School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan.
Molecules. 2020 Oct 27;25(21):4974. doi: 10.3390/molecules25214974.
Saponins are amphiphilic molecules consisting of carbohydrate and either triterpenoid or steroid aglycone moieties and are noted for their multiple biological activities-Fungicidal, antimicrobial, antiviral, anti-inflammatory, anticancer, antioxidant and immunomodulatory effects have all been observed. Saponins from natural sources have long been used in herbal and traditional medicines; however, the isolation of complexed saponins from nature is difficult and laborious, due to the scarce amount and structure heterogeneity. Chemical synthesis is considered a powerful tool to expand the structural diversity of saponin, leading to the discovery of promising compounds. This review focuses on recent developments in the structure optimization and biological evaluation of synthetic triterpenoid and steroid saponin derivatives. By summarizing the structure-activity relationship (SAR) results, we hope to provide the direction for future development of saponin-based bioactive compounds.
皂苷是由碳水化合物和三萜或甾体苷元部分组成的两亲性分子,具有多种生物学活性-已观察到杀菌、抗菌、抗病毒、抗炎、抗癌、抗氧化和免疫调节作用。天然来源的皂苷长期以来一直用于草药和传统药物中;然而,由于数量稀少和结构异质性,从自然界中分离复杂的皂苷是困难和费力的。化学合成被认为是扩展皂苷结构多样性的有力工具,导致发现有前途的化合物。本综述重点介绍了合成三萜和甾体皂苷衍生物的结构优化和生物学评价的最新进展。通过总结结构-活性关系(SAR)结果,我们希望为基于皂苷的生物活性化合物的未来发展提供方向。