3. 021 ± 1. 318,0. 391 ± 0. 147 before treatment and 28 days after treatment, respectively. There was no statistical significance on CYP1A2, but on NAT2. Conclusion Ginkgo biloba tablets has no influence on CYP1A2 activity, but the NAT2. They may not modify the efficacy of drugs which metabolized by CYP1A2, but can impact the effects of drugs whieh metabolized by NAT2.

关 键 词：银杏叶片 咖啡因 细胞色素P4501A2 N-乙酰基转移酶 

分 类 号：R286[医药卫生—中药学] R285[医药卫生—中医学]