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trans-2-Aminocyclohexanol-based amphiphiles as highly efficient helper lipids for gene delivery by lipoplexes
Biochimica et Biophysica Acta (BBA) - Biomembranes
  • Yu Zheng, University of the Pacific
  • Xin Liu, University of the Pacific
  • Nataliya M. Samoshina, University of the Pacific
  • Vyacheslav V. Samoshin, University of the Pacific
  • Andreas H. Franz, University of the Pacific
  • Xin Guo, University of the Pacific
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Lipidic amphiphiles equipped with the trans-2-aminocyclohexanol (TACH) moiety are promising pH-sensitive conformational switches (“flipids”) that can trigger a lipid bilayer perturbation in response to increased acidity. Because pH-sensitivity was shown to improve the efficiency of several gene delivery systems, we expected that such flipids could significantly enhance the gene transfection by lipoplexes. Thus a series of novel lipids with various TACH-based head groups and hydrocarbon tails were designed, prepared and incorporated into lipoplexes that contain the cationic lipid 1,2-dioleoyl-3-trimethylammonio-propane (DOTAP) and plasmid DNA encoding a luciferase gene. B16F1 and HeLa cells were transfected with such lipoplexes in both serum-free and serum-containing media. The lipoplexes consisting of TACH-lipids exhibited up to two orders of magnitude better transfection efficiency and yet similar toxicity compared to the ones with the conventional helper lipids 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) or cholesterol. Thus, the TACH-lipids can be used as novel helper lipids for efficient gene transfection with low cytotoxicity.
Citation Information
Yu Zheng, Xin Liu, Nataliya M. Samoshina, Vyacheslav V. Samoshin, et al.. "trans-2-Aminocyclohexanol-based amphiphiles as highly efficient helper lipids for gene delivery by lipoplexes" Biochimica et Biophysica Acta (BBA) - Biomembranes Vol. 1848 Iss. 12 (2015) p. 3113 - 3125 ISSN: 0005-2736
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