Investigational Medicinal Chemistry and Pharmacology 2018; 1(1):2
Abstract
Background: Cancer chemotherapy is challenged by drug resistance of malignant cells. In the present work, we evaluated the cytotoxicity of four catechin derivatives, 4’-methylepigallocatechin (1), gallocatechin (2), epigallocatechin (3), epigallocatechin-3-O-gallate (4) against nine drug sensitive and multidrug resistant (MDR) cancer cell lines.
Methods: The resazurin reduction assay was used to evaluate the cytotoxicity of the compounds.
Results: Catechin derivatives 1-4 displayed selective cytotoxic effect with IC50 values below 90 µM on the leukemia CCRF-CEM cells and it drug resistant subline CEM/ADR5000. In contrast, no IC50 values could be measured in all 7 carcinoma cell lines tested. CEM/ADR5000 cells were much more cross-resistant to doxorubicin than to compounds 1-4.
Conclusions: Hence, the four compounds may serve as lead drugs for further derivatization and can be explored in more details for their possible use to treat leukemia.
Keywords: catechin; cytotoxicity; epigallocatechin-3-O-gallate; multidrug resistance; leukemia.
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