Journal
JOURNAL OF NATURAL PRODUCTS
Volume 72, Issue 1, Pages 39-43Publisher
AMER CHEMICAL SOC
DOI: 10.1021/np800491u
Keywords
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Funding
- Plant Diversity Research Center [PF06204-00]
- Molecular and Cellular BioDiscovery Research Program, Korea [M 1060100015]
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Hypoxia-inducible factor-1 (HIF-1) is the central mediator of cellular responses to low oxygen concentrations and vital to many aspects of cancer biology. Bioassay-guided fractionation of the chloroform-soluble extracts of Morus species using a hypoxia response element (HRE)-dependent reporter assay led to identification of six benzofurans (1-6) and two chalcone-derived Diels-Alder adducts (7, 8) from Mori Cortex Radicis and three prenylated benzofurans (9-11) and four chalcone-derived Diels-Alder adducts (12-15) from Morus bombycis. The structure of the new 2-arylben-zofuran-type compound, moracin Q (3), was elucidated by spectroscopic methods, and the absolute configuration of 2 was determined for the first time. The selected compounds (1-3, 5, 7, 9; 10, and 12) from the cell-based reporter assay were found to inhibit hypoxia-induced HIF-1 alpha accumulation in a dose-dependent manner in human hepatocelluar carcinoma cell-line Hep3B cells. Furthermore, these compounds were also active against hypoxia-induced vascular endothelial growth factor (VEGF) secretion in Hep3B cells.
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