雷公藤红素药理活性与结构修饰研究进展

Research progress on pharmacological effects and structural modification of celastrol

雷公藤红素是一种天然的木栓烷型五环三萜,卫矛科植物雷公藤(Tripterygium wilfordii Hook.f.)的有效活性成分之一,具有多种药理活性,是目前广受关注的热点天然产物。天然产物及其衍生物是新药开发的重要来源,国内外研究者以雷公藤红素为母核进行大量化学结构修饰研究,并结合活性筛选,发现许多活性更为突出的候选化合物。本文通过对其药理活性和结构修饰的研究进展进行归纳总结,对进一步深入开展药理学研究,以及指导合成新的高效低毒的雷公藤红素衍生物具有重要意义。

Celastrol is one of the active ingredients in Tripterygium wilfordii Hook.f..It is a natural friedelane pentacyclic triterpene which possesses a variety of pharmacological activities.Natural products as well as their derivatives serve as important sources in discovery of new bioactive agents.Therefore,many studies via synthesizing the derivatives of celastrol to find some more bioactive candidate compounds have been carried out.In this paper,the recent research progress of pharmacological activity and structural modification of celastrol were critically reviewed,which was of great significance for its further pharmacological research,providing valuable guidance for the synthesis of new high-efficiency and low-toxicity celastrol derivatives.