Abstract
The interactions of synthetic and natural anthracyclines were studied by determination of binding constants to calf thymus DNA using spectrophotometric titration and thermal denaturation of drug-DNA solutions to determine the Tm values. The two ways of evaluation of DNA-drug interaction showed reasonable correlation. In particular, the glycosides with non-natural aglycones or major structural deviation showed consistently lower binding constants and Tm values. In the case of daunorubicin and 4-demethoxydaunorubicin these data also correlated reasonably with antitumor efficacy. However, in other instances, there were many deviations and a direct simple correlation between binding parameters and biological activity can not be established.
Keywords: DNA-drug binding constants, Anthraquinone, Daunosamine glycosides, DNA, Intercalation, Thermal denaturation, Melting points Tm
Current Bioactive Compounds
Title: Interaction of Natural and Synthetic Anthracyclines with DNA (Supporting Material)
Volume: 4 Issue: 3
Author(s): Karsten Krohn
Affiliation:
Keywords: DNA-drug binding constants, Anthraquinone, Daunosamine glycosides, DNA, Intercalation, Thermal denaturation, Melting points Tm
Abstract: The interactions of synthetic and natural anthracyclines were studied by determination of binding constants to calf thymus DNA using spectrophotometric titration and thermal denaturation of drug-DNA solutions to determine the Tm values. The two ways of evaluation of DNA-drug interaction showed reasonable correlation. In particular, the glycosides with non-natural aglycones or major structural deviation showed consistently lower binding constants and Tm values. In the case of daunorubicin and 4-demethoxydaunorubicin these data also correlated reasonably with antitumor efficacy. However, in other instances, there were many deviations and a direct simple correlation between binding parameters and biological activity can not be established.
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Cite this article as:
Krohn Karsten, Interaction of Natural and Synthetic Anthracyclines with DNA (Supporting Material), Current Bioactive Compounds 2008; 4 (3) . https://dx.doi.org/10.2174/157340708786305943
DOI https://dx.doi.org/10.2174/157340708786305943 |
Print ISSN 1573-4072 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6646 |
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