Inhibiting mitochondrial permeability transition pore opening: a new paradigm for myocardial preconditioning?

Cardiovasc Res. 2002 Aug 15;55(3):534-43. doi: 10.1016/s0008-6363(02)00455-8.

Abstract

Objective: We propose that ischemic preconditioning (IPC) and mitochondrial K(ATP) channel activation protect the myocardium by inhibiting mitochondrial permeability transition pore (MPTP) opening at reperfusion.

Methods: Isolated rat hearts were subjected to 35 min ischemia/120 min reperfusion and assigned to the following groups: (1) control; (2) IPC of 2x5 min each of preceding global ischemia; (3,4,5) 0.2 micromol/l cyclosporin A (CsA, which inhibits MPTP opening), 5 micromol/l FK506 (which inhibits the phosphatase calcineurin without inhibiting MPTP opening), or 20 micromol/l atractyloside (Atr, a MPTP opener) given at reperfusion; (6,7) pre-treatment with 30 micromol/l diazoxide (Diaz, a mitochondrial K(ATP) channel opener) or 200 nmol/l 2 chloro-N(6)-cyclopentyl-adenosine (CCPA, an adenosine A1 receptor agonist); (8) IPC+Atr; (9) Diaz+Atr; (10) CCPA+Atr. The effect of mitochondrial K(ATP) channel activation on calcium-induced MPTP opening in isolated calcein-loaded mitochondria was also assessed.

Results: IPC, CsA when given at reperfusion, and pre-treatment with diazoxide or CCPA all limited infarct size (19.9+/-2.6% in IPC; 24.6+/-1.9% in CsA, 18.0+/-1.7% in Diaz, 20.4+/-3.3% in CCPA vs. 44.7+/-2.0% in control, P<0.0001). Opening the MPTP with atractyloside at reperfusion abolished this cardio-protective effect (47.7+/-1.8% in IPC+Atr, 42.3+/-3.2% in Diaz+Atr, 51.2+/-1.6% in CCPA+Atr). Atractyloside and FK506, given at reperfusion, did not influence infarct size (45.7+/-2.1% in Atr and 43.1+/-3.6% in FK506 vs. 44.7+/-2.0% in control, P=NS). Diazoxide (30 micromol/l) was shown to reduce calcium-induced MPTP opening by 52.5+/-8.0% in calcein-loaded mitochondria. 5-Hydroxydecanoic acid (100 micromol/l) was able to abolish the cardio-protective effects of both diazoxide and IPC.

Conclusion: One interpretation of these data is that IPC and mitochondrial K(ATP) channel activation may protect the myocardium by inhibiting MPTP opening at reperfusion.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives
  • Adenosine / pharmacology
  • Analysis of Variance
  • Animals
  • Atractyloside / pharmacology
  • Calcineurin Inhibitors
  • Cyclosporine / pharmacology*
  • Decanoic Acids / pharmacology
  • Diazoxide / pharmacology
  • Enzyme Inhibitors / pharmacology
  • Hydroxy Acids / pharmacology
  • Ion Channels / drug effects*
  • Ischemic Preconditioning, Myocardial / methods*
  • Male
  • Mitochondria, Heart / metabolism*
  • Mitochondrial Membrane Transport Proteins
  • Mitochondrial Permeability Transition Pore
  • Myocardial Ischemia / metabolism*
  • Myocardial Reperfusion Injury / metabolism
  • Perfusion
  • Permeability
  • Potassium Channel Blockers / pharmacology
  • Potassium Channels / drug effects
  • Potassium Channels, Calcium-Activated / metabolism
  • Purinergic P1 Receptor Agonists
  • Random Allocation
  • Rats
  • Rats, Sprague-Dawley
  • Tacrolimus / pharmacology

Substances

  • Calcineurin Inhibitors
  • Decanoic Acids
  • Enzyme Inhibitors
  • Hydroxy Acids
  • Ion Channels
  • Mitochondrial Membrane Transport Proteins
  • Mitochondrial Permeability Transition Pore
  • Potassium Channel Blockers
  • Potassium Channels
  • Potassium Channels, Calcium-Activated
  • Purinergic P1 Receptor Agonists
  • Atractyloside
  • 2-chloro-N(6)cyclopentyladenosine
  • 5-hydroxydecanoic acid
  • Cyclosporine
  • Adenosine
  • Diazoxide
  • Tacrolimus