摘要
小肠是口服药物的主要吸收器官,同时也是进行药物代谢的重要场所。小肠黏膜上皮细胞含有大量Ⅰ、Ⅱ药物代谢酶,其中以CYP450酶最为重要,参与众多药物的生物转化。小肠CYP450主要有CYP1A1、CYP2C9、CYP2C19、CYP2J2、CYP2D6、CYP3A6种同工酶,其中CYP3A和CYP2C在小肠中表达最高,分别约占CYP450总含量80%和16%。与肝脏相比,小肠CYP450酶活性及其表达更易受到外源性化合物影响。本文重点讨论小肠CYP450s活性与表达及其在药物代谢中的作用以及由CYP450s的诱导或抑制引起的药物相互作用。
The uptake of oral administered drugs primarily occurs in the small intestine,which also has the capability to metabolize drugs.Both phase I and phase II metabolic enzymes were expressed in the intestinal mucosa,and cytochromes P450（CYP450s） are the principle enzymes attributed to the biotransformation of drugs.CYP3A and CYP2C are the most abundant subfamilies,accounting for approximately 80% and 16% of total CYP450s in the intestine.Compared to the liver,the expression and activity of CYP450 enzymes in the intestine was susceptible to inducers or inhibitors,leading to drug-drug interaction.This article reviews the expression of CYP enzymes in small intestine and the role of the gut wall in CYP-mediated xenobiotic metabolism.Possible drug-drug interactions due to induction or inhibition of CYP enzymes in the small intestine are also addressed.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2010年第2期186-192,共7页
Journal of China Pharmaceutical University
关键词
CYP450酶
肠首过代谢
药物相互作用
药物代谢
cytochrome P450 intestinal first-pass metabolism drug interaction drug metabolism
