以咖啡因为代谢探针测定细胞色素P450 CYP2A6活性  

Determination of the activity of cytochrome P-450 CYP2A6 by HPLC method with caffeine as metabolizing probe

作　　者：李军[1] 彭向前[2] 张鉴[1] 徐济萍[1] 

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：《药学学报》2006年第3期282-284,共3页Acta Pharmaceutica Sinica

基　　金：山东省自然科学基金资助项目(Q99C05).

摘　　要：Aim To establish a HPLC method for determining five major metabolites of caffeine in the urine,5-acetylamino-6-formylamino-3-methyluracil(AFMU),1-methylxanthine(1X),1-methyluric acid(1U),1,7-dimethyluric acid(17U) and 1,7-dimethylxanthine(17X) and assess the activity of cytochrome P-450 CYP2A6.Methods The contents of five major metabolites of caffeine in the urine were determined by RP-HPLC method.Frequency distribution histogram was drawn by calculating the 17U/(AFMU+1X+1U+17X+17U) and then evaluated the activity of CYP2A6.Results The frequency distribution histograms of CYP2A6 approximately indicated three distinct groups,the cut of point is 0.23 between fast metabolizer and intermediate type.And the cut of point is 0.15 between slow metabolizer and intermediate type.Conclusion The method is simple and rapid,suitable for the determination of metabolites of caffeine in urine.The method can be used to assay the activity of CYP2A6.Aim To establish a HPLC method for determining five major metabolites of caffeine in the urine, 5-aeetylamino-6-formylamino-3-methyluracil （ AFMU ） , 1 -methylxanthine （ 1X）, 1 -methyluric acid （1U）, 1,7-dimethyluric acid （17U） and 1,7-dimethylxanthine （17X） and assess the activity of cytochrome P-450 CYP2A6. Methods The contents of five major metabolites of caffeine in the urine were determined by RP-HPLC method. Frequency distribution histogram was drawn by calculating the 17U/ （AFMU ＋ 1X ＋ 1U ＋ 17X ＋ 17U） and then evaluated the activity of CYP2A6. Results The frequency distribution histograms of CYP2A6 approximately indicated three distinct groups, the cut of point is O. 23 between fast metabolizer and intermediate type. And the cut of point is O. 15 between slow metabolizer and intermediate type. Conclusion The method is simple and rapid, suitable for the determination of metabolitcs of caffeine in urine. The method can be used to assay the activity of CYP2A6.

关 键 词：咖啡因代谢物 高效液相色谱法 细胞色素P450 CYP2A6 

分 类 号：R968.1[医药卫生—药理学]