Squalenoyl Gemcitabine Monophosphate: Synthesis, Characterisation of Nanoassemblies and Biological Evaluation
作者:Joachim Caron、Elise Lepeltier、L. Harivardhan Reddy、Sinda Lepêtre-Mouelhi、Séverine Wack、Claudie Bourgaux、Patrick Couvreur、Didier Desmaële
DOI:10.1002/ejoc.201100036
日期:2011.5
Trialkylammonium 4-(N)-1,1',2-trisnor-squalenoylgemcitabine monophosphate (SQdFdC-MP) salts were prepared from 1,1',2-trisnor-squalenoylgemcitabine by phosphoramidite-type chemistry. This amphiphilic molecule self-assembled into nanoassemblies of about 100 nm in size in aqueous solutions. Cryo-TEM and small-angle X-ray scattering (SAXS) investigations revealed that SQdFdC-MP molecules self-organized
三烷基铵 4-(N)-1,1',2-trisnor-squalenoylgemcitabine monophosphate (SQdFdC-MP) 盐由 1,1',2-trisnor-squalenoylgemcitabine 通过亚磷酰胺型化学制备。这种两亲性分子在水溶液中自组装成大小约为 100 nm 的纳米组件。冷冻 TEM 和小角 X 射线散射 (SAXS) 研究表明 SQdFdC-MP 分子自组织成单层脂质体,膜厚约为 70 A。这种脂质体三烷基铵 SQdFdC-MP 制剂对白血病细胞显示出显着的抗癌活性. 这些结果表明带负电荷的核苷酸类似物的角鲨烯缀合物有效地渗透到肿瘤细胞中。此外,