A selective phosphodiesterase-4 inhibitor reduces leukocyte infiltration, oxidative processes, and tissue damage after spinal cord injury

J Neurotrauma. 2011 Jun;28(6):1035-49. doi: 10.1089/neu.2010.1575. Epub 2011 May 5.

Abstract

We tested the hypothesis that a selective phosphodiesterase type 4 inhibitor (PDE4-I; IC486051) would attenuate early inflammatory and oxidative processes following spinal cord injury (SCI) when delivered during the first 3 days after injury. Rats receiving a moderately severe thoracic-clip-compression SCI were treated with the PDE4-I (0.5, 1.0, and 3.0 mg/kg IV) in bolus doses from 2-60 h post-injury. Doses at 0.5 mg/kg and 1.0 mg/kg significantly decreased myeloperoxidase (MPO) enzymatic activity (neutrophils), expression of a neutrophil-associated protein and of ED-1 (macrophages), and estimates of lipid peroxidation in cord lesion homogenates at 24 h and 72 h post-injury by 25-40%. The 3.0 mg/kg dose had small or no effects on these measures. The PDE4-I treatment (0.5 or 1.0 mg/kg) reduced expression of the oxidative enzymes gp91(phox), inducible nitric oxide synthase, and cyclooxygenase-2, and diminished free radical generation by up to 40%. Treatment with 0.5 mg/kg PDE4-I improved motor function (as assessed by the Basso-Beattie-Bresnahan scale) significantly from 4-8 weeks after SCI (average difference 1.3 points). Mechanical allodynia elicited from the hindpaw decreased by up to 25%. The PDE4-I treatment also increased white matter volume near the lesion at 8 weeks after SCI. In conclusion, the PDE4-I reduced key markers of oxidative stress and leukocyte infiltration, producing cellular protection, locomotor improvements, and a reduction in neuropathic pain. Early inhibition of PDE4 is neuroprotective after SCI when given acutely and briefly at sufficient doses.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chemotaxis, Leukocyte / drug effects*
  • Chemotaxis, Leukocyte / physiology
  • Cyclic Nucleotide Phosphodiesterases, Type 4 / metabolism
  • Disease Models, Animal
  • Female
  • Male
  • Myelitis / drug therapy
  • Myelitis / enzymology
  • Myelitis / pathology
  • Nerve Degeneration / enzymology
  • Nerve Degeneration / pathology
  • Nerve Degeneration / prevention & control*
  • Neuroprotective Agents / pharmacology*
  • Oxidative Stress / drug effects*
  • Oxidative Stress / physiology
  • Phosphodiesterase 4 Inhibitors / pharmacology*
  • Phosphodiesterase 4 Inhibitors / therapeutic use
  • Rats
  • Rats, Wistar
  • Spinal Cord Injuries / drug therapy*
  • Spinal Cord Injuries / enzymology
  • Spinal Cord Injuries / pathology

Substances

  • Neuroprotective Agents
  • Phosphodiesterase 4 Inhibitors
  • Cyclic Nucleotide Phosphodiesterases, Type 4