Ebselen induces mitochondrial permeability transition because of its interaction with adenine nucleotide translocase

Life Sci. 2015 Oct 15:139:108-13. doi: 10.1016/j.lfs.2015.08.011. Epub 2015 Aug 24.

Abstract

Aims: Mitochondrial permeability transition is a process established through massive Ca(2+) load in addition to an inducer reagent. Ebselen (Ebs), an antioxidant seleno compound, has been introduced as a reagent which inhibits mitochondrial dysfunction induced by permeability transition. Paradoxically enough, it has been shown that Ebs may also be able to induce the opening of the mitochondrial non-selective pores. This study was performed with the purpose of establishing the membrane system involved in Ebs-induced pore opening.

Main methods: Permeability transition was appraised by analyzing the following: i) matrix Ca(2+) release, and mitochondrial swelling, ii) efflux of cytochrome c, and iii) the inhibition of superoxide dismutase. All of these adverse reactions were inhibited by N-ethylmaleimide and cyclosporin A.

Key findings: At concentrations from 5 to 20 μM, we found that Ebs induces non-specific membrane permeability. Remarkably, Ebs blocks the binding of the fluorescent reagent eosin-5-maleimide to the thiol groups of the adenine nucleotide translocase.

Significance: Based on the above, it is tempting to hypothesize that Ebs induces pore opening through its binding to the ADP/ATP carrier.

Keywords: ADP/ATP translocase; Calcium; Ebselen; Mitochondria; Permeability transition.

MeSH terms

  • Animals
  • Antioxidants / pharmacology*
  • Atractyloside
  • Azoles / pharmacology*
  • Calcium / metabolism
  • Isoindoles
  • Mitochondria / drug effects*
  • Mitochondria / metabolism
  • Mitochondrial ADP, ATP Translocases / metabolism*
  • Mitochondrial Swelling / drug effects*
  • Organoselenium Compounds / pharmacology*
  • Permeability / drug effects*
  • Rats

Substances

  • Antioxidants
  • Azoles
  • Isoindoles
  • Organoselenium Compounds
  • Atractyloside
  • ebselen
  • Mitochondrial ADP, ATP Translocases
  • Calcium