title: Linear cyclen-based polyamine as a novel and efficient reagent in gene delivery.
abstract: Linear cyclen-based polyamine (LCPA, M(w) = 7392, M(w)/M(n) = 1.19) as a novel non-viral gene vector was designed and synthesized from 1,7-diprotected 1,4,7,10-tetraazacyclododecane (cyclen), bis(beta-hydroxylethyl)amine and epichlorohydrin. Agarose gel retardation and fluorescent titration using ethidium bromide showed the good DNA-binding ability of LCPA. It could retard pDNA at an N/P ratio of 4 and form polyplexes with sizes around 250-300 nm from an N/P ratio of 10 to 60 and relatively lower zeta-potential values (< +3 mV) even at the N/P ratio of 60. The cytotoxicity of LCPA assayed by MTT is much lower than that of 25 kDa PEI. In vitro transfection against A549 and 293 cells showed that the transfection efficiency of LCPA/DNA polyplexes is close to that of 25 kDa PEI at an N/P ratio of 10-15, indicating that the new material could be a promising non-viral polycationic reagent for gene delivery.
authors.affiliation: Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, 610064, PR China.
authors.forename: Yong-Zhe
authors.initials: YZ
authors.lastname: Xiang
authors.forename: Zhi-Hua
authors.initials: ZH
authors.lastname: Feng
authors.forename: Ji
authors.initials: J
authors.lastname: Zhang
authors.forename: Yi-Le
authors.initials: YL
authors.lastname: Liao
authors.forename: Chuan-Jiang
authors.initials: CJ
authors.lastname: Yu
authors.forename: Wen-Jing
authors.initials: WJ
authors.lastname: Yi
authors.forename: Wen
authors.initials: W
authors.lastname: Zhu
authors.forename: Xiao-Qi
authors.initials: XQ
authors.lastname: Yu
mesh_terms: D002021:Buffers; D002460:Cell Line; D000080027:Cyclams; D004247:DNA / Q000378:metabolism; D004587:Electrophoresis, Agar Gel; D004811:Epichlorohydrin / Q000737:chemistry; D018014:Gene Transfer Techniques; D006571:Heterocyclic Compounds / Q000737:chemistry*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007202:Indicators and Reagents / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D010316:Particle Size; D010957:Plasmids / Q000235:genetics; D011073:Polyamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism* / Q000633:toxicity; D014162:Transfection
chemical_list: D002021:Buffers; D000080027:Cyclams; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D011073:Polyamines; D004811:Epichlorohydrin; D004247:DNA; C038072:cyclen