GSK-3 beta inhibition and prevention of mitochondrial apoptosis inducing factor release are not involved in the antioxidant properties of SB-415286

Eur J Pharmacol. 2008 Jul 7;588(2-3):239-43. doi: 10.1016/j.ejphar.2008.04.019. Epub 2008 Apr 11.

Abstract

The antioxidant effects of lithium and SB-415286, two glycogen synthase kinase-3 beta (GSK-3 beta) inhibitors, were studied in cerebellar granule neurons by measuring changes in 2, 7-dichlorodihydrofluorescein diacetate (H2DCFDA) fluorescence. GSK-3 beta inhibitors inhibit apoptosis mediated by serum and potassium withdrawal (S/K withdrawal) and GSK-3 beta activation, as measured by beta-catenin degradation. Furthermore, as both drugs prevent mitochondrial apoptosis inducing factor (AIF) release, these data indicate that GSK-3 beta inhibitors prevent caspase-independent apoptosis in cerebellar granule neurons induced by S/K withdrawal. While the most specific GSK-3 beta inhibitor, SB-415286, demonstrated antioxidant effects, Li+ 10 mM did not. These results indicate that lithium 10 mM and SB-415286 20 microM exert anti-apoptotic effects in cases of S/K withdrawal mediated by GSK-3 beta inhibition. However, these antioxidant properties are independent of GSK-3 beta inhibition and prevention of mitochondrial AIF release.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminophenols / pharmacology*
  • Animals
  • Antioxidants / pharmacology*
  • Apoptosis Inducing Factor / metabolism*
  • Cells, Cultured
  • Cerebellum / drug effects*
  • Cerebellum / metabolism
  • Glycogen Synthase Kinase 3 / antagonists & inhibitors*
  • Glycogen Synthase Kinase 3 beta
  • Lithium / pharmacology
  • Maleimides / pharmacology*
  • Neuroprotective Agents / pharmacology*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • 3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
  • Aminophenols
  • Antioxidants
  • Apoptosis Inducing Factor
  • Maleimides
  • Neuroprotective Agents
  • Lithium
  • Glycogen Synthase Kinase 3 beta
  • Glycogen Synthase Kinase 3