Hypoxia-Inducible Factor-1 Inhibitory Benzofurans and Chalcone-Derived Diels−Alder Adducts from Morus Species
Citations Over TimeTop 10% of 2008 papers
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.
Related Papers
- → Synthesis and Evaluation of Chalcone Derivatives as Novel Sunscreen Agent(2021)50 cited
- → Two New Hydroxy Chalcone Derivatives from Thymus cilicicus(2007)13 cited
- → Chalcone Ditosylates as Potent Precursor for Synthesis of Some 4,5-Disubstituted Isoxazoles with Antioxidant and Anti-inflammatory Activities(2019)2 cited
- → Molecular Docking Studies of Indolyl-Benzodioxyl-Chalcone, Pyrrolyl-Benzodioxyl- Chalcone, and Thiophenyl-Benzodioxyl-Chalcone as an Antimalarial Agent(2021)1 cited
- Relationship between Structure and SHG Effect of Substituted Thienyl Chalcone(1997)