Design, Synthesis, and inVitro Transfection Biology of Novel Tocopherol Based Monocationic Lipids: A Structure−Activity Investigation

摘要: Herein, we report on the design, synthesis, and in vitro gene delivery efficacies of five novel tocopherol based cationic lipids (1−5) transfecting CHO, B16F10, A-549, HepG2 cells. The transfer efficiencies were evaluated by both β-galactosidase reporter expression inverted fluorescent microscopic experiments. results present structure−activity investigation convincingly demonstrate that lipid with three hydroxyl groups its headgroup region showed 4-fold better transfection efficiency than commercial formulation. also these may be targeted to liver. Transfection all relevant was maintained even when serum during conditions. indicated designed systems are quite capable transferring DNA into four types cells studied low or no toxicity.