依泽替米贝通过 ABCG8 功能刺激粪便中性固醇排泄。
Ezetimibe stimulates faecal neutral sterol excretion depending on abcg8 function in mice.
机构信息
Department of Vascular Medicine, University of Amsterdam, Amsterdam, The Netherlands.
出版信息
FEBS Lett. 2010 Aug 20;584(16):3625-8. doi: 10.1016/j.febslet.2010.07.035. Epub 2010 Jul 24.
Ezetimibe stimulates faecal neutral sterol (FNS) excretion in mice, which cannot be explained by cholesterol absorption inhibition alone. We investigated whether these effects are mediated via the sterol exporter ATP binding cassette transporter G8 (abcg8). Ezetimibe increased FNS excretion 2.7-fold in WT mice and 1.5-fold in abcg8(-/-) mice, without affecting biliary cholesterol secretion. Daily FNS excretion exceeded the sum of dietary cholesterol intake and biliary secretion by about 60%. Ezetimibe enhanced this 'extra' FNS excretion by 3.5-fold and 1.5-fold in wildtype (WT) and abcg8(-/-) mice, respectively. Ezetimibe stimulates fecal sterol excretion of non-biliary and non-dietary origin, probably through stimulation of trans-intestinal cholesterol excretion. We show that this effect depends on intact abcg8 function.
依折麦布刺激小鼠粪便中性固醇（FNS）排泄，这不能仅用胆固醇吸收抑制来解释。我们研究了这些作用是否通过固醇外排 ABC 转运体 G8（abcg8）介导。依折麦布使 WT 小鼠 FNS 排泄增加 2.7 倍，使 abcg8(-/-) 小鼠增加 1.5 倍，而不影响胆汁胆固醇分泌。每日 FNS 排泄量超过饮食胆固醇摄入和胆汁分泌的总和约 60%。依折麦布分别使野生型（WT）和 abcg8(-/-) 小鼠的“额外”FNS 排泄增加 3.5 倍和 1.5 倍。依折麦布刺激非胆汁和非饮食来源的粪便固醇排泄，可能通过刺激跨肠胆固醇排泄。我们表明，这种作用取决于完整的 abcg8 功能。
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