期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 7, 页码 1771-1775出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.02.034
关键词
Triazacyclononane; Cationic lipids; Gene delivery; Transfection
资金
- National Program on Key Basic Research Project of China (973 Program) [2012CB720603]
- National Science Foundation of China [21232005, J1310008, J1103315]
- Specialized Research Fund for the Doctoral Program of Higher Education [20120181130006]
- Program for New Century Excellent Talents in University [NCET-11-0354]
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. (C) 2014 Elsevier Ltd. All rights reserved.
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