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

Reference:

Blagbrough, I. S., Al-Hadithi, D. and Geall, A. J., 2000. Cheno-, urso- and deoxycholic acid spermine conjugates: Relative binding affinities for calf thymus DNA. Tetrahedron, 56 (21), pp. 3439-3447.

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Official URL:

http://dx.doi.org/10.1016/S0040-4020(00)00265-9

Abstract

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.

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