Ibudilast attenuates astrocyte apoptosis via cyclic GMP signalling pathway in an in vitro reperfusion model

Br J Pharmacol. 2001 Jul;133(6):841-8. doi: 10.1038/sj.bjp.0704146.

Abstract

We examined the effect of 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine (ibudilast), which has been clinically used for bronchial asthma and cerebrovascular disorders, on cell viability induced in a model of reperfusion injury. Ibudilast at 10 - 100 microM significantly attenuated the H(2)O(2)-induced decrease in cell viability. Ibudilast inhibited the H(2)O(2)-induced cytochrome c release, caspase-3 activation, DNA ladder formation and nuclear condensation, suggesting its anti-apoptotic effect. Phosphodiesterase inhibitors such as theophylline, pentoxyfylline, vinpocetine, dipyridamole and zaprinast, which increased the guanosine-3',5'-cyclic monophosphate (cyclic GMP) level, and dibutyryl cyclic GMP attenuated the H(2)O(2)-induced injury in astrocytes. Ibudilast increased the cyclic GMP level in astrocytes. The cyclic GMP-dependent protein kinase inhibitor KT5823 blocked the protective effects of ibudilast and dipyridamole on the H(2)O(2)-induced decrease in cell viability, while the cyclic AMP-dependent protein kinase inhibitor KT5720, the cyclic AMP antagonist Rp-cyclic AMPS, the mitogen-activated protein/extracellular signal-regulated kinase inhibitor PD98059 and the leukotriene D(4) antagonist LY 171883 did not. KT5823 also blocked the effect of ibudilast on the H(2)O(2)-induced cytochrome c release and caspase-3-like protease activation. These findings suggest that ibudilast prevents the H(2)O(2)-induced delayed apoptosis of astrocytes via a cyclic GMP, but not cyclic AMP, signalling pathway.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / pharmacology
  • Animals
  • Animals, Newborn
  • Apoptosis / drug effects*
  • Astrocytes / cytology
  • Astrocytes / drug effects*
  • Astrocytes / metabolism
  • Carbazoles*
  • Cell Survival / drug effects
  • Cyclic GMP / metabolism*
  • Cyclic GMP-Dependent Protein Kinases / antagonists & inhibitors
  • Cytochrome c Group / drug effects
  • Cytochrome c Group / metabolism
  • DNA / drug effects
  • DNA / genetics
  • DNA / metabolism
  • Dipyridamole / pharmacology
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology
  • Hydrogen Peroxide / pharmacology
  • Indoles*
  • Mitochondria / drug effects
  • Mitochondria / metabolism
  • Pentoxifylline / pharmacology
  • Peptide Hydrolases / drug effects
  • Peptide Hydrolases / metabolism
  • Phosphodiesterase Inhibitors / pharmacology
  • Purinones / pharmacology
  • Pyridines / pharmacology*
  • Rats
  • Rats, Wistar
  • Reperfusion Injury
  • Signal Transduction
  • Theophylline / pharmacology
  • Vinca Alkaloids / pharmacology

Substances

  • Alkaloids
  • Carbazoles
  • Cytochrome c Group
  • Enzyme Inhibitors
  • Indoles
  • Phosphodiesterase Inhibitors
  • Purinones
  • Pyridines
  • Vinca Alkaloids
  • KT 5823
  • vinpocetine
  • Dipyridamole
  • DNA
  • Hydrogen Peroxide
  • Theophylline
  • Cyclic GMP-Dependent Protein Kinases
  • Peptide Hydrolases
  • DEVDase
  • zaprinast
  • Cyclic GMP
  • ibudilast
  • Pentoxifylline