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

Title
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
Author(s)
정태천김미진타라만카다얏엄연지이응석박필훈
Keywords
MONOCYTE CHEMOATTRACTANT PROTEIN-1; HUMAN ENDOTHELIAL-CELLS; KAPPA-B; GENE-EXPRESSION; INFLAMMATORY RESPONSE; EPITHELIAL-CELLS; NADPH OXIDASE; ALPHA; INDUCTION; PATHWAY
Issue Date
201503
Publisher
KOREAN SOC APPLIED PHARMACOLOGY
Citation
BIOMOLECULES & THERAPEUTICS, v.23, no.2, pp.119 - 127
Abstract
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.
URI
http://hdl.handle.net/YU.REPOSITORY/33226http://dx.doi.org/10.4062/biomolther.2014.127
ISSN
1976-9148
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약학대학 > 약학부 > Articles
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