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

Ian S Blagbrough, D Al-Hadithi, A J Geall

Research output: Contribution to journalArticlepeer-review

31 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)3439-3447
Number of pages9
JournalTetrahedron
Volume56
Issue number21
DOIs
Publication statusPublished - 2000

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