Farnesoid X receptor regulators from natural products and their biological function.

Peng Wan, N I Hengfan, Guo Dale, Deng Yun, Dai Manyun
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Abstract

Metabolic syndrome (MetS) has been a growing public health concern worldwide without specific medicine. Through summarizing the chemical structure type and effect mechanisms of natural products targeted on farnesoid X receptor (FXR), to provide the research basis for exploring the treatment of MetS. The following databases were searched for natural products which targeting FXR: PubMed, Embase, the Cochrane Library, Web of Science, China National Knowledge Infrastructure Database, Wanfang Database, China Science and Technology Journal Database, and Chinese Biomedical Literature Database. Totally 120 natural products were summarized, including terpenoids (51 compounds), steroidal saponins (27 compounds), phenylpropanolds (19 compounds), flavonoids (13 compounds), alkaloids (3 compounds) and others (7 compounds), most researches focus on terpenoids and part of synthetic FXR regulators were based on the structure of terpenoids. FXR regulators could improve cholestasis and liver injury, hyperlipidemia, diabetes and atherosclerosis. FXR is a potential target of treating MetS. Natural products are characteristics with unique novel structures and special biological activity, and they are important sources of bioactive precursor compounds and drug discovery. Exploring the effects and mechanism of natural products and its derivative on MetS by targeting FXR may be a new way to develop the new drugs of treating MetS.

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Farnesoid X受体调节剂的天然产物及其生物学功能。
代谢综合征(MetS)已成为全球日益关注的公共卫生问题,目前尚无专门的药物。通过对farnesoid X受体(FXR)靶向天然产物的化学结构、类型及作用机制的综述,为探索MetS的治疗方法提供研究依据。针对FXR的天然产物检索数据库为PubMed、Embase、Cochrane图书馆、Web of Science、中国国家知识基础数据库、万方数据库、中国科技期刊数据库和中国生物医学文献数据库。综述了120种天然产物,其中萜类51种,甾体皂苷27种,苯丙醇19种,黄酮类13种,生物碱3种,其他7种,研究多集中在萜类上,部分合成的FXR调节剂是基于萜类的结构。FXR调节剂可改善胆汁淤积和肝损伤、高脂血症、糖尿病和动脉粥样硬化。FXR是治疗MetS的潜在靶点。天然产物具有独特新颖的结构和特殊的生物活性,是生物活性前体化合物和药物发现的重要来源。以FXR为靶点,探索天然产物及其衍生物对MetS的作用及其机制,可能是开发治疗MetS新药的新途径。
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