Phosphatidylinositol 3-kinase inhibitor failed to reduce cerebral vasospasm in dog model of experimental subarachnoid hemorrhage

Stroke. 2002 Feb;33(2):593-9. doi: 10.1161/hs0202.103398.

Abstract

Background and purpose: Phosphatidylinositol 3-kinase (PI3-kinase) is involved in smooth muscle contraction induced by growth factors and/or G protein-coupled receptor agonists. To evaluate the role of PI3-kinase in the pathogenesis of delayed vasospasm, we applied 2 PI3-kinase inhibitors to an established canine double-hemorrhage model of experimental subarachnoid hemorrhage.

Methods: Twenty-four dogs underwent double blood injections via the cisterna magna on days 0 and 2. The dogs were killed on day 7. Dogs were treated with either vehicle (dimethyl sulfoxide), wortmannin, or LY294002 once per day on day 2 through day 6. Angiography was performed before blood injection and before the dogs were killed. The basilar arteries were collected for morphology, Western blot analysis, and PI3-kinase activity.

Results: The residual diameter of the basilar arteries in the dimethyl sulfoxide treatment group, which was compared with day 0 angiogram, decreased markedly on day 7 (the percentage of the residual diameter was 47.8+/-0.8%). Wortmannin and LY294002 did not significantly change residual diameter on day 7. Both PI3-kinase inhibitors abolished PI3-kinase activity compared with the vehicle treatment group. However, both PI3-kinase inhibitors failed to significantly attenuate PI3-kinase protein expression (Western blot) (P>0.05, ANOVA).

Conclusions: Delayed treatment, which was to mimic the clinical situation, with PI3-kinase inhibitors failed to reverse vasospasm. PI3-kinase may not play an important role in the delayed vasospasm. The possible effect of PI3-kinase inhibitors in the early stage of vasospasm was not investigated in the present study.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androstadienes / pharmacology
  • Animals
  • Basilar Artery / drug effects
  • Basilar Artery / pathology
  • Blotting, Western
  • Brain / drug effects
  • Brain / pathology
  • Brain / physiopathology
  • Cerebral Angiography
  • Chromones / pharmacology
  • Disease Models, Animal
  • Dogs
  • Enzyme Inhibitors / pharmacology*
  • Morpholines / pharmacology
  • Phosphatidylinositol 3-Kinases / analysis
  • Phosphoinositide-3 Kinase Inhibitors*
  • Subarachnoid Hemorrhage / complications
  • Subarachnoid Hemorrhage / drug therapy*
  • Subarachnoid Hemorrhage / pathology
  • Subarachnoid Hemorrhage / physiopathology
  • Treatment Failure
  • Vascular Patency / drug effects
  • Vasospasm, Intracranial / drug therapy*
  • Vasospasm, Intracranial / etiology
  • Vasospasm, Intracranial / pathology
  • Vasospasm, Intracranial / physiopathology
  • Wortmannin

Substances

  • Androstadienes
  • Chromones
  • Enzyme Inhibitors
  • Morpholines
  • Phosphoinositide-3 Kinase Inhibitors
  • 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
  • Wortmannin