Department of Pharmaceutical Sciences, Oregon State University , 203 Pharmacy Building, Corvallis, Oregon 97331-4003, United States.
Laboratory of Chemical Genomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School Xili , Nanshan District, Shenzhen 518055, China.
Org Lett. 2016 Mar 18;18(6):1374-7. doi: 10.1021/acs.orglett.6b00308. Epub 2016 Feb 25.
Recollection of the tunicate source of the mandelalides has provided new and known analogues that have facilitated expanded analyses of the disputed cancer cytotoxicity of mandelalide A following a number of recent reported total syntheses. Using newly characterized mandelalide E, reisolated natural mandelalides B and C, and synthetic mandelalide A, the cytotoxicity of the mandelalides is demonstrated to be strongly influenced by compound glycosylation and assay cell density. Glycosylated mandelalides reduced the viability of human cancer cells cultured at a high starting density with a rank order of potency A > B ≫ E, yet display dramatically reduced cytotoxic efficacy against low density cultures.
短指软珊瑚来源的曼德林类化合物的重现为曼德林 A 的有争议的抗癌细胞毒性提供了新的和已知的类似物,这些类似物促进了在最近报道的许多全合成之后对其进行了扩展分析。使用新表征的曼德林 E、重新分离的天然曼德林 B 和 C 以及合成的曼德林 A,证明曼德林类化合物的细胞毒性强烈受化合物糖基化和测定细胞密度的影响。糖基化的曼德林类化合物降低了高起始密度培养的人癌细胞的活力,其效力顺序为 A > B > > E,但对低密度培养物的细胞毒性作用显著降低。