Sildenafil mediates blood-flow redistribution and neuroprotection after neonatal hypoxia-ischemia

Stroke. 2014 Mar;45(3):850-6. doi: 10.1161/STROKEAHA.113.003606. Epub 2014 Jan 28.

Abstract

Background and purpose: The best conceivable treatment for hypoxia-ischemia (HI) is the restoration of blood flow to the hypoxic-ischemic region(s). Our objective was to examine whether boosting NO-cGMP signaling using sildenafil citrate, a phosphodiesterase-type 5 inhibitor, could modify cerebral blood flow and reduce lesions in the developing brain.

Methods: HI was induced in P7 Sprague-Dawley rats by unilateral carotid artery occlusion and hypoxia, and followed by either PBS or sildenafil. Blood-flow velocities were measured by ultrasound imaging with sequential Doppler recordings to evaluate collateral recruitment. Cell death, blood-brain barrier integrity, and glial activation were analyzed by immunohistochemistry. Motor behavior was evaluated using an open-field device adapted to neonatal animals.

Results: Sildenafil citrate (10 mg/kg) induced collateral patency, reduced terminal dUTP nick-end labeling-positive cells, reactive astrogliosis, and macrophage/microglial activation at 72 hours and 7 days post-HI. Sildenafil also reduced the number of terminal dUTP nick-end labeling-positive endothelial cells within lesion site. Seven days after HI and sildenafil treatment, tissue loss was significantly reduced, and animals recovered motor coordination.

Conclusions: Our findings strongly indicate that sildenafil citrate treatment, associated with a significant increase in cerebral blood flow, reduces HI damage and improves motor locomotion in neonatal rats. Sildenafil may represent an interesting therapeutic strategy for neonatal neuroprotection.

Keywords: neonatal stroke; nitric oxide; sildenafil.

MeSH terms

  • Animals
  • Animals, Newborn / physiology*
  • Blood Gas Analysis
  • Blood Pressure / drug effects
  • Blood Pressure / physiology
  • Cell Death / drug effects
  • Cerebrovascular Circulation / drug effects*
  • Cyclic GMP / physiology
  • Functional Laterality / physiology
  • Hypoxia-Ischemia, Brain / drug therapy*
  • Hypoxia-Ischemia, Brain / physiopathology
  • Hypoxia-Ischemia, Brain / psychology
  • Immunohistochemistry
  • In Situ Nick-End Labeling
  • Inflammation / pathology
  • Macrophage Activation / drug effects
  • Microcirculation / drug effects
  • Motor Activity / drug effects
  • Neuroglia / drug effects
  • Neuroprotective Agents*
  • Nitric Oxide / physiology
  • Phosphodiesterase Inhibitors / pharmacology*
  • Piperazines / pharmacology*
  • Psychomotor Performance / drug effects
  • Purines / pharmacology
  • Rats
  • Sildenafil Citrate
  • Sulfones / pharmacology*

Substances

  • Neuroprotective Agents
  • Phosphodiesterase Inhibitors
  • Piperazines
  • Purines
  • Sulfones
  • Nitric Oxide
  • Sildenafil Citrate
  • Cyclic GMP