Sildenafil reduces neuroinflammation in cerebellum, restores GABAergic tone, and improves motor in-coordination in rats with hepatic encephalopathy

CNS Neurosci Ther. 2017 May;23(5):386-394. doi: 10.1111/cns.12688. Epub 2017 Mar 11.

Abstract

Aims: Patients with liver disease may develop hepatic encephalopathy (HE), with cognitive impairment and motor in-coordination. Rats with HE due to portacaval shunts (PCS) show motor in-coordination. We hypothesized that in PCS rats: (i) Motor in-coordination would be due to enhanced GABAergic tone in cerebellum; (ii) increased GABAergic tone would be due to neuroinflammation; (iii) increasing cGMP would reduce neuroinflammation and GABAergic tone and restore motor coordination. To assess these hypotheses, we assessed if (i) treatment with sildenafil reduces neuroinflammation; (ii) reduced neuroinflammation is associated with reduced GABAergic tone and restored motor coordination.

Methods: Rats were treated with sildenafil to increase cGMP. Microglia and astrocytes activation were analyzed by immunohistochemistry, extracellular GABA by microdialysis, and motor coordination in the beam walking.

Results: PCS rats show neuroinflammation in cerebellum, with microglia and astrocytes activation, increased IL-1b and TNF-a and reduced YM-1 and IL-4. Membrane expression of the GABA transporter GAT1 is reduced, while GAT3 is increased. Extracellular GABA and motor in-coordination are increased. Sildenafil treatment eliminates neuroinflammation, microglia and astrocytes activation; changes in membrane expression of GABA transporters; and restores motor coordination.

Conclusions: This study supports an interplay between cGMP-neuroinflammation and GABAergic neurotransmission in impairing motor coordination in PCS rats.

Keywords: GABAergic neurotransmission; GAT3; cGMP, neuroinflammation; hepatic encephalopathy; sildenafil.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Astrocytes / drug effects
  • Astrocytes / pathology
  • Astrocytes / physiology
  • Cerebellum / drug effects*
  • Cerebellum / immunology
  • Cerebellum / pathology
  • Disease Models, Animal
  • GABA Plasma Membrane Transport Proteins / metabolism
  • Hepatic Encephalopathy / drug therapy*
  • Hepatic Encephalopathy / pathology
  • Hepatic Encephalopathy / physiopathology
  • Interleukin-1beta / metabolism
  • Interleukin-4 / metabolism
  • Male
  • Microglia / drug effects
  • Microglia / pathology
  • Microglia / physiology
  • Motor Skills / drug effects*
  • Motor Skills / physiology
  • Neuroimmunomodulation / drug effects
  • Neuroimmunomodulation / physiology
  • Rats, Wistar
  • Sildenafil Citrate / pharmacology*
  • Tumor Necrosis Factor-alpha / metabolism
  • gamma-Aminobutyric Acid / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • GABA Plasma Membrane Transport Proteins
  • IL1B protein, rat
  • Interleukin-1beta
  • Slc6a11 protein, rat
  • Tumor Necrosis Factor-alpha
  • Interleukin-4
  • gamma-Aminobutyric Acid
  • Sildenafil Citrate