Grefhorst Aldo, Verkade Henkjan J, Groen Albert K
AMSTERDAM UNIVERSITY MEDICAL CENTERS, AMSTERDAM, THE NETHERLANDS.
UNIVERSITY MEDICAL CENTER GRONINGEN, UNIVERSITY OF GRONINGEN, GRONINGEN, THE NETHERLANDS.
Methodist Debakey Cardiovasc J. 2019 Jan-Mar;15(1):70-76. doi: 10.14797/mdcj-15-1-70.
Besides the well-known hepatobiliary pathway of cholesterol excretion into the feces, transintestinal cholesterol excretion (TICE) is a second major pathway through which cholesterol is disposed from the body. In the process of TICE, cholesterol is taken up from lipoprotein particles at the basolateral side of the enterocyte and translocates towards the apical side of the enterocyte. At the apical side, the ATP-binding cassette transporters G5 and G8 form a heterodimer that transports cholesterol into the intestinal lumen. A substantial amount of the secreted cholesterol is likely reabsorbed by the cholesterol influx transporter Niemann-Pick C1-Like 1 (NPC1L1) since recent data indicate that inhibition of NPC1L1 increases the efficacy of TICE for disposal of cholesterol via the feces. The pathways and proteins involved in intracellular cholesterol trafficking in the enterocyte have not yet been identified. Therefore, in addition to discussing known mediators of TICE, this review will also examine potential candidates involved in cholesterol translocation in the enterocyte. Both the cholesterol reuptake and efflux pathways can be influenced by pharmaceutical means; thus, the TICE pathway is a very attractive target to increase cholesterol excretion from the body and prevent or mitigate atherosclerotic cardiovascular disease.
除了众所周知的胆固醇经肝胆途径排泄至粪便外,经肠胆固醇排泄(TICE)是胆固醇从体内排出的第二条主要途径。在TICE过程中,胆固醇在肠上皮细胞基底外侧从脂蛋白颗粒摄取,并向肠上皮细胞顶端侧转运。在顶端侧,ATP结合盒转运体G5和G8形成异源二聚体,将胆固醇转运至肠腔。由于最近的数据表明抑制尼曼-皮克C1样1型(NPC1L1)胆固醇流入转运体可提高TICE经粪便排泄胆固醇的效率,因此大量分泌的胆固醇可能会被NPC1L1重新吸收。肠上皮细胞内胆固醇转运所涉及的途径和蛋白质尚未明确。因此,除了讨论已知的TICE介质外,本综述还将研究参与肠上皮细胞胆固醇转运的潜在候选物。胆固醇再摄取和流出途径均可受到药物手段的影响;因此,TICE途径是增加体内胆固醇排泄、预防或减轻动脉粥样硬化性心血管疾病的极具吸引力的靶点。