trans-2-Aminocyclohexanol-based amphiphiles as highly efficient helper lipids for gene delivery by lipoplexes
Document Type
Article
Publication Title
Biochimica et Biophysica Acta (BBA) - Biomembranes
Department
Chemistry
ISSN
0005-2736
Volume
1848
Issue
12
DOI
10.1016/j.bbamem.2015.08.021
First Page
3113
Last Page
3125
Publication Date
12-1-2015
Abstract
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.
Recommended Citation
Zheng, Y.,
Liu, X.,
Samoshina, N. M.,
Samoshin, V. V.,
Franz, A. H.,
&
Guo, X.
(2015).
trans-2-Aminocyclohexanol-based amphiphiles as highly efficient helper lipids for gene delivery by lipoplexes.
Biochimica et Biophysica Acta (BBA) - Biomembranes, 1848(12), 3113–3125.
DOI: 10.1016/j.bbamem.2015.08.021
https://scholarlycommons.pacific.edu/cop-facarticles/123
