Abstract
Flavonoids are a class of compounds that exist in nature with the structure of 2-phenyl-chromone. In Chinese traditional medicine, herbal drugs containing flavonoids are widely used for the treatment of inflammation, cardiovascular disease, tumor and so on. In this study, we investigated the anti-inflammatory effect and related mechanisms of a novel synthetic flavonoid, (E)-1-(4-ethoxyphenyl)-3-(4-nitrophenyl)-prop-2-en-1-one (ETH) in lipopolysaccharide (LPS) stimulated macrophages. Our results showed that ETH inhibited LPS-induced TNF-α and IL-6 release in a dose-dependent manner, and decreased TNF-α, IL-1β, IL-6 and iNOS mRNA production. LPS-induced expression of cyclooxygenase-2 (COX-2) was also significantly attenuated by ETH. Pretreatment with ETH reduced the I-κBα phosphorylation, p65 nuclear translocation as well as NF-κB-dependent transcriptional activity. In addition, ETH exhibited a significant protection against LPS-induced inflammatory mortality in mice. Taken together, these findings suggest that ETH can inhibit LPS-induced inflammation via suppressing NF-κB signaling pathway, indicating that ETH may be a potential anti-inflammatory agent.
Copyright © 2013 Elsevier B.V. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Blotting, Western
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Cell Culture Techniques
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Cell Line
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Cell Survival / drug effects
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Chalcones / chemistry
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Chalcones / pharmacology*
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Dose-Response Relationship, Drug
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Flavonoids / chemistry
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Flavonoids / pharmacology*
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Gene Expression Regulation / drug effects*
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Interleukin-1beta / genetics
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Interleukin-6 / genetics
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Lipopolysaccharides / toxicity*
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Macrophages / drug effects
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Macrophages / immunology
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Male
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Medicine, Chinese Traditional
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Mice
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Mice, Inbred C57BL
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Mice, Inbred ICR
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Molecular Structure
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NF-kappa B / antagonists & inhibitors*
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NF-kappa B / biosynthesis
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Nitric Oxide Synthase Type II / genetics
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Protein Transport
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Real-Time Polymerase Chain Reaction
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Shock, Septic / prevention & control
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Signal Transduction / drug effects*
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Survival Analysis
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Tumor Necrosis Factor-alpha / genetics
Substances
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1-(4-ethoxyphenyl)-3-(4-nitrophenyl)-prop-2-en-1-one
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Anti-Inflammatory Agents, Non-Steroidal
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Chalcones
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Flavonoids
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Interleukin-1beta
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Interleukin-6
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Lipopolysaccharides
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NF-kappa B
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Tumor Necrosis Factor-alpha
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lipopolysaccharide, E coli O55-B5
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Nitric Oxide Synthase Type II
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Nos2 protein, mouse