Fisetin inhibits TNF-α-induced inflammatory action and hydrogen peroxide-induced oxidative damage in human keratinocyte HaCaT cells through PI3K/AKT/Nrf-2-mediated heme oxygenase-1 expression

Int Immunopharmacol. 2015 Dec;29(2):246-253. doi: 10.1016/j.intimp.2015.11.014. Epub 2015 Nov 14.

Abstract

Oxidative skin damage and skin inflammation play key roles in the pathogenesis of skin-related diseases. Fisetin is a naturally occurring flavonoid abundantly found in several vegetables and fruits. Fisetin has been shown to exert various positive biological effects, such as anti-cancer, anti-proliferative, neuroprotective and anti-oxidative effects. In this study, we investigate the skin protective effects and anti-inflammatory properties of fisetin in hydrogen peroxide- and TNF-α-challenged human keratinocyte HaCaT cells. When HaCaT cells were treated with non-cytotoxic concentrations of fisetin (1-20μM), heme oxygenase (HO)-1 mRNA and protein expression increased in a dose-dependent manner. Furthermore, fisetin dose-dependently increased cell viability and reduced ROS production in hydrogen peroxide-treated HaCaT cells. Fisetin also inhibited the production of NO, PGE2 IL-1β, IL-6, expression of iNOS and COX-2, and activation of NF-κB in HaCaT cells treated with TNF-α. Fisetin induced Nrf2 translocation to the nuclei. HO-1 siRNA transient transfection reversed the effects of fisetin on cytoprotection, ROS reduction, NO, PGE2, IL-1β, IL-6, and TNF-α production, and NF-κB DNA-binding activity. Moreover, fisetin increased Akt phosphorylation and a PI3K pathway inhibitor (LY294002) abolished fisetin-induced cytoprotection and NO inhibition. Taken together, these results provide evidence for a beneficial role of fisetin in skin therapy.

Keywords: Anti-skin inflammation; Fisetin; Heme oxygenase-1; Human keratinocyte HaCaT; Skin protective effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antioxidants / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Flavonoids / pharmacology*
  • Flavonols
  • Heme Oxygenase-1 / biosynthesis*
  • Heme Oxygenase-1 / genetics
  • Humans
  • Hydrogen Peroxide / antagonists & inhibitors*
  • Hydrogen Peroxide / toxicity
  • Inflammation / chemically induced
  • Inflammation / prevention & control*
  • Keratinocytes / drug effects*
  • NF-E2-Related Factor 2 / metabolism
  • Oncogene Protein v-akt / metabolism
  • Oxidants / toxicity*
  • Oxidative Stress / drug effects*
  • Phosphatidylinositol 3-Kinases / metabolism
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors*
  • Tumor Necrosis Factor-alpha / toxicity

Substances

  • Antioxidants
  • Flavonoids
  • Flavonols
  • NF-E2-Related Factor 2
  • NFE2L2 protein, human
  • Oxidants
  • Tumor Necrosis Factor-alpha
  • Hydrogen Peroxide
  • Heme Oxygenase-1
  • Oncogene Protein v-akt
  • fisetin