Anti-inflammatory effect of afatinib (an EGFR-TKI) on OGD-induced neuroinflammation

Sci Rep. 2019 Feb 21;9(1):2516. doi: 10.1038/s41598-019-38676-7.

Abstract

Activated epidermal growth factor receptor (EGFR) has been proposed in the pathophysiology of neurodegenerative diseases. In the present study, the anti-inflammatory effect of afatinib, an EGFR-tyrosine kinase inhibitor (EGFR-TKIs) was investigated using CTX-TNA2 cells and primary cultured astrocytes subjected to oxygen/glucose deprivation (OGD). We found that OGD induced EGFR phosphorylation and activated subsequent signaling pathways, including phosphorylation of AKT and extracellular signal-regulated kinases (ERK). Afatinib blocked OGD-induced phosphorylation of EGFR, AKT and ERK. At the same time, afatinib attenuated OGD-induced elevations in glial fibrillary acidic protein (a biomarker of activated astrocytes) and proliferating cell nuclear antigen expression (a cell proliferating biomarker) as well as hypoxia-induced migratory ability. Furthermore, afatinib decreased OGD-induced increases in cyclooxygenase-II and inducible nitric oxide synthase expression of the treated astrocytes as well as NO content in the culture medium. Moreover, afatinib attenuated OGD-induced caspase 1 activation (a biomarker of inflammasome activation) and interleukin-1β levels (a pro-inflammatory cytokine). Collectively, afatinib could block OGD-induced EGFR activation and its downstream signaling pathways in astrocytes. Moreover, afatinib attenuated OGD-induced astrocyte activation, proliferation and inflammasome activation. These data support the involvement of EGFR activation in neuroinflammation. Furthermore, EGFR-TKIs may be promising in inhibiting neuroinflammation in the CNS neurodegenerative diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Afatinib / pharmacology*
  • Animals
  • Astrocytes / drug effects
  • Astrocytes / metabolism
  • Astrocytes / pathology
  • Cell Hypoxia / drug effects
  • Cell Proliferation / drug effects
  • Cultural Deprivation
  • Cyclooxygenase 2 / genetics
  • Gene Expression Regulation / drug effects
  • Genes, erbB-1 / genetics*
  • Glucose / metabolism
  • Inflammation / drug therapy*
  • Inflammation / genetics
  • Inflammation / pathology
  • MAP Kinase Signaling System / drug effects
  • Neurodegenerative Diseases / drug therapy*
  • Neurodegenerative Diseases / genetics
  • Neurodegenerative Diseases / pathology
  • Neuroglia / drug effects
  • Nitric Oxide / genetics
  • Nitric Oxide Synthase Type II / genetics
  • Oxygen / metabolism
  • Phosphorylation / drug effects
  • Primary Cell Culture
  • Protein Kinase Inhibitors / pharmacology
  • Rats

Substances

  • Protein Kinase Inhibitors
  • Nitric Oxide
  • Afatinib
  • Nitric Oxide Synthase Type II
  • Cyclooxygenase 2
  • Glucose
  • Oxygen