The Korean Journal of Physiology and Pharmacology

The Korean Society of Pharmacology (대한약리학회)
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2-(4-Hydroxyphenyl)-5-(3-Hydroxypropenyl)-7-Methoxybenzofuran, a Novel Ailanthoidol Derivative, Exerts Anti-Inflammatory Effect through Downregulation of Mitogen-Activated Protein Kinase in Lipopolysaccharide-Treated RAW 264.7 Cells

  • Kim, Hyeon Jin (Department of Biomedical Science, College of Natural Science, Catholic University of Daegu) ;
  • Jun, Jong-Gab (Department of Chemistry and Institute of Natural Medicine, Hallym University) ;
  • Kim, Jin-Kyung (Department of Biomedical Science, College of Natural Science, Catholic University of Daegu)
  • Received : 2013.03.05
  • Accepted : 2013.05.02
  • Published : 2013.06.30
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Abstract

We reported that ailanthoidol, a neolignan from Zanthoxylum ailanthoides and Salvia miltiorrhiza Bunge, inhibited inflammatory reactions by macrophages and protected mice from endotoxin shock. We examined the anti-inflammatory activity of six synthetic ailanthoidol derivatives (compounds 1-6). Among them, compound 4, 2-(4-hydroxyphenyl)-5-(3-hydroxypropenyl)-7-methoxybenzofuran, had the lowest $IC_{50}$ value concerning nitric oxide (NO) release from lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Compound 4 suppressed the generation of prostaglandin (PG) $E_2$ and the expression of inducible NO synthase and cyclooxygenase (COX)-2 induced by LPS, and inhibited the release of LPS-induced pro-inflammatory cytokines from RAW264.7 cells. The underlying mechanism of compound 4 on anti-inflammatory action was correlated with the down-regulation of mitogen-activated protein kinase and activator protein-1 activation. Compound 4 is potentially an effective functional chemical candidate for the prevention of inflammatory diseases.

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References

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