小肠胆固醇吸收的研究进展

胆固醇是生命活动必不可少的脂类物质,但当体内胆固醇水平过高时,就会引起高胆固醇血症,进而导致动脉粥样硬化、脑中风和冠心病。人体内胆固醇有两种来源:以乙酰辅酶A为原料从头合成,或者通过小肠从食物中吸收。现今,过量的胆固醇摄取是引起高胆固醇血症的重要原因。胆固醇在小肠中的吸收是一个复杂的、由多个步骤组成的连续的分解、转运以及重新酯化的过程。其中由Niemann-Pick C1 Like 1(NPC1L1)蛋白介导肠道中胆固醇进入吸收细胞,是胆固醇吸收的限速步骤。本文重点总结了小肠胆固醇吸收的分子途径、调控机制、医药研发现状及与low-density lipoprotein receptor(LDLR)内吞过程的比较。

The research perspective of intestinal cholesterol absorption

Cholesterol is an essential lipid with many physiological functions. High level of cholesterol is called hypercholesterolemia which is a major risk factor for atherosclerosis, stroke and heart disease. The humans obtain cholesterol through de novo synthesis from acetyl-CoA and intestinal absorption from food. In developed societies, excessive cholesterol absorption is an important reason of hypercholesterolemia. In- testinal cholesterol absorption is a sophisticated process including hydrolysis, transport and re-esterification. Niemann-Pick C1 Like 1 （NPC1L1） facilitates cholesterol entering enterocytes that is the rate-limiting step. This review summarizes the molecular pathway and regulation of intestinal cholesterol absorption, and devel- opment of cholesterol absorption inhibitors. The endocytosis of NPC 1 L 1 and low-density lipoprotein receptor （LDLR） is compared, too.