Polycationic Telomers and Cotelomers for Gene Transfer: Synthesis and Evaluation of Their an Vitro Transfection Efficiency

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• 作者：Nathalie Van Craynest ; Catherine Santaella ; Otmane Boussif ; and Pierre Vierling
• 刊名：Bioconjugate Chemistry
• 出版年：2002
• 出版时间：January 2002
• 年：2002
• 卷：13
• 期：1
• 页码：59 - 75
• 全文大小：739K
• 年卷期：v.13,no.1(January 2002)
• ISSN：1520-4812

文摘

We report on the synthesis of a series of lipopolyamine telomers, [I(Asp)-14,n_A(NH), I(His)-18,n_A(NH),I-18,n_B(NMe), Gal-n_A(NH)], and random cotelomers, [I-18,n_A(NH)-n_B(NMe) and I-18,n_A(NH)-n_C(OH)],and on their in vitro gene transfer capability. They were obtained by a telomerization process of variousamino-acrylamide taxogens with various lipophilic thiol telogens which might also contain an asparticor a histidine residue or with a thiogalactosyle derivative. For N/P ratios (N = number of (co)telomeramine equivalents, P = number of DNA phosphates) from 0.8 to 10, these polyamine (co)telomerscondensed DNA, with or without the use of DOPE, forming (co)teloplexes of mean sizes less than 200nm, except for N/P 1.25 for which precipitates were observed. Some trends, structure-transfectionefficiency relationships, were established. Thus, aspartic-containing telomers were found to lead toefficient formulations for plasmid delivery to A549 cells and for N/P ratios from 1.25 to 5.