不同结构型熊果酸衍生物在抗肿瘤方面的研究进展

熊果酸是一种植物中常见的五环三萜类活性产物,具有广谱且显著的的抗肿瘤活性,但是较差的水溶性限制了其作为抗癌药物的应用。因此,对熊果酸的结构母核进行适当的修饰,引入特殊的药效基团,以改善其临床应用的局限性,成为了当前人们研究的热点。本综述总结了近10年来报道的具有抗肿瘤活性的熊果酸的各种合成衍生物,以探究不同基团修饰对抗肿瘤活性的影响,为研究熊果酸抗肿瘤方面的构效关系提供参考。

Research progress in anti-tumor effects of different structural types of ursolic acid derivatives

Ursolic acid is a common pentacyclic triterpenoid active product in plants, with broad-spectrum and significant anti-tumor activity. However, its poor water solubility limits its application as an anticancer drug. Therefore, appropriate modification of the structural matrices of ursolic acid and introduction of special pharmacodynamic moieties to improve the limitations of its clinical applications have become a hot topic of current research. This review summarizes various synthetic derivatives of ursolic acid with anti-tumor activity reported in the last 10 years to explore the effects of different group modifications on anti-tumor activity and provide a reference for studying the structure-activity relationship of ursolic acid in anti-tumor aspects.