| In vitro: |
| Phytochemistry Letters, 2013, 6(3):331-336. | | Prenylflavone derivatives from Broussonetia papyrifera, inhibit the growth of breast cancer cells in vitro and in vivo.[Reference: WebLink] |
METHODS AND RESULTS:
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.
CONCLUSIONS:
Our results demonstrated that prenylflavones from B. Papyrifera exhibit potent anti-tumor activity. |
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