Study of the protective effect of calcium channel blockers against neuronal damage induced by glutamate in cultured hippocampal neurons

Pharmacol Rep. 2013;65(3):730-6. doi: 10.1016/s1734-1140(13)71052-1.

Abstract

Background: The aim of this study was to examine the putative protective effect of calcium channel blockers on hippocampal neurons in the experimental model of excitotoxic damage.

Methods: Seven-day old primary dissociated cultures of rat hippocampal neural cells containing one of the following calcium channel blockers: cinnarizine, flunarizine or nimodipine were exposed to glutamate-induced injury. Quantitative assessments of neuronal injury were accomplished by measuring lactate dehydrogenase (LDH) activity in the media 24 h after exposure to glutamate and by counting and establishing the apoptotic and necrotic cells in flow cytometry with Annexin V-FITC/PI staining.

Results: In our experiment, glutamate induced a 339% elevation of apoptotic cells and a 289% increase of necrotic cells in hippocampal neurons as compared to control cultures without drugs. In cultures containing flunarizine, glutamate-induced cell apoptosis was suppressed by 62% while necrosis showed no significant alternation. Cinnarizine exerted no anti-apoptotic effects on glutamate-injured cultured hippocampal neurons, while nimodipine intensified the apoptotic pathway of cell death and promoted an increase in the number of apoptotic neurons by 26%. When cinnarizine or nimodipine were used, the percentage of necrotic cells was significantly lower when compared with glutamate-injured cultures and it amounted to 44% and 24% for cinnarizine and nimodipine, respectively.

Conclusions: The obtained results suggest the beneficial anti-apoptotic potential of flunarizine and the anti-necrotic potential of cinnarizine against glutamate-induced death of cultured hippocampal neurons. Nimodipine can protect neurons against necrosis, but has an intensified adverse pro-apoptotic effect on cultured neurons in the experimental model of excitotoxic injury.

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Calcium Channel Blockers / pharmacology*
  • Cell Death / drug effects
  • Cells, Cultured
  • Glutamic Acid / adverse effects*
  • Glutamic Acid / metabolism
  • Hippocampus / drug effects*
  • Hippocampus / metabolism
  • L-Lactate Dehydrogenase / metabolism
  • Necrosis / drug therapy
  • Necrosis / metabolism
  • Nervous System Diseases / drug therapy*
  • Nervous System Diseases / metabolism
  • Neurons / drug effects*
  • Neurons / metabolism
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Calcium Channel Blockers
  • Glutamic Acid
  • L-Lactate Dehydrogenase