Charge effect in the interaction of doxorubicin and derivatives with polydeoxynucleotides

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The equilibrium interaction of doxorubicin and its N-acetyl derivative with a series of purine-pyrimidine alternating polydeoxynucleotides has been studied through spectrofluorometry to assess the relevance of the electrostatic contribution to DNA intercalation. The results have shown that: (a) the suppression of the positive charge on the aminosugar has: (I) a profound negative effect on the free energy of intercalation, as expected, and (II) a negligible influence on the base specificity, which supports the notion of an essentially electrostatic effect of N-acetylation on intercalation; (b) a reasonably good accord with the demands of a polyelectrolytic model, due to Friedman and Manning, is found. © 1992.



Doxorubicin, Drug-DNA intercalation, Polyelectrolyte effect

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BBA - Gene Structure and Expression, v. 1129, n. 3, p. 294-302, 1992.