Comparative Cytotoxicity of Artemisinin and Cisplatin and Their Interactions with Chlorogenic Acids in MCF7 Breast Cancer Cells

In parts of Africa and Asia, self‐medication with a hot water infusion of Artemisia annua (Artemisia tea) is a common practice for a number of ailments including malaria and cancer. In our earlier work, such an extract showed better potency than artemisinin alone against both chloroquine‐sensitive a...

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Veröffentlicht in:ChemMedChem 2014-12, Vol.9 (12), p.2791-2797
Hauptverfasser: Suberu, John O., Romero-Canelón, Isolda, Sullivan, Neil, Lapkin, Alexei A., Barker, Guy C.
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Sprache:eng
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Zusammenfassung:In parts of Africa and Asia, self‐medication with a hot water infusion of Artemisia annua (Artemisia tea) is a common practice for a number of ailments including malaria and cancer. In our earlier work, such an extract showed better potency than artemisinin alone against both chloroquine‐sensitive and ‐resistant parasites. In this study, in vitro tests of the infusion in MCF7 cells showed high IC50 values (>200 μM). The combination of artemisinin and 3‐caffeoylquinic acid (3CA), two major components in the extract, was strongly antagonistic and gave a near total loss of cytotoxicity for artemisinin. We observed that the interaction of 3CAs with another cytotoxic compound, cisplatin, showed potentiation of activity by 2.5‐fold. The chelation of cellular iron by 3CA is hypothesized as a possible explanation for the loss of artemisinin activity. Ironing out the infusion: Strong antagonistic interactions between artemisinin and chlorogenic acids in MCF7 cells has negative implications for the use of Artemisia tea in chemotherapy. It is possible that the chlorogenic acids present sap artemisinin of its potency by chelating cellular iron.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.201402285