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肝内胆汁瘀积是临床常见病、多发病,其形成机制十分复杂。熊脱氧胆酸和奥贝胆酸是目前FDA批准的仅有的2个用于治疗胆汁瘀积的药物。法尼醇X受体(FXR)是胆汁酸合成和转运的关键调节因子,其高表达对于维持胆汁酸的内环境稳态、降低胆汁酸对肝脏的毒性具有重要意义。中药可以通过多靶点、多途径发挥作用,针对主要发病机制的同时,兼顾次要发病机制,相互协同,在治疗肝内胆汁瘀积方面疗效显著。多种中药及其提取物或有效成分被证明能够通过激活FXR靶点而发挥保肝利胆作用,引起国内外广泛关注。对胆汁酸的体内代谢过程和FXR在肝内胆汁瘀积治疗中的作用进行概述,总结了基于调控FXR的中药治疗肝内胆汁瘀积的研究进展,以期为中药新药的开发提供参考。
Intrahepatic cholestasis is a common clinical disease, frequently-occurring disease, the formation mechanism is very complicated. Ursodeoxycholic acid and acornic acid are the only 2 drugs currently approved by the FDA for the treatment of cholestasis. Farnesol X receptor (FXR) is a key regulator of bile acid synthesis and transport, and its high expression is important for maintaining the homeostasis of bile acids and reducing the toxicity of bile acids to the liver. Traditional Chinese medicine can play a role through multiple targets and multiple pathways. It is effective in treating intrahepatic cholestasis due to its main pathogenesis, taking into account the secondary pathogenesis and mutual cooperation. A variety of traditional Chinese medicine and its extracts or active ingredients have been shown to activate liver and gallbladder through the activation of FXR targets, causing widespread concern at home and abroad. This review summarizes the metabolic processes of bile acids in vivo and the role of FXR in the treatment of intrahepatic cholestasis, and summarizes the research progress of the treatment of intrahepatic cholestasis by traditional Chinese medicine on the basis of the regulation of FXR in order to provide a reference for the development of new drugs in traditional Chinese medicine.