Abstract
Imperatorin is a type of coumarin compound with antibacterial and antiviral activities. In the present study, we examined the anti-inflammatory effects of imperatorin in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages by investigating its impact on the production and expression of cytokines and the major signal-transduction pathways. We found that imperatorin downregulated LPS-induced levels of TNF-α, IL-1β, and IL-6 in RAW 264.7 macrophages in a concentration-dependent manner, and it significantly inhibited expression of TNF-α and IL-6 (P < 0.05 or P < 0.01). The phosphorylation of mitogen-activated protein kinases and nuclear factor-kappaB (NF-κB) p65 protein were analyzed by western blotting. In RAW 264.7 macrophages treated with 1 mg/L of LPS, imperatorin significantly inhibited p38 and Jun N-terminal kinase phosphorylation protein expression. However, there was no significant change in p-ERK. Furthermore, imperatorin also inhibited NF-κB translocation into the nucleus through blockage of IκBα phosphorylation and degradation.
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 / pharmacology
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Cell Line
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Cell Survival
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Enzyme Activation / drug effects
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Furocoumarins / pharmacology*
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I-kappa B Kinase / metabolism
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Inflammation / drug therapy*
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Inflammation Mediators / immunology
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Inflammation Mediators / metabolism
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Interleukin-1beta / biosynthesis
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Interleukin-1beta / drug effects
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Interleukin-1beta / metabolism
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Interleukin-6 / biosynthesis
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Interleukin-6 / metabolism
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JNK Mitogen-Activated Protein Kinases / metabolism
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Lipopolysaccharides
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Macrophages / immunology*
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Mice
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Mitogen-Activated Protein Kinases / drug effects
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Mitogen-Activated Protein Kinases / metabolism
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NF-kappa B / drug effects
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NF-kappa B / metabolism*
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Phosphorylation / drug effects
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Protein Transport
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Transcription Factor RelA / metabolism
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Tumor Necrosis Factor-alpha / biosynthesis
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Tumor Necrosis Factor-alpha / drug effects
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Tumor Necrosis Factor-alpha / metabolism
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p38 Mitogen-Activated Protein Kinases / metabolism
Substances
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Anti-Inflammatory Agents
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Furocoumarins
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Inflammation Mediators
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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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Rela protein, mouse
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Transcription Factor RelA
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Tumor Necrosis Factor-alpha
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I-kappa B Kinase
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JNK Mitogen-Activated Protein Kinases
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Mitogen-Activated Protein Kinases
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p38 Mitogen-Activated Protein Kinases
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imperatorin