title: Novel cationic lipids possessing protonated cyclen and imidazolium salt for gene delivery.
abstract: In this study, two novel protonated cyclen and imidazolium salt-containing cationic lipids differing only in their hydrophobic region (cholesterol or diosgenin) 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 DLS, gel retardation assay, ethidium bromide intercalation assay, and TEM demonstrated that these amphiphilic molecules are able to bind and compact DNA into nanometer particles that could be used as non-viral gene delivery agents. Our results from in vitro transfection showed that in association with DOPE, two cationic lipids can induce effective gene transfection in HEK293 cells. Furthermore, the gene transfection efficiencies of two cationic lipids were dramatically increased in the presence of calcium ion (Ca(2+)). It is notable that the gene transfection abilities of two cationic lipids were maintained in the presence of 10% serum. 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 vector.
authors: Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, PR China.
authors: Qing-Dong
authors: QD
authors: Huang
authors: Wen-Jing
authors: WJ
authors: Ou
authors: Hong
authors: H
authors: Chen
authors: Zhi-Hua
authors: ZH
authors: Feng
authors: Jing-Yi
authors: JY
authors: Wang
authors: Ji
authors: J
authors: Zhang
authors: Wen
authors: W
authors: Zhu
authors: Xiao-Qi
authors: XQ
authors: Yu
mesh_terms: D002412:Cations / Q000138:chemical synthesis; D000080027:Cyclams; D004247:DNA / Q000737:chemistry; D004339:Drug Compounding; D016503:Drug Delivery Systems; D015316:Genetic Therapy / Q000379:methods*; D005822:Genetic Vectors; D057809:HEK293 Cells; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis*; D008055:Lipids / Q000138:chemical synthesis* / Q000737:chemistry; D008081:Liposomes / Q000737:chemistry*; D053758:Nanoparticles; D014162:Transfection
chemical_list: D002412:Cations; D000080027:Cyclams; D006571:Heterocyclic Compounds; D007093:Imidazoles; D008055:Lipids; D008081:Liposomes; D004247:DNA; C038072:cyclen