title: Synthesis of linear polyethylenimine derivatives for DNA transfection.
abstract: A series of linear polymers containing varying amounts of ethylenimine or N-propylethylenimine units were synthesized by hydrolysis and/or reduction of polyethyloxazolines. The pK(a)s of the polyamines were determined potentiometrically. Gel mobility shift assay showed that the efficiency of DNA complexation was related to the fraction of amino groups that are protonated at neutral pH. The effects of cationic charge density and molar weight of the polymers on the transfection efficiency were evaluated on HepG2 cells. The results obtained with different copolymers show that the transfection efficiency primarily depends on the fraction of ethylenimine units included in the polymer albeit the molar weight is also of importance. On the basis of the results obtained with poly(N-propylethylenimines), we also demonstrate that the high transfection efficiency of polyethylenimines does not solely rely on their capacity to capture protons which are transferred into the endo-lysosomes during acidification.
authors.affiliation: Laboratory Matériaux Polymères aux Interfaces, UMR CNRS 7581, University of Evry, Bld Mitterrand, 91025 Evry Cedex, France.
authors.forename: Blandine
authors.initials: B
authors.lastname: Brissault
authors.forename: Antoine
authors.initials: A
authors.lastname: Kichler
authors.forename: Christine
authors.initials: C
authors.lastname: Guis
authors.forename: Christian
authors.initials: C
authors.lastname: Leborgne
authors.forename: Olivier
authors.initials: O
authors.lastname: Danos
authors.forename: Hervé
authors.initials: H
authors.lastname: Cheradame
mesh_terms: D045744:Cell Line, Tumor; D004247:DNA / Q000032:analysis / Q000235:genetics*; D006801:Humans; D011094:Polyethyleneimine / Q000031:analogs & derivatives* / Q000032:analysis / Q000138:chemical synthesis*; D014162:Transfection / Q000379:methods*
chemical_list: D011094:Polyethyleneimine; D004247:DNA