期刊
JOURNAL OF NATURAL PRODUCTS
卷 83, 期 5, 页码 1461-1472出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.9b01022
关键词
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资金
- Ministry of Science and Technology of Taiwan [MOST-108-2320-B-182-038-MY3, MOST-106-2320-B-182-017]
- Chang Gung Medical Research Program [BMRPC17, CMRPD1J0281]
- Intramural Research Program of the National Institutes of Health, National Cancer Institute, Center for Cancer Research
- NATIONAL CANCER INSTITUTE [ZIABC010030] Funding Source: NIH RePORTER
The overexpression of the ATP-binding cassette (ABC) transporter ABCG2 has been linked to clinical multidrug resistance in solid tumors and blood cancers, which remains a significant obstacle to successful cancer chemotherapy. For years, the potential modulatory effect of bioactive compounds derived from natural sources on ABCG2-mediated multidrug resistance has been investigated, as they are inherently well tolerated and offer a broad range of chemical scaffolds. Licochalcone A (LCA), a natural chalcone isolated from the root of Glycyrrhiza inf lata, is known to possess a broad spectrum of biological and pharmacological activities, including pro-apoptotic and antiproliferative effects in various cancer cell lines. In this study, the chemosensitization effect of LCA was examined in ABCG2-overexpressing multidrug-resistant cancer cells. Experimental data demonstrated that LCA inhibits the drug transport function of ABCG2 and reverses ABCG2-mediated multidrug resistance in human multidrug-resistant cancer cell lines in a concentration-dependent manner. Results of LCA-stimulated ABCG2 ATPase activity and the in silico docking analysis of LCA to the inward-open conformation of human ABCG2 suggest that LCA binds ABCG2 in the transmembrane substrate-binding pocket. This study provides evidence that LCA should be further evaluated as a modulator of ABCG2 in drug combination therapy trials against ABCG2-expressing drug-resistant tumors.
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