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Cytotoxic Effect of Chalcone Derivatives in MCF-7 Human Breast Cancer and HT-1080 Human Fibrosarcoma Cells  

Kang, You-Ra (College of Pharmacy and Department of Yeungnam University)
Park, Min-A (College of Pharmacy and Department of Yeungnam University)
Cho, Mi-Yeon (College of Pharmacy and Department of Yeungnam University)
Lee, Kyung-Hee (Food and Nutrition, Yeungnam University)
Kim, Jung-Ae (College of Pharmacy and Department of Yeungnam University)
Publication Information
YAKHAK HOEJI / v.54, no.1, 2010 , pp. 27-31 More about this Journal
Abstract
Xanthohumol, a prenylated chalcone of the Hop plant (Humulus lupulus L.), has been reported to suppress tumor growth. 4-hydroxychalcone and isobavachalcone are chalcone derivatives and they have similar structure with xanthohumol. In the present study, we investigated the cytotoxic activities of chalcone and its derivatives, 4-hydroxychalcone, xanthohumol, and isobavachalcone, in MCF-7 and adriamycin resistant MCF-7 (MCF-7/ADR) breast cancer cells and HT-1080 fibrosarcoma cells. In a cell viability assay using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) reagent, chalcone and 4-hydroxychalcone decreased cell viability in HT-1080 cells, but not in MCF-7 and MCF-7/ADR cells. Isobavachalcone showed similar cytotoxicity in HT-1080 cells, and only limited cytotoxicity in MCF-7 and MCF-7/ADR cells at very high concentration (50 ${\mu}M$). In contrast, xanthohumol showed concentration-dependent cytotoxicity in MCF-7, MCF-7/ADR, and HT-1080 cancer cells. Taken together, the structure-activity relationship of chalcone and its derivatives indicate that chalcones may be valuable cytotoxic compounds against selective cancer types.
Keywords
chalcone; 4-hydroxychalcone; xanthohumol; isobavachalcone;
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