Empagliflozin Mitigates PTZ-Induced Seizures in Rats: Modulating Npas4 and CREB-BDNF Signaling Pathway

J Neuroimmune Pharmacol. 2025 Jan 7;20(1):5. doi: 10.1007/s11481-024-10162-6.

Abstract

Empagliflozin (EMPA) is one of the sodium/glucose cotransporter 2 (SGLT2) inhibitors that has been recently approved for the treatment of diabetes mellitus type II. Recently, EMPA has shown protective effects in different neurological disorders, besides its antidiabetic activity. Kindling is a relevant model to study epilepsy and neuroplasticity. This study aimed to investigate the potential protective effects of EMPA (1 and 3 mg/kg orally) against convulsant effects induced by pentylenetetrazole (PTZ) using a modified window- (win-) PTZ kindling protocol. The biochemical dysfunction and hippocampal damage induced by PTZ were profoundly reversed by EMPA treatment in a dose-dependent manner, as evidenced by the significant increase in reduced glutathione (GSH) and decrease in malondialdehyde (MDA) hippocampal contents. Furthermore, EMPA counteracted PTZ-induced neuronal damage in the hippocampal region, as confirmed by histopathological examination of the hippocampal tissues. EMPA impaired astrocytosis and showed an antiapoptotic effect through a significant reduction of glial fibrillary acidic protein (GFAP) and BCL2-Associated X Protein (BAX) expressions, respectively. Interestingly, EMPA exhibited an antiepileptic effect against PTZ-induced seizures through significantly reducing neuronal PAS domain Protein 4 (Npas4), cyclic adenosine monophosphate (cAMP) response element binding protein (CREB) hippocampal expressions, and enhancing the brain-derived neurotrophic factor (BDNF)-tropomyosin receptor kinase B (TrkB) pathway, which are found to be involved in epileptogenesis, eventually leading to significant improvement of behavioral impairments induced by PTZ. Hence, these results showed further prospective insights for EMPA as a neuroprotective agent.

Keywords: BDNF; CREB; Empagliflozin; Neuroplasticity; Npas4; PTZ.

MeSH terms

  • Animals
  • Anticonvulsants / pharmacology
  • Anticonvulsants / therapeutic use
  • Benzhydryl Compounds* / pharmacology
  • Benzhydryl Compounds* / therapeutic use
  • Brain-Derived Neurotrophic Factor* / metabolism
  • Cyclic AMP Response Element-Binding Protein / metabolism
  • Glucosides* / pharmacology
  • Glucosides* / therapeutic use
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • Hippocampus / pathology
  • Kindling, Neurologic / drug effects
  • Male
  • Pentylenetetrazole* / toxicity
  • Rats
  • Rats, Wistar
  • Seizures* / chemically induced
  • Seizures* / drug therapy
  • Seizures* / metabolism
  • Seizures* / prevention & control
  • Signal Transduction* / drug effects
  • Sodium-Glucose Transporter 2 Inhibitors / pharmacology
  • Sodium-Glucose Transporter 2 Inhibitors / therapeutic use

Substances

  • Pentylenetetrazole
  • Glucosides
  • Benzhydryl Compounds
  • Brain-Derived Neurotrophic Factor
  • Bdnf protein, rat
  • empagliflozin
  • Cyclic AMP Response Element-Binding Protein
  • Creb1 protein, rat
  • Sodium-Glucose Transporter 2 Inhibitors
  • Anticonvulsants