咖啡因探针法测定正常人肝脏药物代谢酶CYP1A2活性  

Determination of Activity of Drug-metabolizing Enzyme CYP1A2 in Livers of Healthy Adults by Caffeine Probe Method

作　　者：张鉴[1] 彭向前[1] 李军[1] 

机构地区：[1]山东省立医院临床药理中心,济南市250021

出　　处：《中国药房》2005年第16期1216-1218,共3页China Pharmacy

基　　金：山东省自然科学基金(Q99C05);山东省卫生厅科研项目(1998CA1DBB5)

摘　　要：目的:建立咖啡因4种主要代谢物含量的测定方法,探讨咖啡因代谢物在药物代谢酶CYP1A2活性评价中的意义。方法:采用反相高效液相梯度洗脱法测定尿液内咖啡因代谢产物5—乙酰氨基—6—甲酰氨基—3—甲基尿酸(AFMU)、1—甲基尿酸(1U)、1—甲基黄嘌呤(1X)和1,7—二甲基尿酸(17U)的相对含量,计算代谢物比率(AFMU+1X+1U)/17U,绘制频数分布直方图,评价CYP1A2活性。结果:受试者代谢物比率平均值为4.27,呈正态分布。结论:本方法简便、准确、快速,适合于尿液中咖啡因代谢物的测定及CYP1A2活性的研究。OBJECTIVE： To establish a method for the determination of 4 major caffeine metabolites and to discuss the significance of which in the evaluation of the activity of drug - metabolizing enzyme CYPIA2. METHODS： The caffeine metabolites in the urine like 5- acetylamino- 6- formamido- 3- methyluric acid （AFMU）, 1- methyluric acid（1U），1-methylxanthine（1X） and 1， 7-dimethyluricacid（17U） were determined by RP-HPLC gradient elution method, the ratios of metabolins（AFMU ＋ 1X ＋ 1U）/ 17U was calculated， the frequency distribution histogram was drawn and the activity of CYP1A2 was evaluated. RESULTS： The mean value of the ratio of the metabolins in the subjects was 4.27, which was in normal distribution， CONCLUSION： The method is simple，accurate and rapid, which is suitable for the determination of caffeine metabolites in urine and the study of the activities of CYP1A2。

关 键 词：咖啡因 代谢物 高效液相色谱法 CYP1A2 探针法 

分 类 号：R969.1[医药卫生—药理学]