咖啡因探针法测定正常人肝脏N-乙酰化转移酶活性  

Determination of Activity of N-acetyltransferase Using Caffeine as a Metabolic Probe①

作　　者：李军 [1] 彭向前 [2] 张鉴 [1] 徐济萍 [2] 

机构地区：[1]山东省立医院临床药理中心,山东,济南,250021 [2]山东大学药学院,山东,济南,250012

出　　处：《解放军药学学报》2005年第6期407-409,共3页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金：山东省自然科学基金;No.Q99C05

摘　　要：目的建立一套测定咖啡因的3种主要代谢物5乙酰氨基6甲酰氨基3甲基尿酸(AFMU)、1甲基黄嘌呤(1X)和1甲基尿酸(1U)的高效液相色谱法,探讨咖啡因代谢物在N乙酰化酶活性评价中的意义。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AFMU、1U和1X的相对含量,计算AFMU/(AFMU+1X+1U)比值,绘制概率分布直方图,确定正常人快、慢乙酰化代谢表型的截点(临界点)。结果受试者可明显划分为快乙酰化者和慢乙酰化者,快、慢乙酰化代谢表型的临界点为0.26,快、慢乙酰化表型之比73∶17。结论本方法简便、准确、快速,适合于尿中咖啡因代谢物的测定及N乙酰化转移酶活性的研究。Aim To establish a HPLC method for determining three major metabolites of caffeine, 5-acetylamino-6- formylamino-3-methyluracil（AFMU）, 1-methylxanthine（1X） and 1-methyluric acid（ 1 U） ,and evaluate the function of caffeine as a metabolic probe for acetylator phenotyping. Methods The contents of metabolites of caffeine in the urine was determined by RP-HPLC method. The acetylator＇ s status was phenotyped by measuring the AFMU/（AFMU ＋ 1X ＋ 1U）.Frequency distribution histograms were drawn to determine the slow and fast acetylate phenotype status among people. Resuits The frequence distribution histograms indicated two distinct groups, the cut of point is 0.26, the ratio of the fast acetylator to the slow acetylator was 73 ： 17. Conclusion The method is simple, accurate and quick, suitable for the determination of metabolites of caffeine in urine. The method is used to assay the activities of N-acetyltransferase.

关 键 词：咖啡因代谢物 高效液相色谱 N-乙酰化转移酶 多态性 代谢探针 

分 类 号：R969.1[医药卫生—药理学]