Rotundarpene inhibits toll-like receptor 2 activation-induced production of inflammatory mediators in keratinocytes by suppressing the Akt and NF-κB pathways

Int Immunopharmacol. 2014 Feb;18(2):325-32. doi: 10.1016/j.intimp.2013.12.016. Epub 2013 Dec 28.

Abstract

Microbial components have been shown to be involved in the pathogenesis of inflammatory skin diseases. The extract of from the barks of Ilex rotunda Thunb has demonstrated anti-inflammatory and anti-oxidant effects. However, the effect of hemiterpene rotundarpene (4-caffeoyl-3-methyl-but-2-ene-1,4-diol) on the Toll-like receptor (TLR)-2 activation-induced production of inflammatory mediators in keratinocytes has not been studied. Using human keratinocytes, we investigated the effect of rotundarpene on the inflammatory mediator production in relation to the TLR-2-mediated-Akt and NF-κB pathways, which regulates the transcription genes involved in immune and inflammatory responses. Rotundarpene, Akt inhibitor, Bay 11-7085 and N-acetylcysteine each attenuated the lipoteichoic acid- or peptidoglycan-induced production of cytokines and chemokines, expression of TLR-2, activation of NF-κB and Akt, and formation of reactive oxygen species in keratinocytes. Cyclosporine A attenuated the bacterial component-induced production of inflammatory mediators but did not reduce the formation of reactive oxygen species. The results show that rotundarpene may attenuate the bacterial component-stimulated production of inflammatory mediators in keratinocytes by suppressing the TLR-2-mediated activation of the Akt and NF-κB pathways. The effect of rotundarpene may be attributed to its inhibitory effect on the formation of reactive oxygen species. Rotundarpene may exert a preventive effect against the bacterial component-mediated inflammatory skin diseases.

Keywords: Akt and NF-κB pathways; Inflammatory mediator production; Keratinocytes; Microbial components; Rotundarpene; Toll-like receptor-2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents / pharmacology*
  • Caffeic Acids / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cytokines / metabolism
  • Dinoprostone / metabolism
  • Hemiterpenes / pharmacology*
  • Humans
  • Ilex
  • Keratinocytes
  • Lipopolysaccharides / pharmacology
  • NF-kappa B / antagonists & inhibitors*
  • Plant Bark
  • Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
  • Reactive Oxygen Species / metabolism
  • Teichoic Acids / pharmacology
  • Toll-Like Receptor 2 / antagonists & inhibitors*

Substances

  • Anti-Inflammatory Agents
  • Caffeic Acids
  • Cytokines
  • Hemiterpenes
  • Lipopolysaccharides
  • NF-kappa B
  • Reactive Oxygen Species
  • TLR2 protein, human
  • Teichoic Acids
  • Toll-Like Receptor 2
  • rotundarpene
  • lipoteichoic acid
  • Proto-Oncogene Proteins c-akt
  • Dinoprostone