Lipophosphoramidates as Lipidic Part of Lipospermines for Gene Delivery

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• 作者：Franç ; ois Lamarche ; Mathieu Mé ; vel ; Tristan Montier ; Laure Burel-Deschamps ; Philippe Giamarchi ; Rapha&euml ; l Tripier ; Pascal Delé ; pine ; Tony Le Gall ; Dominique Cartier ; Pierre Lehn
• 刊名：Bioconjugate Chemistry
• 出版年：2007
• 出版时间：September 2007
• 年：2007
• 卷：18
• 期：5
• 页码：1575 - 1582
• 全文大小：325K
• 年卷期：v.18,no.5(September 2007)
• ISSN：1520-4812

文摘

The DNA compacting properties of polyamines (especially spermine) are well-known, hence the use of spermineas 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. Physicochemicalmeasurements (particle size, zeta potentials, pK_a determination) and gel retardation assays were also performed.Theoretical membrane-disrupting ability was established by FRET. Taken together, our results indicate thatlipophosphoramidates constitute an interesting alternative to "classical" lipidic parts of cationic lipids used asDNA carriers.