法尼醇X受体天然激动剂的研究进展

Research progress on natural agonists of Farnesoid X receptor

关键词:  法尼醇X受体  胆汁酸受体  天然激动剂

Key words:  Farnesoid X receptor  bile acid receptor  natural agonist

摘要:

法尼醇X受体（Farnesoid X receptor，FXR），又称胆汁酸受体，因与代谢调节密切相关，FXR激动剂目前成为代谢性疾病治疗的药物研发热点。FXR天然激动剂来源广泛且大部分具有无或低毒副作用的特点，主要分为动物源性激动剂、植物源性激动剂和微生物源性激动剂三大类。动物源性激动剂包括鹅脱氧胆酸、胆酸、脱氧胆酸、石胆酸和熊去氧胆酸等内源性胆汁酸，以及雄甾酮；植物源性激动剂包括植物和植物提取物，如泽泻提取物、咖啡醇、香豆雌酚、葡萄内脂和薯蓣皂苷；微生物源性激动剂包括细格菌素。本文就FXR天然激动剂的研究进展进行综述。

Abstract:

Due to the significant association of Farnesoid X receptor (FXR) with metabolic regulation, FXR agonists have become a hotspot for drug research and development in the treatment of metabolic diseases. FXR natural agonists have a wide range of sources and most of them have the characteristics of no or low side effects. They are mainly divided into three categories:animal-derived agonists, plant-derived agonists and microbial-derived agonists. Animal-derived agonists include endogenous bile acids such as chenodeoxycholic acid, cholic acid, deoxycholic acid, lithocholic acid and ursodeoxycholic acid as well as androsterone; plant-derived agonists include plants and plant extracts, such as Alisma extract, caffeol, couestrol, grape lactone and dioscin; microbial-derived agonists include serotonin. This article reviews the research progress of FXR natural agonists.