Melatonin Induces AGS Gastric Cancer Cell Apoptosis via Regulating PERK/eIF2α and HSF1/NF-κB Signaling Pathway

Ann Clin Lab Sci. 2022 Jan;52(1):40-47.

Abstract

Objective: Melatonin exhibits numerous anti-cancer activities in the treatment of human cancers. Nevertheless, the mechanisms of anti-gastric cancer effect of melatonin is still unclear. The aim of the study is to investigate the interaction between melatonin, endoplasmic reticulum (ER) stress, NF-κB signaling and HSF1 protein in gastric cancer cells.

Methods: In the current study, we used CCK-8, flow cytometry and Western blot to research anticancer mechanism of melatonin in AGS cells.

Results: The data demonstrated that melatonin could suppress cell proliferation and increase cell apoptosis. We explore that the ER stress and NF-kB signaling pathways play crucial roles in the cell apoptosis process. Of note, melatonin increased the expression of p-PERK and p-eIF2α, and decreased the expression of p-P65 and p-IκBα. A combination of melatonin and PERK inhibitor (GSK2606414) or NF-κB inhibitor (Bay11-7082) suppressed the activation PERK/eIF2α and NF-κB signaling pathway. Subsequently, the expression of HSF1 protein was upregulated by melatonin and kept its expression by Bay 11-7082.

Conclusion: These results suggest that melatonin induces AGS cell apoptosis by up-regulating PERK/eIF2α and downregulating NF-κB signaling pathway.

Keywords: HSF1; NF-κB; PERK/eIF2α; apoptosis; gastric cancer; melatonin.

MeSH terms

  • Apoptosis / drug effects
  • Eukaryotic Initiation Factor-2* / metabolism
  • Heat Shock Transcription Factors* / metabolism
  • Humans
  • Melatonin* / pharmacology
  • NF-kappa B* / metabolism
  • Signal Transduction / drug effects
  • Stomach Neoplasms* / drug therapy
  • Stomach Neoplasms* / metabolism
  • Stomach Neoplasms* / pathology
  • eIF-2 Kinase* / metabolism

Substances

  • EIF2S1 protein, human
  • Eukaryotic Initiation Factor-2
  • HSF1 protein, human
  • Heat Shock Transcription Factors
  • NF-kappa B
  • EIF2AK3 protein, human
  • eIF-2 Kinase
  • Melatonin