Fluoxetine suppresses inflammatory reaction in microglia under OGD/R challenge via modulation of NF-κB signaling

Biosci Rep. 2019 Apr 26;39(4):BSR20181584. doi: 10.1042/BSR20181584. Print 2019 Apr 30.

Abstract

We aimed to investigate the anti-inflammatory role of fluoxetine, a selective serotonin reuptake inhibitor, in microglia (MG) and the mechanisms under oxygen glucose deprivation/reoxygenation (OGD/R). An OGD/R model on BV-2 cells was used for the study of microglia under ischemia/reperfusion injury in ischemic stroke. Lentiviral transfection was applied to knock down IκB-α. Enzyme-linked immunosorbent assay (ELISA) was used for detecting levels of TNF-α, IL-1β, and IL-6, and real-time PCR was used to assess the expression of IκB-α protein. Western blotting was applied to analyze NF-κB-signaling related proteins and Cell Counting Kit-8 (CCK-8) was used for assessing cell viability. Molecular docking and drug affinity responsive target stability (DARTS) assay were used for the detection of the interaction between IκB-α and fluoxetine. We found that fluoxetine decreased the levels of TNF-α, IL-1β, and IL-6 in supernatant as well as NF-κB subunits p65 and p50 in BV-2 cells under OGD/R. Fluoxetine significantly increased the level of IκB-α through the inhibition of IκB-α ubiquitylation and promoted the bonding of IκB-α and fluoxetine in BV-2 cells under OGD/R. Knocking down IκB-α attenuated the decreasing effect of TNF-α, IL-1β, and IL-6 as well as p65 and p50 in BV-2 cells under OGD/R led to by fluoxetine. In conclusion, our present study demonstrated the anti-inflammatory role of fluoxetine and its mechanisms related to the modulation of NF-κB-related signaling in MG under ischemia/reperfusion challenge.

Keywords: NF-κB; OGD/R; fluoxetine; inflammation; microglia.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Fluoxetine / pharmacology*
  • Gene Expression Regulation / drug effects
  • Glucose / metabolism
  • Humans
  • Inflammation / drug therapy*
  • Interleukin-1beta / genetics
  • Interleukin-6 / genetics
  • Mice
  • Microglia / drug effects
  • Microglia / pathology
  • Molecular Docking Simulation
  • NF-KappaB Inhibitor alpha / genetics
  • NF-kappa B / genetics*
  • Oxygen / pharmacology
  • Reperfusion Injury / drug therapy*
  • Reperfusion Injury / genetics
  • Reperfusion Injury / pathology
  • Selective Serotonin Reuptake Inhibitors / pharmacology
  • Signal Transduction / drug effects
  • Transcription Factor RelA / genetics
  • Tumor Necrosis Factor-alpha / genetics

Substances

  • IL1B protein, mouse
  • Interleukin-1beta
  • Interleukin-6
  • NF-kappa B
  • Serotonin Uptake Inhibitors
  • Transcription Factor RelA
  • Tumor Necrosis Factor-alpha
  • Fluoxetine
  • NF-KappaB Inhibitor alpha
  • Glucose
  • Oxygen