GSK-3β as a target for protection against transient cerebral ischemia

Int J Med Sci. 2017 Mar 11;14(4):333-339. doi: 10.7150/ijms.17514. eCollection 2017.

Abstract

Stroke remains the leading cause of death and disability worldwide. This fact highlights the need to search for potential drug targets that can reduce stroke-related brain damage. We showed recently that a glycogen synthase kinase-3β (GSK-3β) inhibitor attenuates tissue plasminogen activator-induced hemorrhagic transformation after permanent focal cerebral ischemia. Here, we examined whether GSK-3β inhibition mitigates early ischemia-reperfusion stroke injury and investigated its potential mechanism of action. We used the rat middle cerebral artery occlusion (MCAO) model to mimic transient cerebral ischemia. At 3.5 h after MCAO, cerebral blood flow was restored, and rats were administered DMSO (vehicle, 1% in saline) or GSK-3β inhibitor TWS119 (30 mg/kg) by intraperitoneal injection. Animals were sacrificed 24 h after MCAO. TWS119 treatment reduced neurologic deficits, brain edema, infarct volume, and blood-brain barrier permeability compared with those in the vehicle group. TWS119 treatment also increased the protein expression of β-catenin and zonula occludens-1 but decreased β-catenin phosphorylation while suppressing the expression of GSK-3β. These results indicate that GSK-3β inhibition protects the blood-brain barrier and attenuates early ischemia-reperfusion stroke injury. This protection may be related to early activation of the Wnt/β-catenin signaling pathway.

Keywords: TWS119; Wnt/β-catenin signaling; blood-brain barrier; ischemic stroke.

MeSH terms

  • Animals
  • Blood-Brain Barrier / drug effects
  • Brain / blood supply
  • Brain / physiopathology
  • Disease Models, Animal
  • Gene Expression Regulation / drug effects
  • Glycogen Synthase Kinase 3 beta / antagonists & inhibitors*
  • Glycogen Synthase Kinase 3 beta / genetics
  • Humans
  • Infarction, Middle Cerebral Artery / drug therapy
  • Infarction, Middle Cerebral Artery / genetics
  • Infarction, Middle Cerebral Artery / physiopathology
  • Ischemic Attack, Transient / drug therapy*
  • Ischemic Attack, Transient / genetics
  • Ischemic Attack, Transient / physiopathology
  • Pyrimidines / administration & dosage
  • Pyrroles / administration & dosage
  • Rats
  • Stroke / drug therapy*
  • Stroke / genetics
  • Stroke / physiopathology
  • Wnt Signaling Pathway / genetics
  • Zonula Occludens-1 Protein / genetics
  • beta Catenin / genetics*

Substances

  • Ctnnb1 protein, rat
  • Pyrimidines
  • Pyrroles
  • TWS 119
  • Zonula Occludens-1 Protein
  • beta Catenin
  • Glycogen Synthase Kinase 3 beta