雷公藤甲素的不良反应及减毒研究进展

Research Progress on Toxicity and Attenuation of Triptolide

雷公藤甲素(TP)是从卫矛科植物雷公藤中分离出的一种环氧化二萜内酯化合物,是雷公藤的主要活性成分之一,具有免疫活性、抗炎、抗风湿和抗肿瘤作用。然而,TP水溶性差,体内消除快,高活性的TP可诱发多器官毒性,阻碍了其在临床中的应用。主要对近3年来TP在基础研究中的不良反应及机制,剂型及给药方式转换,配伍减毒等多方面进行整合归纳,以期为TP的毒性作用及减毒增效研究的深入探索提供参考。

Triptolide(TP),an epoxide diterpene lactone compound isolated from Leigongteng(Tripterygium wilfordii),is one of the main active components.TP has immunological activity,anti-inflammatory,anti-rheumatic and anti-tumor effects.However,TP has poor water solubility,fast elimination in vivo.Highly active TP can induce multi-organ toxicity,hindering the development of its preparations and its clinical application.This article mainly summarized its toxicities and mechanisms of TP in basic research in the past three years,such as the conversion of dosage forms,administration methods and compatibility attenuation,with a view to in-depth exploration of toxicity and attenuation of TP and enhancing efficiency research for reference.