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Cyclen‐Based Cationic Lipids Containing Carbamate Linkages as Efficient Gene Delivery Vectors with Low Toxicity
Author(s) -
Huang QingDong,
Ren Jiang,
Chen Hong,
Ou WenJing,
Zhang Ji,
Fu Yun,
Zhu Wen,
Yu XiaoQi
Publication year - 2012
Publication title -
chempluschem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.801
H-Index - 61
ISSN - 2192-6506
DOI - 10.1002/cplu.201200060
Subject(s) - cationic polymerization , gene delivery , transfection , cyclen , cationic liposome , lipofectamine , chemistry , liposome , ethidium bromide , amphiphile , cytotoxicity , biophysics , combinatorial chemistry , biochemistry , in vitro , organic chemistry , dna , biology , gene , polymer , copolymer , vector (molecular biology) , recombinant dna
Two novel cationic lipids based on protonated cyclen and steroid (cholesterol or diosgenin) moieties with carbamate linkage have been designed and synthesized for gene delivery. Cationic liposomes were easily prepared from each of these lipids individually or from the mixtures of each cationic lipid and dioleoylphosphatidyl ethanolamine (DOPE). Several studies including dynamic light scattering, gel retardation assay, ethidium bromide intercalation assay, and transmission electron microscopy (TEM) imaging demonstrate that these amphiphilic molecules are able to bind and compact DNA into nanoparticles which may act as nonviral gene delivery agents. Results from in vitro transfection show that in association with (DOPE), two cationic lipids can induce effective gene transfection in HEK 293, A549, and H460 cells. Especially, in tumor cells (A549 and H460), the gene transfection efficiency of two cationic lipids were found to be higher than that of commercially available Lipofectamine 2000. The lipoplexes formed from both cationic lipids were found to have low cytotoxicity in three cell lines even at high N/P ratios.