Wang Liming, Wang Zengshang, Su Sheng, Xing Ying, Li Yali, Li Ming, Liu Jiangyun, Yang Shilin
College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China; Key Lab of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China; Department of the VIP Internal Medicine, The First Affiliated Hospital of Xinjiang Medical University, Urumqi 830011, China.
Carbohydr Res. 2017 Apr 10;442:9-16. doi: 10.1016/j.carres.2017.02.010. Epub 2017 Feb 28.
An array of oleanolic acid-type saponins based on β-hederin has been synthesized in a linear or one-pot manner. The cell viability assays indicate that synthetic saponins show antiproliferation activities in three cancer cell lines with IC values of 2.4-15.1 μM and hederacolchiside A being the most potent. The results demonstrate that the type of terminal monosaccharides and linkage position have apparent effects on cytotoxicities and selectivities of these saponins against cancer cell lines tested. This study is helpful for future development of more potent anticancer leads.
基于β-常春藤皂苷元的一系列齐墩果酸型皂苷已通过线性或一锅法合成。细胞活力测定表明，合成皂苷在三种癌细胞系中显示出抗增殖活性，IC值为2.4-15.1 μM，其中常春藤皂苷元A的活性最强。结果表明，末端单糖的类型和连接位置对这些皂苷对所测试癌细胞系的细胞毒性和选择性有明显影响。该研究有助于未来开发更有效的抗癌先导物。
