雷公藤红素的抗肿瘤作用及结构改造研究进展

Progress on Anti-tumor Effects and Structural Modification of Celastrol

雷公藤红素是从中药雷公藤中分离得到的五环三萜类化合物,具有广泛的生物学活性,特别是抗肿瘤作用比较显著,但因其毒副作用大、水溶性差,受限于临床应用.笔者查阅了2009年-2018年以来国内外文献,对雷公藤红素抗肿瘤作用及其结构改造工作进行综述,旨在为进一步开展结构改造工作和抗肿瘤新药研发奠定基础.

Celastrol is a pentacyclic triterpenoid isolated from the traditional Chinese medicine Tripterygium wilfordii.It has a wide range of biological activities, especially the Anticancer effect.Although celastrol has important pharmacological activity, its poor water solubility and high toxicity restricts its application.After reviewing the domestic and foreign literatures from 2009 to 2018, the author reviewed the anti-tumor effect of Celastrol and its structural modification work.The purpose of this paper is to lay a foundation for further structural modification and the development of new anticancer drugs.