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DNA-binding parameters of daunorubicin and doxorubicin in the conditions used for studying the interaction of anthracycline-DNA complexes with cells in vitro

  • DNA-Binding Parameters
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Summary

Affinity constants of daunorubicin and doxorubicin for DNA at 37°C and in presence of 10% serum were determined by an optical method and calculated from Scatchard plots. Values from 0.10 to 0.12 and from 0.13 to 0.16x106 M−1 were obtained for daunorubicin and doxorubicin, respectively. According to these affinity constants, the amounts of free drugs were calculated for various concentrations of daunorubicin-DNA or doxorubicin-DNA and for various molar ratios. In a large range of concentrations there is rather stable concentration of both free drugs, and these concentrations are inversely proportional to the nucleotides/drug ratio.

The amount of free drug present in the medium is low as long as the concentration of daunorubicin-DNA or doxorubicin-DNA is higher than 1 μg/ml (expressed as drug concentration). At lower concentrations, however, the percentage of free drug increases very sharply.

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Abbreviations

DNR:

daunorubicin

DOX:

doxorubicin

D:

drug

D t :

total concentration of D

D f :

concentration of free D

(D-DNA) b :

concentration of D-DNA complex

DNA t :

total concentration of DNA nucleotides

DNA f :

concentration of free DNA nucleotides

FCS:

fetal calf serum

Ka :

affinity constant

NBCS:

newborn calf serum

PBS:

phosphate buffered saline

References

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Authors and Affiliations

  1. International Institute of Cellular and Molecular Pathology, 75, avenue Hippocrate, B-1200, Brussels, Belgium

    Y.-J. Schneider, R. Baurain, A. Zenebergh & A. Trouet

  2. Université Catholique de Louvain, 75, avenue Hippocrate, B-1200, Brussels, Belgium

    Y.-J. Schneider, R. Baurain, A. Zenebergh & A. Trouet

Authors
  1. Y.-J. Schneider
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  2. R. Baurain
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  3. A. Zenebergh
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  4. A. Trouet
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Schneider, YJ., Baurain, R., Zenebergh, A. et al. DNA-binding parameters of daunorubicin and doxorubicin in the conditions used for studying the interaction of anthracycline-DNA complexes with cells in vitro. Cancer Chemother. Pharmacol. 2, 7–10 (1979). https://doi.org/10.1007/BF00253097

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  • DOI: https://doi.org/10.1007/BF00253097

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