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  • Title: Lipophosphoramidates as lipidic part of lipospermines for gene delivery.
    Author: Lamarche F, Mével M, Montier T, Burel-Deschamps L, Giamarchi P, Tripier R, Delépine P, Le Gall T, Cartier D, Lehn P, Jaffrès PA, Clément JC.
    Journal: Bioconjug Chem; 2007; 18(5):1575-82. PubMed ID: 17676781.
    Abstract:
    The DNA compacting properties of polyamines (especially spermine) are well-known, hence the use of spermine as the cationic part in several synthetic DNA carriers. Here, we describe the synthesis of modified spermines, with a "lipophosphoramidate" as the lipidic part, and their use for efficient in vitro transfection. Physicochemical measurements (particle size, zeta potentials, pKa determination) and gel retardation assays were also performed. Theoretical membrane-disrupting ability was established by FRET. Taken together, our results indicate that lipophosphoramidates constitute an interesting alternative to "classical" lipidic parts of cationic lipids used as DNA carriers.
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