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肠胆酸受体是葡萄糖内稳态的关键调节因子。

Intestinal bile acid receptors are key regulators of glucose homeostasis.

机构信息

Institut National de la Santé et de la Recherche Médicale, U1048, Université Paul Sabatier, UPS, Institut des Maladies Métaboliques et Cardiovasculaires (I2MC),CHU Rangueil,1 Avenue Jean Poulhès,BP84225, 31432 Toulouse,Cedex 4,France.

University Lille, Inserm, Centre Hospitalier Universitaire de Lille, Institut Pasteur de Lille, U1011-European Genomic Institute for Diabetes,Lille,France.

出版信息

Proc Nutr Soc. 2017 Aug;76(3):192-202. doi: 10.1017/S0029665116002834. Epub 2016 Nov 16.

Abstract

In addition to their well-known function as dietary lipid detergents, bile acids have emerged as important signalling molecules that regulate energy homeostasis. Recent studies have highlighted that disrupted bile acid metabolism is associated with metabolism disorders such as dyslipidaemia, intestinal chronic inflammatory diseases and obesity. In particular, type 2 diabetes (T2D) is associated with quantitative and qualitative modifications in bile acid metabolism. Bile acids bind and modulate the activity of transmembrane and nuclear receptors (NR). Among these receptors, the G-protein-coupled bile acid receptor 1 (TGR5) and the NR farnesoid X receptor (FXR) are implicated in the regulation of bile acid, lipid, glucose and energy homeostasis. The role of these receptors in the intestine in energy metabolism regulation has been recently highlighted. More precisely, recent studies have shown that FXR is important for glucose homeostasis in particular in metabolic disorders such as T2D and obesity. This review highlights the growing importance of the bile acid receptors TGR5 and FXR in the intestine as key regulators of glucose metabolism and their potential as therapeutic targets.

摘要

除了作为膳食脂质清洁剂的众所周知的功能外,胆汁酸已成为调节能量平衡的重要信号分子。最近的研究强调,胆汁酸代谢紊乱与代谢紊乱有关,如血脂异常、肠道慢性炎症性疾病和肥胖症。特别是 2 型糖尿病(T2D)与胆汁酸代谢的定量和定性改变有关。胆汁酸结合并调节跨膜和核受体(NR)的活性。在这些受体中,G 蛋白偶联胆汁酸受体 1(TGR5)和核受体法尼醇 X 受体(FXR)参与调节胆汁酸、脂质、葡萄糖和能量平衡。这些受体在肠道中对能量代谢调节的作用最近得到了强调。更具体地说,最近的研究表明,FXR 对葡萄糖平衡特别重要,尤其是在代谢紊乱如 T2D 和肥胖症中。这篇综述强调了胆汁酸受体 TGR5 和 FXR 在肠道中作为葡萄糖代谢关键调节剂的重要性及其作为治疗靶点的潜力。

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