Dramatic influence of the hydroxy functionality of azasugar moiety in the head group region of tocopherol-based cationic lipids on in vitro gene transfection efficacies

摘要: Cationic lipids have been effectively used as nonviral vectors for the delivery of polynucleic acids into cytosol. In particular, having hydroxy groups in head group region facilitate strong binding with negatively charged phosphate DNA via hydrogen bonding and electrostatic interactions and, thus regulate transfection efficiency. this regard, we designed synthesised two cationic lipids, namely, aza sugar group-based (Toc-Aza) non-aza sugar-based (Toc-Pyr) control lipid. A well-known co-lipid, 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) was to formulate liposomes lipoplexes, which were biophysically characterised hydrodynamic diameters, global surface charges, binding. Three cell lines, HEK-293, CHO, HepG2 viability assays vitro studies. studies revealed that lipid without hydroxyl on (pyrrolidine group) showed contrast efficacies at a 2 : 1 charge ratio all three lines studied. Toc-Aza almost 10-fold better activities than Toc-Pyr More importantly, 1.5-fold activity HEK-293 cells similar pattern efficiency CHO when compared commercially available Lipofectamine 2000. These findings improve knowledge their effects variation functional group.