Wang Ming, Sun Shuo, Alberti Kyle A, Xu Qiaobing
ACS Synth Biol. 2012 Sep 21;1(9):403-7. doi: 10.1021/sb300023h. Epub 2012 Jun 13.
A combinatorial library of unsaturated lipidoids was synthesized through the Michael addition of amines to oleyl acrylamide. Their capability in facilitating in vitro gene delivery was evaluated by transfecting HeLa cells with EGFP-encoding plasmid DNA and mRNA. The preliminary screening results indicated that lipidoids with unsaturated oleyl tails are superior transfection agents compared to saturated lipidoids with n-octadecyl tails under the same conditions. The different transfection abilities of the unsaturated and saturated lipidioids were ascribed to the large, tightly packed lipoplexes of saturated lipidoids. The potential applications of the library of lipidoids were further expanded by looking at their ability to transfect fibroblasts as well as different cancerous cell lines.
通过胺与油酰丙烯酰胺的迈克尔加成反应合成了不饱和类脂的组合文库。通过用编码增强绿色荧光蛋白(EGFP)的质粒DNA和mRNA转染HeLa细胞,评估了它们在促进体外基因递送方面的能力。初步筛选结果表明,在相同条件下,具有不饱和油酰尾部的类脂比具有正十八烷基尾部的饱和类脂是更优异的转染剂。不饱和类脂和饱和类脂不同的转染能力归因于饱和类脂形成的大的、紧密堆积的脂质体复合物。通过研究它们转染成纤维细胞以及不同癌细胞系的能力,进一步拓展了类脂文库的潜在应用。