肝脏在药物的体内清除过程中具有重要作用,它不仅是药物代谢的主要场所,还控制着药物及其代谢物的胆汁排泄过程。转运体是控制细胞内外物质传输的一类功能性膜蛋白,其在肝脏有广泛表达,并能对药物进入肝细胞以及排泄至胆汁的过程进行调控,因而,对于肝脏清除过程具有重要作用。本文从肝脏中重要转运体的分布、功能以及底物选择性出发,对其在药物的肝脏清除中的作用、由其引起的药物药物相互作用以及重要转运体的基因多态性研究进行了综述。
Liver is regarded as one of the most important organs for drug clearance in the body,which mediates both the metabolism and biliary excretion of drugs.Transporters are a class of functional membrane proteins and control the movement of substances into or out of cells.Transporters,which are extensively expressed in the liver,play important roles in the drug hepatic disposition by regulating the uptake of drugs from blood into hepatocytes or the efflux of drugs and their metabolites into bile.In this review,the localization,functions and substrate selectivity of the major transporters in the liver will be summarized,and the impacts of these transporters on drug hepatic disposition,the potential drug-drug interactions as well as their genetic polymorphisms will also be reviewed.