Dicationic lipophosphoramidates as DNA carriers.
Lipophosphoramidates with two different permanent cations as polar heads were synthesized and evaluated for their gene transfer activity. Physicochemical measurements (particle size, zeta potentials) and gel retardation assays were also performed. In vitro biological evaluation was conducted with A542 and HeLa cell lines, and cytotoxicity determined by a chemiluminescent assay. The set of results indicates that, on the whole, dicationic lipophosphoramidates constitute an interesting alternative to their monocationic analogues.
UMR CNRS 6521, Université de Bretagne Occidentale, UFR Sciences, 6, Avenue Le Gorgeu, CS 93837, F-29238 Brest cedex 3, France.
Mathieu
M
Mével
Tristan
T
Montier
François
F
Lamarche
Pascal
P
Delépine
Tony
T
Le Gall
Jean-Jacques
JJ
Yaouanc
Paul-Alain
PA
Jaffrès
Dominique
D
Cartier
Pierre
P
Lehn
Jean-Claude
JC
Clément
D000577:Amides / Q000138:chemical synthesis*; D000818:Animals; D002412:Cations; D045744:Cell Line, Tumor; D003601:Cytotoxicity Tests, Immunologic; D004247:DNA / Q000008:administration & dosage / Q000235:genetics / Q000378:metabolism*; D004337:Drug Carriers / Q000138:chemical synthesis*; D018014:Gene Transfer Techniques; D006367:HeLa Cells; D006801:Humans; D008163:Luminescent Measurements; D010743:Phospholipids / Q000138:chemical synthesis*; D063088:Phosphoramides; D010756:Phosphoric Acids / Q000138:chemical synthesis*; D013997:Time Factors
D000577:Amides; D002412:Cations; D004337:Drug Carriers; D010743:Phospholipids; D063088:Phosphoramides; D010756:Phosphoric Acids; C005438:phosphoramide; D004247:DNA