A mechanism for the action of the compound DA-6034 on NF-κB pathway activation in Helicobacter pylori-infected gastric epithelial cells

Scand J Immunol. 2011 Sep;74(3):253-263. doi: 10.1111/j.1365-3083.2011.02577.x.

Abstract

DA-6034 is a synthetic derivative of eupatilin, a flavonoid with anti-inflammatory effects. The aim of this study was to investigate the effects of DA-6034 on the interactions between IκB kinase (IKK) and heat shock protein 90 (Hsp90), and activation of the nuclear factor-kappaB (NF-κB) signalling pathway in human gastric epithelial cells infected with Helicobacter pylori. MKN-45 gastric epithelial cell line was treated with DA-6034 and H. pylori. DA-6034 significantly inhibited NF-κB activation and upregulated the expressions of interleukin-8 (IL-8) and monocyte chemoattractant protein-1 in MKN-45 cells infected with H. pylori. However, DA-6034 did not influence activator protein-1 DNA binding activity in H. pylori-infected gastric epithelial cells. Pretreatment with DA-6034 attenuated the H. pylori-induced increase in IKK activity, and Hsp90 was associated with IKK-α and IKK-γ in MKN-45 cells. Treatment with DA-6034 dissociated the Hsp90 and IKK-γ complex in H. pylori-infected cells, leading to the inhibition of IL-8 expression. These results suggest that the eupatilin derivative 7-carboxymethyloxy-3',4',5-trimethoxy flavone has anti-inflammatory activity in gastric epithelial cells infected with H. pylori through the promotion of the dissociation of the IKK-γ-Hsp90 complex and suppression of NF-κB signalling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / metabolism
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cell Line
  • Chemokine CCL2 / biosynthesis
  • Chemokine CCL2 / genetics
  • Electrophoretic Mobility Shift Assay
  • Flavonoids / metabolism
  • Flavonoids / pharmacology*
  • Gastric Mucosa / metabolism
  • Gastric Mucosa / microbiology*
  • HSP90 Heat-Shock Proteins / metabolism*
  • Helicobacter pylori / drug effects*
  • Helicobacter pylori / pathogenicity
  • Humans
  • I-kappa B Kinase / metabolism*
  • Immunoblotting
  • Interleukin-8 / biosynthesis
  • Interleukin-8 / genetics
  • NF-kappa B / metabolism*
  • Polymerase Chain Reaction
  • Signal Transduction / drug effects
  • Transcription Factor AP-1 / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Chemokine CCL2
  • Flavonoids
  • HSP90 Heat-Shock Proteins
  • Interleukin-8
  • NF-kappa B
  • Transcription Factor AP-1
  • I-kappa B Kinase
  • recoflavone