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Chrysin is a natural, biologically active compound extracted from many plants, honey and propolis. It possesses potent anti-inflammation, anti-cancer and anti-oxidation properties. The mechanism by which chrysin suppresses COX-2 expression remains poorly understood. In the present report, we investigated the effect of chrysin on the expression of COX-2 in lipopolysaccharide (LPS)-activated Raw 264.7 cells. Chrysin significantly suppressed the LPS-induced COX-2 protein and mRNA expression in a dose-dependent manner. The ability of chrysin to suppress the expression of the COX-2 was investigated using luciferase reporters controlled by various cis-elements in COX-2 promoter region. Mutational analysis and electrophoretic mobility shift assay verified that nuclear factor for IL-6 was identified as responsible for the chrysin-mediated COX-2 downregulation. These results will provide new insights into the anti-inflammatory and anti-carcinogenic properties of chrysin.

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Abstract. Resveratrol (3,4',5 tri-hydroxystilbene), a naturally occurring polyphenolic compound highly enriched in grapes and red wine, has been shown to induce anti-proliferation and apoptosis of human cancer cell lines. Resveratrol-induced dose-dependent apoptotic cell death in colon carcinoma cells, was measured by FACS analysis. Treatment of HT29 human colon carcinoma cells with resveratrol was found to induce a number of signature ER stress markers; phosphorylation of eukaryotic initiation factor-2α (eIF-2α), ER stress-specific XBP1 splicing and CCAAT/enhancer-binding proteinhomologous protein (CHOP). In addition, resveratrol induced up-regulation of glucose-regulated protein (GRP)-78, suggesting the induction of ER stress. Furthermore, the inhibition of caspase-4 activity by z-LEVD-fmk significantly reduced resveratrol-induced apoptosis. Taken together, the present study therefore provides strong evidence to support an important role of ER stress response in mediating the resveratrol-induced apoptosis.