Linear cyclen-based polyamine as a novel and efficient reagent in gene delivery.
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.
Xiang
Yong-Zhe
YZ
Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu, 610064, PR China.
Feng
Zhi-Hua
ZH
Zhang
Ji
J
Liao
Yi-Le
YL
Yu
Chuan-Jiang
CJ
Yi
Wen-Jing
WJ
Zhu
Wen
W
Yu
Xiao-Qi
XQ
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
D002021:Buffers; D000080027:Cyclams; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D011073:Polyamines; D004811:Epichlorohydrin; D004247:DNA; C038072:cyclen