TACN-based cationic lipids with amino acid backbone and double tails: Materials for non-viral gene delivery

Cationic lipids have become an efficient type of non-viral vectors for gene delivery. In this Letter, four cationic lipids containing 1,4,7-triazacyclononane (TACN) headgroup, glutamic/aspartic acid backbone and dioleyl tails were designed and synthesized. The TACN headgroup gives these lipids excel...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-04, Vol.24 (7), p.1771-1775
Main Authors: Wang, Bing, Yi, Wen-Jing, Zhang, Ji, Zhang, Qin-Fang, Xun, Miao-Miao, Yu, Xiao-Qi
Format: Article
Language:English
Subjects:
Amino Acids - chemistry
Cationic lipids
Cations - chemistry
Cell Line, Tumor
Cell Survival - drug effects
DNA - chemistry
DNA - genetics
Gene delivery
Gene Transfer Techniques
Heterocyclic Compounds - chemistry
Humans
Lipids - chemical synthesis
Lipids - chemistry
Lipids - pharmacology
Molecular Structure
Particle Size
Plasmids
Structure-Activity Relationship
Transfection
Triazacyclononane
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Summary:Cationic lipids have become an efficient type of non-viral vectors for gene delivery. In this Letter, four cationic lipids containing 1,4,7-triazacyclononane (TACN) headgroup, glutamic/aspartic acid backbone and dioleyl tails were designed and synthesized. The TACN headgroup gives these lipids excellent pH buffering capacities, which were higher than branched 25kDa PEI. Cationic liposomes prepared from these lipids and DOPE showed good DNA affinity, and full DNA condensation was found at N/P ratio of 3 via agarose gel electrophoresis. The lipoplexes were characterized by dynamic light scattering (DLS) assay, which gave proper particle sizes and zeta-potentials for transfection. In vitro gene transfection results in two cell lines reveal that TAN (with aspartic acid and amide bond in the structure) shows the best transfection efficiency, which is close to commercially available transfection agent Lipofectamine 2000.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.02.034