Antiproliferative Activity of Derivatives of Ouabain, Digoxin and Proscillaridin A in Human MCF-7 and MDA-MB-231 Breast Cancer Cells

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  • Winnicka Katarzyna
    Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Bialystok
  • Bielawski Krzysztof
    Department of Medicinal Chemistry and Drug Technology, Faculty of Pharmacy, Medical University of Bialystok
  • Bielawska Anna
    Department of Medicinal Chemistry and Drug Technology, Faculty of Pharmacy, Medical University of Bialystok
  • Surażyński Arkadiusz
    Department of Medicinal Chemistry and Drug Technology, Faculty of Pharmacy, Medical University of Bialystok

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Three derivatives of ouabain, digoxin and proscillaridin A containing the carboxylic group instead of the lactone moiety were synthesized and examined for cytotoxicity in human breast cancer cells. Evaluation of the cytotoxicity of these compounds employing an MTT assay and inhibition of [3H]thymidine incorporation into DNA in both MCF-7 and MDA-MB-231 breast cancer cells demonstrated that compound 3, the most active of the series, proved to be only slightly less potent than proscillaridin A. We evaluated the effects of these compounds 1—3 on change in intracellular Ca2+, appearance of apoptosis, inhibition of DNA topoisomerase I and II, and the activity of caspase-3 in breast cancer cells. These studies indicate that the increase in potency for 3 may be related, in part, to an activation of caspase-3, increasing free calcium concentration and topoisomerase II inhibition. All these data emphasize the potential usefulness of these derivatives of cardiac glycosides as anticancer agents.

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