.咖啡因体内代谢及其应用的研究进展.pdf

·256 · 生理科学进展 20 10 年第 4 1卷第 4 期 咖啡因体内代谢及其应用的研究进展 陈　尧 　周宏灏 △ (中南大学临床药理研究所 , 长沙 4 10078) 摘要 　咖啡因是从茶叶、咖啡果中提取出来的一种生物碱 ,常用于治疗神经衰弱和昏迷复苏 。咖啡 因体内代谢过程复杂 ,现已发现咖啡因的 15种代谢产物 ,参与代谢过程的酶类也被逐一证实 。尿 ( ) 液咖啡因代谢产物比率 UCMR s 常用于多种药物代谢酶活性的评估 ,主要包括 CYP1A2、CYP2A 6、 N 乙酰转移酶和黄嘌呤氧化酶 ,咖啡因及其代谢产物检测方法也逐步得到改进与更新 。总之 ,咖啡 因与人类健康密切相关 , 以及其重要的科研应用价值 ,一直受到普遍关注 。 关键词 　咖啡因; 药物代谢 ; 代谢酶 中图分类号 　R969 Progress in the Re search of Caffe ine M etabolism and Its A pplica tion in V ivo　CHEN Yao, ZHOU HongH ao ( Ins titu te of C lin ica l P ha rm acology, Cen tra l S ou th Un ivers ity, Changsha 4 10078, Ch ina) A b stract　Caffeine, a k ind of alkalo id, extracted from tea and coffee fru it, is common ly u sed in the treatm en t of neu ra sthen ia and for com a recovery. The m etabo lic p roce ss of caffeine in vivo is comp lex. F ifteen k ind s of m etabo lite s have been found, and the enzym e s invo lved in the m etabo lic p roce sse s have also been confirm ed. The u rinary caffeine m etabo lite s ratio s are common ly u sed in the a sse ssm en t of ac tivitie s of drug m etabo lizing enzym e s, m ain ly including CYP 1A2 , CYP2A 6 , N acetyltran sfera se and xan th ine oxida se. M ethod s for detection of caffeine and its m etabo lite s have been imp roved steep ly. In b rief, caffeine ha s been p aid clo se atten tion due to its in tim ate connection w ith hum an health a s well a s its im portance in app lication in scien tific re search. Key words　caffeine; drug m etabo lism ; m etabo lic enzym e s ( ) [ 2 ] 　　咖啡因 caffeine 是从茶叶、咖啡果中提取出来 精神药品范