基于二相代谢酶探讨何首乌肝毒性风险及其发生机制  

Discussion on the Risk and Mechanism of Polygonum Multiflorum HepatotoxicityBased on the Two-phase Metabolic Enzyme UGT1A1

作　　者：逄瑜 汪祺[2] PANG Yu;WANG Qi(Center for Drug Reevaluation,NMPA,Beijing 100022,China;National Institutes for Food and Drug control,Beijing 100050,China)

机构地区：[1]国家药品监督管理局药品评价中心,北京100022 [2]中国食品药品检定研究院,北京100050

出　　处：《中国药物评价》2021年第4期284-287,共4页Chinese Journal of Drug Evaluation

基　　金：国家自然基金(基于何首乌固有肝毒性假说的物质基础及肝毒性作用机制研究81773874)。

摘　　要：基于二相代谢酶阐释何首乌的毒性作用机制,结合临床报道与文献研究,推测何首乌致肝毒性作用机制是由于服用何首乌后,其中的蒽醌、蒽酮类原型成分堆积,抑制了胆红素代谢酶UGT1A1酶的活性,使胆红素代谢受阻蓄积引起中毒;二相代谢酶UGT1A1为何首乌的主要作用靶点,蒽醌、蒽酮类成分为潜在的肝毒性成分。In this study we aimed to elucidate the toxic mechanism and potential toxic components of Polygonum multiflorum(P.M.)based on biphasic metabolic enzyme UGT1A1.Combined with clinical reports and literature research,speculated the mechanism of hepatotoxicity induced by P.M.was due to the accumulation of anthraquinone prototypes in P.M.after administration,which would inhibit the UGT1A1 enzyme activity.That could result in the accumulation of bilirubin metabolism induced hepatotoxicity.We speculated the UGT1A1 enzyme was the main target of P.M.and the anthraquinones were the main potential hepatotoxic components.

关 键 词：何首乌 肝毒性 UGT1A1酶 蒽醌 

分 类 号：R994.13[医药卫生—毒理学]