Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.
Basic Information
ID: ALA1151479
Journal: J Nat Prod
Title: Hypoxia-inducible factor-1 inhibitory benzofurans and chalcone-derived diels-alder adducts from Morus species.
Authors: Dat NT, Jin X, Lee K, Hong YS, Kim YH, Lee JJ.
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-1alpha 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.
CiteXplore: 19072214
DOI: 10.1021/np800491u
Patent ID: ┄