| Literature DB >> 20527891 |
Juma Hoshino1, Eun-Jung Park, Tamara P Kondratyuk, Laura Marler, John M Pezzuto, Richard B van Breemen, Shunyan Mo, Yongchao Li, Mark Cushman.
Abstract
Five resveratrol sulfate metabolites were synthesized and assessed for activities known to be mediated by resveratrol: inhibition of tumor necrosis factor (TNF) alpha induced NFkappaB activity, cylcooxygenases (COX-1 and COX-2), aromatase, nitric oxide production in endotoxin-stimulated macrophages, proliferation of KB or MCF7 cells, induction of quinone reductase 1 (QR1), accumulation in the sub-G(1) phase of the cell cycle, and quenching of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical. Two metabolites showed activity in these assays; the 3-sulfate exhibited QR1 induction, DPPH free radical scavenging, and COX-1 and COX-2 inhibitory activities and the 4'-sulfate inhibited NFkappaB induction, as well as COX-1 and COX-2 activities. Resveratrol and its 3'-sulfate and 4-sulfate inhibit NO production by NO scavenging and down-regulation of iNOS expression in RAW 264.7 cells. Resveratrol sulfates displayed low antiproliferative activity and negligible uptake in MCF7 cells.Entities:
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Year: 2010 PMID： 20527891 PMCID： PMC2917805 DOI： 10.1021/jm100274c
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446