Anti-inflammatory Mechanism Involved in 4-Ethylguaiacol-Mediated Inhibition of LPS-Induced Inflammation in THP-1 Cells

J Agric Food Chem. 2019 Jan 30;67(4):1230-1243. doi: 10.1021/acs.jafc.8b06263. Epub 2019 Jan 17.

Abstract

4-Ethylguaiacol, a common aroma compound of baijiu (a traditional Chinese alcoholic beverage), was assessed for its potential anti-inflammatory effects in an LPS-induced THP-1 cell model. To characterize the effect of 4-ethylguaiacol on the LPS-induced inflammatory response, the mRNA and protein expression of the TLR4-MAPKs-NF-κB-IκBα-AP-1, Nrf2-HO-1, and AMPK-SIRT1 pathways were monitored by ELISA, real-time PCR, and Western blotting. On the basis of the result, 4-ethylguaiacol exerted anti-inflammatory effects at doses of 10, 100, and 500 μM (the concentration of 4-ethylguaiacol in gujinggong baijiu is in the range of 1044 ± 44 to 1661 ± 63 μg/L) and significantly mitigated LPS-induced inflammation via activation of the Nrf2-HO-1 and AMPK-SIRT1 pathways and inhibition of NF-κB and AP-1 activation, thereby markedly inhibiting the activation of inflammasomes and down-regulating the production of inflammatory cytokines. These results indicated that 4-ethylguaiacol could reverse LPS-induced inflammatory responses and is a natural, potent anti-inflammatory component in baijiu.

Keywords: 4-ethylguaiacol; NF-κB; Nrf2; anti-inflammatory; baijiu.

MeSH terms

  • Alcoholic Beverages / analysis*
  • Anti-Inflammatory Agents / pharmacology*
  • Guaiacol / analogs & derivatives*
  • Guaiacol / pharmacology
  • Humans
  • Inflammation / etiology
  • Inflammation / genetics
  • Inflammation / immunology*
  • Lipopolysaccharides / adverse effects*
  • Lipopolysaccharides / immunology
  • Monocytes / drug effects
  • Monocytes / immunology
  • NF-E2-Related Factor 2 / genetics
  • NF-E2-Related Factor 2 / immunology
  • NF-kappa B / genetics
  • NF-kappa B / immunology
  • THP-1 Cells
  • Toll-Like Receptor 4 / genetics
  • Toll-Like Receptor 4 / immunology

Substances

  • Anti-Inflammatory Agents
  • Lipopolysaccharides
  • NF-E2-Related Factor 2
  • NF-kappa B
  • NFE2L2 protein, human
  • Toll-Like Receptor 4
  • Guaiacol
  • 4-ethylguaiacol