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Cationic Lipids Containing Cyclen and Ammonium Moieties as Gene Delivery Vectors
Author(s) -
Huang QingDong,
Ren Jiang,
Ou WenJing,
Fu Yun,
Cai MaoQiang,
Zhang Ji,
Zhu Wen,
Yu XiaoQi
Publication year - 2012
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2012.01355.x
Subject(s) - cationic polymerization , lipofectamine , transfection , gene delivery , cyclen , cationic liposome , ethidium bromide , chemistry , liposome , amphiphile , biochemistry , biophysics , dna , biology , stereochemistry , organic chemistry , gene , vector (molecular biology) , copolymer , recombinant dna , polymer
In this study, two novel cationic lipids containing protonated cyclen and quaternary ammonium moieties were designed and synthesized as non‐viral gene delivery vectors. The structures of the two lipids differ in their hydrophobic region (cholesterol or diosgenin). Cationic liposomes were easily prepared from the lipids individually or from the mixtures of each cationic lipid and dioleoylphosphatidylethanolamine. Several studies including DLS, gel retardation assay, and ethidium bromide intercalation assay suggest that these amphiphilic molecules are able to bind and compact DNA into nanometer particles which can be used as non‐viral gene delivery agents. Our results from in vitro transfection show that in association with dioleoylphosphatidylethanolamine, two cationic lipids can induce effective gene transfection in human embryonic kidney 293 cells, although the gene transfection efficiencies of two cationic lipids were found to be lower than that of lipofectamine 2000 TM . Besides, different cytotoxicity was found for two lipoplexes. This study demonstrates that the title cationic lipids have large potential to be efficient non‐viral gene vectors.