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Abstract
The antitumor activity of a novel synthetic chalcone derivative, 2′-hydroxy-2,4,6′-trimethoxychalcone (1H3MC), was evaluated using the multi-drug-resistant human uterine sarcoma MES-SA/Dx5 cells. Treatment with 1H3MC reduced P-glycoprotein expression in a time-dependent manner and inhibited MES-SA/Dx5 cell proliferation. Cisplatin alone had no effect on cell viability, but combined treatment with cisplatin and 1H3MC exhibited synergistic cytotoxicity. Furthermore, the combination of cisplatin and 1H3MC synergistically cleaved both caspase-3 and its substrate protein, poly(ADP-ribose) polymerase, which resulted in the fragmentation of genomic DNA, a hallmark of apoptosis. These results suggest that 1H3MC is a promising adjuvant agent for overcoming P-glycoprotein-mediated multi-drug resistance in cancer cells.
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1 Konkuk University, Department of Biological Sciences, College of Biological Science and Biotechnology, Cancer and Metabolism Institute, Seoul, Republic of Korea (GRID:grid.258676.8) (ISNI:0000000405328339)
2 University of California, Division of Biological Sciences, Biology w/Spec Bioinformatics, Revelle College, San Diego, USA (GRID:grid.266100.3) (ISNI:0000000121074242)
3 Dongduk Women’s University, Department of Applied Chemistry, Seoul, Republic of Korea (GRID:grid.412059.b) (ISNI:0000000405325816)