Abstract
Icariin is the major active constituent of Epimedii Herba. Our recent study showed that icariin displayed anti-inflammatory potential. One novel derivate of icariin is 3,5,7-Trihydroxy-4'-methoxy-8-(3-hydroxy-3-methylbutyl)-flavone (ICT). Little is known about ICT's pharmacological activities. In our study, the anti-inflammatory properties of ICT were evaluated. Murine RAW264.7 cells and C57BL/6J mice stimulated by lipopolysaccharide (LPS) was used as in vitro and in vivo inflammatory model, respectively. Our data showed that ICT (1-100 μg/mL) significantly inhibited LPS-induced tumor necrosis factor-α (TNF-α), nitric oxide (NO), prostaglandin E2 (PGE2) production in vitro. These effects did not depend on cytotoxicity. The in vivo assay displayed that pretreatment of C57BL/6J mice with ICT (25-100 mg/kg, by gavage) for 3 days decreased LPS-induced serum levels of TNF-α, PGE2, and neutrophils CD11b expression dose-dependently. Furthermore, our data suggested that ICT reduced NO and PGE2 levels by inhibiting inducible NO synthase and cyclooxygenase-2 protein expression. To our knowledge, it is the first time that the anti-inflammatory effects of ICT have been evaluated.
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 / isolation & purification
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
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Blotting, Western
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CD11b Antigen / immunology
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Cell Line
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Cell Survival / drug effects
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Cell Survival / immunology
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Dinoprostone / blood
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Dinoprostone / immunology
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Enzyme-Linked Immunosorbent Assay
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Female
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Flavones / isolation & purification
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Flavones / pharmacology
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Flavones / therapeutic use*
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Flavonoids / isolation & purification
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Flavonoids / pharmacology
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Flavonoids / therapeutic use*
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Flow Cytometry
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Inflammation / blood
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Inflammation / immunology
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Inflammation / prevention & control*
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Lipopolysaccharides / pharmacology
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Macrophage Activation / drug effects
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Macrophage Activation / immunology
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Macrophages / drug effects*
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Macrophages / immunology
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Macrophages / metabolism
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Mice
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Mice, Inbred C57BL
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Molecular Structure
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Nitric Oxide / biosynthesis
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Tumor Necrosis Factor-alpha / blood
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Tumor Necrosis Factor-alpha / immunology
Substances
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3,5,7-trihydroxy-4'-methoxy-8-(3-hydroxy-3-methylbutyl)flavone
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Anti-Inflammatory Agents, Non-Steroidal
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CD11b Antigen
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Flavones
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Flavonoids
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Lipopolysaccharides
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Tumor Necrosis Factor-alpha
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Nitric Oxide
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Dinoprostone
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icariin