1,8-cineol inhibits the Wnt/β-catenin signaling pathway through GSK-3 dephosphorylation in nasal polyps of chronic rhinosinusitis patients

Eur J Pharmacol. 2018 Sep 15:835:140-146. doi: 10.1016/j.ejphar.2018.07.060. Epub 2018 Aug 3.

Abstract

Chronic rhinosinusitis with nasal polyps (CRSwNP) represents a benign neoplasm of the nasal mucosa, which leads to a decreased breathing capacity and reduced olfaction. The pathogenesis and the molecular mechanisms driving nasal polyps are not very well known. GSK-3 is involved in the regulation of various biosynthetic pathways and various kinases are able to regulate the GSK-3. Therefore, we investigated the effect of the monoterpene oxide 1,8-cineol on the regulation of the Wnt/β-catenin signaling pathway with its central regulator protein GSK-3 in vitro. We determined GSK-3 expression and phosphorylation as well as the expression of negative regulators (Akt and SGK) and downstream activation of β-catenin in nasal polyps of patients with CRSwNP by immunohistochemistry and Western blot experiments. In this study we demonstrated for the first time, that 1,8-cineol acts as a potential inhibitor of the Wnt/β-catenin signaling pathway, by affecting the inhibitory phosphorylation of GSK-3, which is the key regulator of the β-catenin activity. Our data provide novel insights in the regulatory networks responsible for the progression of CRSwNP and furthermore represent a new mechanism of 1,8-cineol activity, which may lead to novel treatment approaches to this natural drug.

Keywords: 1,8-cineol (PubChem CID: 2758); Chronic rhinosinusitis with nasal polyps; GSK-3; Nasal polyps; Wnt; β-catenin.

MeSH terms

  • Eucalyptol / pharmacology*
  • Female
  • Glycogen Synthase Kinase 3 / metabolism*
  • Humans
  • Male
  • Middle Aged
  • Nasal Polyps / complications*
  • Nasal Polyps / metabolism
  • Nasal Polyps / pathology*
  • Phosphorylation / drug effects
  • Sinusitis / complications*
  • Wnt Signaling Pathway / drug effects*

Substances

  • Glycogen Synthase Kinase 3
  • Eucalyptol