顶端钠依赖性胆酸转运体及其抑制剂的研究进展

摘要

The enterohepatic circulation of bile acid plays a very important role in the absorption and metabolism of cholesterol and lipids. Apical sodium-dependent bile acid transporter (ASBT) promotes reabsorption of bile acid in the terminal ileum, and is very important in cholesterol metabolism. Pharmacological evidence showed that the inhibition of ASBT could reduce serum cholesterol and low density lipoprotein remarkably. ASBT is a new target for devoloping plasma cholesterol lowering drugs. In this paper, we describe the ASBT biological functions and features, and its inhibitors are reviewed.%胆汁酸的肠肝循环对于胆固醇及脂类的吸收和代谢具有极其重要的作用.顶端钠依赖性胆酸转运体(apical sodium-dependent bile acid transporter ASBT)主要表达在回肠壁腔侧膜上,负责肠道中绝大部分胆酸的重吸收,在胆固醇代谢中的地位非常重要.药理学试验证明抑制ASBT活性可以有效地降低血清胆固醇和低密度脂蛋白,因此ASBT可以作为降酯药物开发的新靶点.本文阐述了ASBT的生物学功能及特性,并对以ASBT为靶点的抑制剂进行了综述.