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Xanthohumol, a Prenylated Chalcone from Hops, Inhibits the Viability and Stemness of Doxorubicin-Resistant MCF-7/ADR Cells

Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China
State Key Laboratory of Biological Fermentation Engineering of Beer (In Preparation), Qingdao 266061, China
College of Food Science and Engineering, Jiangxi Agricultural University, Nanchang 330045, China
Key Laboratory of Marine Bioactive Substance, the First Institute of Oceanography, State Oceanic Administration, Qingdao 266061, China
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Molecules 2017, 22(1), 36;
Received: 14 November 2016 / Revised: 24 December 2016 / Accepted: 25 December 2016 / Published: 28 December 2016
Xanthohumol is a unique prenylated flavonoid in hops (Humulus lupulus L.) and beer. Xanthohumol has been shown to possess a variety of pharmacological activities. There is little research on its effect on doxorubicin-resistant breast cancer cells (MCF-7/ADR) and the cancer stem-like cells exiting in this cell line. In the present study, we investigate the effect of xanthohumol on the viability and stemness of MCF-7/ADR cells. Xanthohumol inhibits viability, induces apoptosis, and arrests the cell cycle of MCF-7/ADR cells in a dose-dependent manner; in addition, xanthohumol sensitizes the inhibition effect of doxorubicin on MCF-7/ADR cells. Interestingly, we also find that xanthohumol can reduce the stemness of MCF-7/ADR cells evidenced by the xanthohumol-induced decrease in the colony formation, the migration, the percentage of side population cells, the sphere formation, and the down-regulation of stemness-related biomarkers. These results demonstrate that xanthohumol is a promising compound targeting the doxorubicin resistant breast cancer cells and regulating their stemness, which, therefore, will be applied as a potential candidate for the development of a doxorubicin-resistant breast cancer agent and combination therapy of breast cancer. View Full-Text
Keywords: xanthohumol; doxorubicin resistance; viability; stemness xanthohumol; doxorubicin resistance; viability; stemness
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Liu, M.; Yin, H.; Qian, X.; Dong, J.; Qian, Z.; Miao, J. Xanthohumol, a Prenylated Chalcone from Hops, Inhibits the Viability and Stemness of Doxorubicin-Resistant MCF-7/ADR Cells. Molecules 2017, 22, 36.

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