Azithromycin may inhibit interleukin-8 through suppression of Rac1 and a nuclear factor-kappa B pathway in KB cells stimulated with lipopolysaccharide

J Periodontol. 2011 Nov;82(11):1623-31. doi: 10.1902/jop.2011.100721. Epub 2011 Mar 21.

Abstract

Background: Recent studies have shown that the 15-member macrolide antibiotic azithromycin (AZM) not only has antibacterial activity, but also results in the role of immunomodulator. Interleukin (IL)-8 is an important inflammatory mediator in periodontal disease. However, there have been no reports on the effects of AZM on IL-8 production from human oral epithelium. Therefore, we investigated the effects of AZM on IL-8 production in an oral epithelial cell line.

Methods: KB cells were stimulated by Escherichia coli or Aggregatibacter actinomycetemcomitans (previously Actinobacillus actinomycetemcomitans) lipopolysaccharide (LPS) with or without AZM. IL-8 mRNA and protein expression and production in response to LPS were analyzed by quantitative polymerase chain reaction, flow cytometry, and enzyme-linked immunosorbent assay. The activation of nuclear factor-kappa B (NF-κB) and Rac1, which is important for IL-8 expression, was analyzed by enzyme-linked immunosorbent assay and Western blotting, respectively.

Results: IL-8 mRNA expression, IL-8 production, and NF-κB activation in LPS-stimulated KB cells were inhibited by the addition of AZM. LPS-induced Rac1 activation was also suppressed by AZM.

Conclusions: This study suggests that AZM inhibits LPS-induced IL-8 production in an oral epithelial cell line, in part caused by the suppression of Rac1 and NF-κB activation. The use of AZM might provide possible benefits in periodontal therapy, with respect to both its antibacterial action and apparent anti-inflammatory effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Azithromycin / pharmacology*
  • Cells, Cultured
  • Epithelial Cells / cytology
  • Epithelial Cells / drug effects*
  • Epithelial Cells / metabolism
  • Gene Expression Regulation / drug effects
  • Humans
  • Interleukin-8 / drug effects*
  • Lipopolysaccharides / pharmacology
  • NF-kappa B / drug effects
  • NF-kappa B / metabolism
  • Signal Transduction / drug effects*
  • rac1 GTP-Binding Protein / drug effects
  • rac1 GTP-Binding Protein / metabolism

Substances

  • Anti-Bacterial Agents
  • Interleukin-8
  • Lipopolysaccharides
  • NF-kappa B
  • RAC1 protein, human
  • Azithromycin
  • rac1 GTP-Binding Protein