Cheno-, urso- and deoxycholic acid spermine conjugates: Relative binding affinities for calf thymus DNA

被引：37

作者：

Blagbrough, IS ^{[1
]}

Al-Hadithi, D ^{[1
]}

Geall, AJ ^{[1
]}

机构：

[1] Univ Bath, Dept Pharm & Pharmacol, Bath BA2 7AY, Avon, England

来源：

TETRAHEDRON | 2000年 / 56卷 / 21期

基金：

英国工程与自然科学研究理事会;

关键词：

polyamine amides; spermine; bile acids; DNA binding affinity; DNA condensation; lipoplex;

D O I：

10.1016/S0040-4020(00)00265-9

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Cationic lipid polyamine amides (cholan-24-amides) have been prepared from chenodeoxycholic (3 alpha,7 alpha-dihydroxy), ursodeoxycholic (3 alpha,7 beta-dihydroxy), and deoxycholic (3 alpha,12 alpha-dihydroxy) bile acids (5 beta-cholanes) by acylation of tri-Boc protected spermine. Their relative binding affinities for calf thymus DNA were determined using an ethidium bromide displacement assay. These lipopolyamine amides are synthetic vectors for non-viral gene delivery and models for lipoplex formation with respect to lipofection, a key first step in gene therapy. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：3439 / 3447

页数：9

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