Membrane ion transport systems during oxidative stress in rodent brain: protective effect of stobadine and other antioxidants

Life Sci. 1999;65(18-19):1951-8. doi: 10.1016/s0024-3205(99)00454-3.

Abstract

The effect of oxidative stress in vitro induced by radical generating systems (RGS) (Fe2+-EDTA and Fe2+-EDTA plus H2O2) on synaptosomal and microsomal ion transport systems as well as on the membrane fluidity was investigated. Oxidative insult reduced Na+, K+-ATPase activity by 50.7% and Na+-dependent Ca2+ uptake measured in choline media by 46.7%. Membrane fluidity was also significantly reduced as observed with the fluorescent probe. Stobadine (ST) prevented the decrease in membrane fluidity and Na+-dependent Ca2+ uptake, however Na+, K+-ATPase activity was only partially protected, indicating a more complex mechanism of inhibition. Incubation of microsomes with RGS led to the loss of ability of membranes to sequester Ca2+, as well as to the decrease of Ca2+-ATPase activity and to the increase of Ca2+ permeability to 125.1%. The relative potency of the two RGS to decrease membrane fluidity correlated well with the system's potencies to induce lipid peroxidation. The extent of protection against depression of Ca2+ uptake values and Ca2+-ATPase activity by membrane soluble antioxidants (U-74500A, U-83836E, t-butylated hydroxytoluene-BHT and ST) was dependent on the experimental conditions and on the dose and nature of antioxidant used. ST seems to be at least as affective as BHT and 21-aminosteroids, and more potent than tocopherol acetate. Water soluble glutathione had no significant effect on the RGS induced inhibition of Ca2+-ATPase activity. Combination of ST with glutathione enhanced ST antioxidant efficacy, so drug combination might be beneficial therapeutically.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / pharmacology*
  • Biological Transport, Active / drug effects
  • Brain / drug effects*
  • Brain / metabolism
  • Calcium / metabolism
  • Carbolines / pharmacology*
  • Endoplasmic Reticulum / drug effects
  • Endoplasmic Reticulum / enzymology
  • Endoplasmic Reticulum / metabolism
  • Gerbillinae
  • In Vitro Techniques
  • Lipid Peroxidation / drug effects
  • Membrane Fluidity / drug effects
  • Microsomes / drug effects
  • Microsomes / metabolism
  • Neuroprotective Agents / pharmacology*
  • Oxidative Stress / drug effects
  • Oxidative Stress / physiology*
  • Prosencephalon / metabolism
  • Prosencephalon / ultrastructure
  • Rabbits
  • Reactive Oxygen Species / metabolism
  • Reticular Formation / drug effects
  • Reticular Formation / enzymology
  • Reticular Formation / metabolism
  • Sodium-Calcium Exchanger / antagonists & inhibitors
  • Sodium-Calcium Exchanger / metabolism
  • Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors
  • Sodium-Potassium-Exchanging ATPase / metabolism
  • Synaptosomes / drug effects
  • Synaptosomes / enzymology
  • Synaptosomes / metabolism

Substances

  • Antioxidants
  • Carbolines
  • Neuroprotective Agents
  • Reactive Oxygen Species
  • Sodium-Calcium Exchanger
  • Sodium-Potassium-Exchanging ATPase
  • Calcium
  • dicarbine