法尼醇X受体激动剂作为心脏代谢疾病的治疗靶点

Farnesoid X Receptor Agonists as Therapeutic Target for Cardiometabolic Diseases.

作者信息

Li Chao, Yang Jie, Wang Yu, Qi Yingzi, Yang Wenqing, Li Yunlun

机构信息

Experimental Center, Shandong University of Traditional Chinese Medicine, Jinan, China.

Cardiovascular Department, Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, China.

出版信息

Front Pharmacol. 2020 Aug 26;11:1247. doi: 10.3389/fphar.2020.01247. eCollection 2020.

Abstract

Cardiometabolic diseases are characterized as a combination of multiple risk factors for cardiovascular disease (CVD) and metabolic diseases including diabetes mellitus and dyslipidemia. Cardiometabolic diseases are closely associated with cell glucose and lipid metabolism, inflammatory response and mitochondrial function. Farnesoid X Receptor (FXR), a metabolic nuclear receptor, are found to be activated by primary BAs such as chenodeoxycholic acid (CDCA), cholic acid (CA) and synthetic agonists such as obeticholic acid (OCA). FXR plays crucial roles in regulating cholesterol homeostasis, lipid metabolism, glucose metabolism, and intestinal microorganism. Recently, emerging evidence suggests that FXR agonists are functional for metabolic syndrome and cardiovascular diseases and are considered as a potential therapeutic agent. This review will discuss the pathological mechanism of cardiometabolic disease and reviews the potential mechanisms of FXR agonists in the treatment of cardiometabolic disease.

摘要

心脏代谢疾病的特征是心血管疾病(CVD)的多种风险因素与包括糖尿病和血脂异常在内的代谢疾病相结合。心脏代谢疾病与细胞葡萄糖和脂质代谢、炎症反应及线粒体功能密切相关。法尼酯X受体(FXR)是一种代谢性核受体,被发现可被鹅去氧胆酸(CDCA)、胆酸(CA)等初级胆汁酸以及奥贝胆酸(OCA)等合成激动剂激活。FXR在调节胆固醇稳态、脂质代谢、葡萄糖代谢及肠道微生物方面发挥着关键作用。最近,新出现的证据表明,FXR激动剂对代谢综合征和心血管疾病具有作用,被认为是一种潜在的治疗药物。本综述将讨论心脏代谢疾病的病理机制,并综述FXR激动剂治疗心脏代谢疾病的潜在机制。

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