Dexmedetomidine protects H9c2 cardiomyocytes against oxygen-glucose deprivation/reoxygenation-induced intracellular calcium overload and apoptosis through regulating FKBP12.6/RyR2 signaling

Drug Des Devel Ther. 2019 Sep 2:13:3137-3149. doi: 10.2147/DDDT.S219533. eCollection 2019.

Abstract

Purpose: Intracellular calcium ([Ca2+]i) overload is a major cause of cell injury during myocardial ischemia/reperfusion (I/R). Dexmedetomidine (DEX) has been shown to exert anti-inflammatory and organ protective effects. This study aimed to investigate whether pretreatment with DEX could protect H9c2 cardiomyocytes against oxygen-glucose deprivation/reoxygenation (OGD/R) injury through regulating the Ca2+ signaling.

Methods: H9c2 cardiomyocytes were subjected to OGD for 12 h, followed by 3 h of reoxygenation. DEX was administered 1 h prior to OGD/R. Cell viability, lactate dehydrogenase (LDH) release, level of [Ca2+]i, cell apoptosis, and the expression of 12.6-kd FK506-binding protein/ryanodine receptor 2 (FKBP12.6/RyR2) and caspase-3 were assessed.

Results: Cells exposed to OGD/R had decreased cell viability, increased LDH release, elevated [Ca2+]i level and apoptosis rate, down-regulated expression of FKBP12.6, and up-regulated expression of phosphorylated-Ser2814-RyR2 and cleaved caspase-3. Pretreatment with DEX significantly blocked the above-mentioned changes, alleviating the OGD/R-induced injury in H9c2 cells. Moreover, knockdown of FKBP12.6 by small interfering RNA abolished the protective effects of DEX.

Conclusion: This study indicates that DEX pretreatment protects the cardiomyocytes against OGD/R-induced injury by inhibiting [Ca2+]i overload and cell apoptosis via regulating the FKBP12.6/RyR2 signaling. DEX may be used for preventing cardiac I/R injury in the clinical settings.

Keywords: H9c2 cardiomyocytes; apoptosis; dexmedetomidine; intracellular calcium overload, FKBP12.6/RyR2; oxygen-glucose deprivation/reoxygenation.

MeSH terms

  • Adrenergic alpha-2 Receptor Agonists / pharmacology*
  • Apoptosis / drug effects*
  • Calcium / administration & dosage
  • Calcium / analysis
  • Calcium / metabolism*
  • Cell Survival / drug effects
  • Cells, Cultured
  • Dexmedetomidine / pharmacology*
  • Dose-Response Relationship, Drug
  • Glucose / metabolism
  • Humans
  • Myocytes, Cardiac / drug effects*
  • Myocytes, Cardiac / metabolism
  • Oxygen / metabolism*
  • Ryanodine Receptor Calcium Release Channel / genetics
  • Ryanodine Receptor Calcium Release Channel / metabolism*
  • Signal Transduction / drug effects
  • Structure-Activity Relationship
  • Tacrolimus Binding Proteins / antagonists & inhibitors*
  • Tacrolimus Binding Proteins / genetics
  • Tacrolimus Binding Proteins / metabolism

Substances

  • Adrenergic alpha-2 Receptor Agonists
  • FKBP12.6 protein, mouse
  • RyR2 protein, human
  • Ryanodine Receptor Calcium Release Channel
  • Dexmedetomidine
  • Tacrolimus Binding Proteins
  • Glucose
  • Oxygen
  • Calcium