Eupatilin inhibits lipopolysaccharide-induced expression of inflammatory mediators in macrophages

Life Sci. 2011 Jun 20;88(25-26):1121-6. doi: 10.1016/j.lfs.2011.04.011. Epub 2011 Apr 30.

Abstract

Aims: Eupatilin (5,7-dihydroxy-3,4,6-trimethoxyflavone) is a pharmacologically active ingredients in Stillen(TM), a drug for the gastric mucosal ulcers. Eupatilin has been known to possess anti-peptic, anti-cancer, and anti-allergy activity. In this report, we defined the effect of eupatilin on the endotoxin-induced inflammation in lipopolysaccharide (LPS)-stimulated macrophages.

Main methods: Mouse J774A.1 cell line and mouse peritoneal macrophages were used. Gene expression and production of inflammatory mediators were determined by real-time PCR and Western blot.

Key findings: Eupatilin dose-dependently suppressed LPS-induced expression of inducible nitric oxide synthase (iNOS) and production of nitric oxide (NO). Eupatilin decreased LPS-induced expression of inflammatory mediators and pro-inflammatory cytokines such as cyclooxygenase-2, monocyte chemoattractant protein-1, tumor necrosis factor-α, interleukin (IL)-1β and IL-6. In addition, this suppression of inflammatory mediators was nuclear factor (NF)-κB dependent.

Significance: Our findings imply that eupatilin suppresses inflammatory responses by the inhibition of NF-κB signaling pathway, and downstream inflammatory mediators in endotoxin-stimulated macrophages.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Artemisia / chemistry
  • Blotting, Western
  • Cell Culture Techniques
  • Cell Line
  • Cell Survival / drug effects
  • Cell Survival / immunology
  • Cytokines / genetics
  • Cytokines / immunology
  • Dose-Response Relationship, Drug
  • Flavonoids / chemistry
  • Flavonoids / isolation & purification
  • Flavonoids / pharmacology*
  • Gene Expression / drug effects
  • Inflammation Mediators / antagonists & inhibitors*
  • Inflammation Mediators / immunology
  • Lipopolysaccharides / pharmacology*
  • Macrophages, Peritoneal / drug effects*
  • Macrophages, Peritoneal / immunology*
  • Mice
  • Mice, Inbred BALB C
  • Molecular Structure
  • NF-kappa B / antagonists & inhibitors
  • NF-kappa B / genetics
  • NF-kappa B / immunology
  • Nitric Oxide / biosynthesis
  • Nitric Oxide Synthase Type II / genetics
  • Reverse Transcriptase Polymerase Chain Reaction

Substances

  • Cytokines
  • Flavonoids
  • Inflammation Mediators
  • Lipopolysaccharides
  • NF-kappa B
  • lipopolysaccharide, E. coli O26-B6
  • Nitric Oxide
  • eupatilin
  • Nitric Oxide Synthase Type II
  • Nos2 protein, mouse