银杏叶片对人药物代谢酶CYP2A6、XO和NAT2活性的影响  

Effect of ginkgo biloba tablets on Cytochrome P4502A6,XO and N-acetyltransferase 2 activity in human

作　　者：卢新建 张鉴[2] 初建设 

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

出　　处：《齐鲁药事》2009年第5期297-300,共4页qilu pharmaceutical affairs

摘　　要：目的探讨银杏叶片对人肝脏药物代谢酶CYP2A6、XO和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CYP2A6、XO和NAT2的探针药物,以反相高效液相梯度洗脱法测定30名受试者服用银杏叶前后人尿液内咖啡因5种主要代谢物的相对含量,采用代谢物的比率分别评价人肝脏药物代谢酶CYP2A6、XO和NAT2活性的变化.结果受试者服药前CYP2A6、XO和NAT2平均活性为0.227±0.076、0.723±0.060和0.447±0.172;服用银杏叶片28d后CYP2A6、XO和NAT2平均活性为0.227±0.072、0.728±0.074和0.391±0.147;服药前后酶CYP2A6、XO的活性无显著性差异,酶NAT2的活性有显著性差异.结论银杏叶片可能不会影响其他经CYP2A6、XO酶代谢的药物临床疗效,但是可以影响与之合用经NAT2代谢的药物临床疗效.OBJECTIVE To investigate the effect of ginkgo biloba tablets on Cytochrome P4502A6（CYP2A6） ,Xanthine oxidase（XO） ,N--acetyltransferase 2 （NAT2）activiy in human and to forecast the drug--drug interaction with it, so as to in- struct clinical to prescribe rationaUy. METHODS In thirty volunteers,use two way cross design,caffeine was used as a recta-bolic probe for CYP2A6, XO, NAT2, before and after ginkgo biloba tablets administration, urine samples were collected. The contents of five major metabolites of caffeine in the urine were determined by RP-- HPLC method and then evaluated the activi- ty change of CYP2A6,XO,NAT2 by the ratio of metabolites of caffeine. RESULTS It was found that the average activity of CYP2A6,XO,NAT2 were 0. 227±0. 076,0. 723±0. 060 and 0. 447±0. 172 with before treatment,and 28 days after treatment, the average activity of CYP2A6, XO, NAT2 were 0. 227 ±0. 072,0. 728±0. 074 and 0. 391±0. 147. There was no statistical sig- nificance on CYP2A6,XO,but has statistical significance on NAT2. CONCLUSION Ginkgo biloba tablets has no influence on CYP2A6,XO activity,but the NAT2 activity significantly impact,ginkgo biloba tablets may not modify the efficacy of drugs which metabolized by CYP2A6 and XO taken simultaneously,but can modify the efficacy of drugs which metabolized by NAT2.

关 键 词：银杏叶片 咖啡因代谢物 细胞色素P4502A6 黄嘌呤氧化酶 N-乙酰基转移酶2反相高效液相 

分 类 号：R285.6[医药卫生—中药学]