Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 12, Issue 21, Pages 3484-3492Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ob00384e
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Funding
- National Program on Key Basic Research Project of China (973 Program) [2012CB720603, 2013CB328900]
- National Science Foundation of China [21232005, 51133004, J1310008, J1103315]
- Specialized Research Fund for the Doctoral Program of Higher Education in China [20120181130006]
- Program for New Century Excellent Talents in University [NCET-11-0354]
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A series of novel 1,4,7,10-tetraazacyclododecane (cyclen)-based cationic lipids with asymmetric double hydrophobic tails (cholesteryl and long aliphatic chains) were designed and synthesized. Lysine was chosen as a linking moiety in the molecular backbone. The liposomes formed from 8 and dioleoylphos-phatidylethanolamine (DOPE) could bind and condense plasmid DNA into nanoparticles under a low N/P ratio. These nano-scaled lipoplexes have low cytotoxicity, and might efficiently transfect A549 cells. In vitro transfection results revealed that all cationic lipids showed a comparable or better transfection efficiency (TE) than commercially available Lipofectamine 2000. The length and saturation degree of the aliphatic chain would affect their gene transfection performance, and the linoleic acid-containing 8e could give the best TE.
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