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KMID : 0370220080520010062
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Yakhak Hoeji
2008 Volume.52 No. 1 p.62 ~ p.66
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Inhibitory Effects of Propenone Derivatives on NF-xB activity and IL-8-Induced Monocyte Adhesion to Colon Epithelial Cells
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Park Su-Young
Kim Kyoung-Jin
Lee Jong-Suk
Lee Eung-Seok
Kim Jung-Ae
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Abstract
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In this study, we examined the inhibitory effects of propenone derivatives, 1,3-diphenyl-propenone (DPhP), 3-phenyl-1-thiophen-2-yl-propenone (PhT2P), 3-phenyl-1-thiophen-3-yl-propenone (PhT3P) and 1-furan-2-yl-3-phenyl-propenone (FPhP), on TNF-α-induced nuclear factor (NF)-xB activity and interleukin (IL)-8-induced monocyte adhesion to colon epithelial cells. 1-Furan-2-yl-3-pyridin-2-yl-propenone (FPP-3) that is previously reported as a NF-xB inhibitor suppressed TNF-α-induced monocyte-epithelial cell adhesion in a concentration-dependent manner. The propenone derivatives, DPhP, PhT2P, PhT3P, FPhP, also inhibited TNF-α-induced NF-xB activation in a similar degree to FPP-3. In a DPPH radical scavenging assay, none of the compounds showed DPPH radical scavenging activity, indicating that the inhibitory actions of the propenone derivatives on redox-sensitive NF-xB activity is not due to a simple free radical scavenging activity. In addition, the propenone derivatives also suppressed the IL-8-induced monocyte adhesion to colon epithelial cells. Furthermore, the effective concentrations of the propenone derivatives on both NF-xB activation as well as IL-8 induced monocyte-epithelial cell adhesion were 1000 times lower than 5-aminosalicylic acid (5-ASA), a clinically used drug for inflammatory bowel disease. These results suggest that the propenone derivatives may be a potential lead having a strong inhibitory activity against inflammatory cytokine-induced epithelial inflammation.
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KEYWORD
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TNF-αNF-xB, Propenone, Interleukin-8, 5-aminosalicylic acid
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