Inhibitory Effect of 3-(4-Hydroxyphenyl)-1-(thiophen-2-yl) prop-2-en-1-one, a Chalcone Derivative on MCP-1 Expression in Macrophages via Inhibition of ROS and Akt Signaling

Kim, Mi Jin; Kadayat, Taraman; Um, Yeon Ji; Jeong, Tae Cheon; Lee, Eung-Seok; Park, Pil-Hoon

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자료유형: 학술저널

저자정보: Kim, Mi Jin (College of Pharmacy, Yeungnam University) Kadayat, Taraman (College of Pharmacy, Yeungnam University) Um, Yeon Ji (College of Pharmacy, Yeungnam University) Jeong, Tae Cheon (College of Pharmacy, Yeungnam University) Lee, Eung-Seok (College of Pharmacy, Yeungnam University) Park, Pil-Hoon (College of Pharmacy, Yeungnam University)

저널정보: 한국응용약물학회 Biomolecules & Therapeutics(구 응용약물학회지) Biomolecules & therapeutics 제23권 제2호

발행연도: 2015.1

수록면: 119 - 127 (9page)

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Chalcones (1,3-diaryl-2-propen-1-ones), a subfamily of flavonoid, are widely known to possess potent anti-inflammatory and anti-oxidant properties. In this study, we investigated the effect of 3-(4-Hydroxyphenyl)-1-(thio3-(4-Hydroxyphenyl phen-2-yl)prop-2-en-1-one (TI-I-175), a synthetic chalcone derivative, on endotoxin-induced expression of monocyte chemoattractant protein-1 (MCP-1), one of the key chemokines that regulates migration and infiltration of immune cells, and its potential mechanisms. TI-I-175 potently inhibited MCP-1 mRNA expression stimulated by lipopolysaccharide (LPS) in RAW 264.7 macrophages without significant effect on cell viability. Treatment of cells with TI-I-175 markedly prevented LPS-induced transcriptional activation of activator protein-1 (AP-1) as measured by luciferase reporter assay, while nuclear factor-${\kappa}B$ (NF-${\kappa}B$) activity was not inhibited by TI-I-175, implying that TI-I-175 suppressed MCP-1 expression probably via regulation of AP-1. In addition, TI-I-175 treatment significantly inhibited LPS-induced Akt phosphorylation and led to a significant decrease in reactive oxygen species (ROS) production by LPS, which act as up-stream signaling events required for AP-1 activation in RAW 264.7 macrophages. Taken together, these results indicate that TI-I-175 suppresses MCP-1 gene expression in LPS-stimulated RAW 264.7 macrophages via suppression of ROS production and Akt activation.

#Chalcone #MCP-1 #Reactive oxygen species #Inflammation #Lipopolysaccharide

참고문헌 (37)

참고문헌 신청

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Ban, H. S. / 2004 / Inhibition of lipopolysaccharide-induced expression of inducible nitric oxide synthase and tumor necrosis factor-alpha by 2'-hydroxychalcone derivatives in RAW 264.7 cells / Biochem. Pharmacol 67:1549~1557

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