MHY1485 ameliorates UV-induced skin cell damages via activating mTOR-Nrf2 signaling

Oncotarget. 2017 Feb 21;8(8):12775-12783. doi: 10.18632/oncotarget.14299.

Abstract

Ultra Violet (UV)-caused skin cell damage is a main cause of skin cancer. Here, we studied the activity of MHY1485, a mTOR activator, in UV-treated skin cells. In primary human skin keratinocytes, HaCaT keratinocytes and human skin fibroblasts, MHY1485 ameliorated UV-induced cell death and apoptosis. mTOR activation is required for MHY1485-induced above cytoprotective actions. mTOR kinase inhibitors (OSI-027, AZD-8055 and AZD-2014) or mTOR shRNA knockdown almost abolished MHY1485-induced cytoprotection. Further, MHY1485 treatment in skin cells activated mTOR downstream NF-E2-related factor 2 (Nrf2) signaling, causing Nrf2 Ser-40 phosphorylation, stabilization/upregulation and nuclear translocation, as well as mRNA expression of Nrf2-dictated genes. Contrarily, Nrf2 knockdown or S40T mutation almost nullified MHY1485-induced cytoprotection. MHY1485 suppressed UV-induced reactive oxygen species production and DNA single strand breaks in skin keratinocytes and fibroblasts. Together, we conclude that MHY1485 inhibits UV-induced skin cell damages via activating mTOR-Nrf2 signaling.

Keywords: MHY1485; Nrf2; mTOR; skin cell damage; ultra violet (UV).

MeSH terms

  • Apoptosis / drug effects
  • Apoptosis / radiation effects
  • Blotting, Western
  • Cells, Cultured
  • Cytoprotection*
  • DNA Breaks, Single-Stranded
  • Fibroblasts / drug effects
  • Fibroblasts / metabolism
  • Fibroblasts / radiation effects
  • Gene Knockdown Techniques
  • Humans
  • Keratinocytes / drug effects
  • Keratinocytes / metabolism
  • Keratinocytes / radiation effects
  • Morpholines / pharmacology*
  • NF-E2-Related Factor 2 / drug effects
  • NF-E2-Related Factor 2 / metabolism*
  • Reactive Oxygen Species / metabolism
  • Real-Time Polymerase Chain Reaction
  • Signal Transduction / drug effects
  • Skin / drug effects*
  • Skin / metabolism
  • Skin / radiation effects
  • TOR Serine-Threonine Kinases / drug effects
  • TOR Serine-Threonine Kinases / metabolism*
  • Triazines / pharmacology*
  • Ultraviolet Rays / adverse effects

Substances

  • 4,6-dimorpholino-N-(4-nitrophenyl)-1,3,5-triazin-2-amine
  • Morpholines
  • NF-E2-Related Factor 2
  • NFE2L2 protein, human
  • Reactive Oxygen Species
  • Triazines
  • MTOR protein, human
  • TOR Serine-Threonine Kinases