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- Title
- Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species
- Author(s)
- N T Dat; X Jin; Kyeong Lee; Young-Soo Hong; Y H Kim; Jung Joon Lee
- Bibliographic Citation
- Journal of Natural Products, vol. 72, no. 1, pp. 39-43
- Publication Year
- 2009
- Abstract
- 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-arylbenzofuran-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-1α 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.
- ISSN
- 0163-3864
- Publisher
- Amer Chem Soc
- DOI
- http://dx.doi.org/10.1021/np800491u
- Type
- Article
- Appears in Collections:
- Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
- Files in This Item:
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