五环三萜羽扇豆烷型天然产物抗肿瘤活性研究进展

天然产物是抗肿瘤药物的重要来源。三萜化合物是植物体内重要的次生代谢产物，具有广泛的生物活性，其中五环三萜羽扇豆烷型天然产物对多种肿瘤细胞生长均表现出很强地抑制活性，同时由于毒性较低且作用机制独特，使其成为优秀的抗肿瘤先导化合物。近年来，针对羽扇豆烷型天然产物的抗肿瘤机制研究越发深入，对其结构进行衍生化从而提升活性、改善成药性的研究也越来越多。本文综述了五环三萜中白桦酸、23-羟基白桦酸、桦木醇和羽扇豆醇4个天然活性化合物的来源、抗肿瘤活性、作用机制及结构衍生化等方面国内外的研究进展。

Advances in Research on Lupane-Type-Pentacyclic Triterpenes and Their Anti-tumor Activities

Natural products have been the important and productive source of leading compounds for the development of anti-tumor agents. Naturally occurring triterpenoid saponins are generally plant-derived secondary metabolites, they provide valuable pharmacological properties. Lupane-type pentacyclic triterpenes have broad spectrum of anticancer activity and low toxicity. As a result, lupane-type pentacyclic triterpenes are good lead compounds for the development of anti-cancer agents. In recent years, increasing researches focused on the anti-tumor mechanisms and modifications to improve the pharmacological activity and druggability of lupine-type pentacyclic triterpenes have been conducted. This review focuses on the recent research on the source, anti-tumor activities, mechanisms and modification based on the four specific lupine-type compounds: betulinic acid, 23-hydroxybetulinic acid, betulin and lupeol.