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8375253 
Journal Article 
DNA condensation by bile acid conjugates of thermine and spermine 
Blagbrough, IS; Al-Hadithi, D; Geall, AJ 
1999 
Pharmaceutical Press 
5 
3 
139-144 
English 
DNA condensation was achieved with polyamine conjugates of bile acids. Spermine and thermine, linear tetraamines, were mono-acylated on a primary amine with cholic and lithocholic acids. The resulting polyamine amides were triamines containing either a propyl-butyl or a dipropyl spacing. Thus, the former mimics both the positive charge and its regiochemical distribution found in the natural product spermidine. Calf thymus DNA was extended by saturation with an intercalator, ethidium bromide. DNA binding affinity was then measured by fluorescence quenching with detection of residual intercalated ethidium bromide at 600 nm. The results obtained with this exclusion assay show that polyamine lithocholic acid conjugates condense DNA more efficiently than the analogous cholic acid polyamine amides.