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Bioorg Med Chem Lett. 2014 Apr 1;24(7):1771-5. doi: 10.1016/j.bmcl.2014.02.034. Epub 2014 Feb 22.

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

Author information

1
Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu 610064, PR China.
2
Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu 610064, PR China. Electronic address: ji_zhang@163.com.
3
Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu 610064, PR China. Electronic address: xqyu@scu.edu.cn.

Abstract

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 25 kDa 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.

KEYWORDS:

Cationic lipids; Gene delivery; Transfection; Triazacyclononane

PMID:
24618298
DOI:
10.1016/j.bmcl.2014.02.034
[Indexed for MEDLINE]

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