Prenylflavone derivatives from Broussonetia papyrifera,inhibit the growth of breast cancer cells in vitro and in vivo |
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Authors: | Fujiang Guo Li Feng Cheng Huang Hongxia Ding Xintian Zhang Zhaoyi Wang Yiming Li |
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Institution: | 1. School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, PR China;2. Shenogen Pharma Group Ltd., Suite A205, No. 5 Shangdi Kaituo Road, Haidian, Beijing 100085, PR China;3. Department of Medical Microbiology and Immunology, Creighton University Medical School, 2500 California Plaza, Omaha, NE 68178, USA |
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Abstract: | Two new prenylflavones 5,7,3′,4′-tetrahydroxy-3-methoxy-8-geranylflavone (1) and 5,7,3′,4′-tetrahydroxy-3-methoxy-8,5′-diprenylflavone (2), as well as four known ones, uralenol (3), papyriflavonol A (4), broussoflavonol B (5) and broussochalcone A (6) were isolated and purified from an ethyl acetate-soluble extract of the barks of Broussonetia papyrifera. Their structures were determined with the spectroscopic methods including HR-EI-MS, 1D and 2D NMR. We found that compounds 2–6 showed potent anti-proliferation effects on ER-positive breast cancer MCF-7 cells in vitro. The IC50 values of compounds 2 and 5 were 4.41 and 4.19 μM respectively after the treatment of 72 h. We also found that compounds 2 and 5 strongly down-regulated expression concentrations of estrogen receptor-α (ER-α) and were able to inhibit tumor growth in a xenograft model of the human breast cancer line BCAP-37 in vivo. Our results demonstrated that prenylflavones from B. Papyrifera exhibit potent anti-tumor activity. |
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Keywords: | Prenylflavone Breast cancer Growth inhibition ER-α36 |
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