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胆汁酸核受体FXR在胆汁淤积及其药物治疗中的研究进展
引用本文:徐俐洁,蒋思达,季晖,李婷婷,胡庆华. 胆汁酸核受体FXR在胆汁淤积及其药物治疗中的研究进展[J]. 药学研究, 2018, 37(3): 169-173
作者姓名:徐俐洁  蒋思达  季晖  李婷婷  胡庆华
作者单位:1.中国药科大学药学院,江苏 南京 210009,2.南京市第二十九中学,江苏 南京 210000,1.中国药科大学药学院,江苏 南京 210009,1.中国药科大学药学院,江苏 南京 210009,1.中国药科大学药学院,江苏 南京 210009
基金项目:国家自然科学基金(No.81503150)
摘    要:体内胆汁在生理状况下以肝肠循环的方式处于动态平衡中,而胆汁合成或流动障碍将导致胆汁淤积。胆汁的重要组成之一是胆汁酸,法尼酯X受体(Farnesoid X receptor, FXR)等核受体能通过调控胆汁酸合成代谢酶和胆汁酸转运蛋白调节胆汁酸的合成、转运和代谢等过程。FXR是研究治疗胆汁淤积的靶点之一,除了奥贝胆酸等上市药物外,一些传统保肝利胆的中药提取物也有调控FXR的作用。本文综述了近年来以FXR在胆汁淤积中的作用以及以FXR为靶点的胆汁淤积治疗药物研究进展。

关 键 词:胆汁酸;胆汁淤积;法尼酯X受体

Role of bile acid nuclear receptor FXR in cholestasis and related pharmacotherapy
XU Lijie,JIANG Sid,JI Hui,LI Tingting and HU Qinghua. Role of bile acid nuclear receptor FXR in cholestasis and related pharmacotherapy[J]. Journal of Pharmaceutical Research, 2018, 37(3): 169-173
Authors:XU Lijie  JIANG Sid  JI Hui  LI Tingting  HU Qinghua
Affiliation:1.School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China;2.Nanjing NO.29 High School,Nanjing 210000,China,1.School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China;2.Nanjing NO.29 High School,Nanjing 210000,China,1.School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China;2.Nanjing NO.29 High School,Nanjing 210000,China,1.School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China;2.Nanjing NO.29 High School,Nanjing 210000,China and 1.School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China;2.Nanjing NO.29 High School,Nanjing 210000,China
Abstract:In physiological conditions, bile is dynamically balanced by the enterohepatic circulation in the humans, whereas bile synthesis dysfunction or bile flow disturbance can cause cholestasis.One of the important component of bile is bile acid and nuclear receptors such as Farnesoid X receptor (Farnesoid X receptor,FXR) can regulate the process of bile acid synthesis,transport and metabolism through the regulation of bile acid metabolic enzymes,synthetic enzymes and bile acid transporters.FXR is one of the targets on the treatment of cholestasis.In addition to the listed drugs such as Obeticholic acid,some traditional Chinese medicines with hepatic protection and choleretic effects could also regulate FXR.This review discussed the role of FXR in cholestasis and the progress on the therapeutic drugs of FXR as target for the treatment of cholestatic.
Keywords:Bile acid  Cholestasis  Farnesoid X receptor
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