Nobiletin suppresses oxidative stress and apoptosis in H9c2 cardiomyocytes following hypoxia/reoxygenation injury

Eur J Pharmacol. 2019 Jul 5:854:48-53. doi: 10.1016/j.ejphar.2019.03.056. Epub 2019 Apr 3.

Abstract

Nobiletin (3',4',5,6,7,8-hexamethoxyflavone), a dietary polymethoxylated flavonoid found in Citrus fruits, was reported to exhibit protective activity against ischemia/reperfusion (I/R). However, the role of nobiletin in myocardial I/R injury remains unclear. This study was designed to examine the cardioprotective effect of nobiletin from myocardial hypoxia/reoxygenation (H/R) injury in vitro, and to explore the potential molecular mechanisms. Our results showed that nobiletin improved cell viability in H9c2 cells after H/R treatment. In addition, nobiletin significantly inhibited the production of reactive oxygen species and malondialdehyde (MDA), cell apoptosis, as well as suppressed the levels of pro-inflammatory factors in H/R-stimulated H9c2 cells. Furthermore, we observed that pretreatment with nobiletin significantly activated the Akt/GSK-3β signaling pathway in H/R-stimulated H9c2 cells. Taken together, these findings demonstrated that nobiletin attenuates myocardial I/R injury via the activation of Akt/GSK-3β pathway in H9c2 cardiomyocytes. Thus, nobiletin may be regarded as a promising drug for the prevention of myocardial I/R injury and ischemic heart disease.

Keywords: Akt/GSK-3β pathway; Apoptosis; Hypoxia/reoxygenation (H/R); Nobiletin.

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Cell Hypoxia / drug effects
  • Cell Line
  • Cell Survival / drug effects
  • Cytoprotection / drug effects
  • Flavones / pharmacology*
  • Glycogen Synthase Kinase 3 beta / metabolism
  • Interleukin-1beta / biosynthesis
  • Interleukin-6 / biosynthesis
  • Myocardial Reperfusion Injury / pathology*
  • Myocytes, Cardiac / drug effects*
  • Myocytes, Cardiac / metabolism
  • Myocytes, Cardiac / pathology*
  • Oxidative Stress / drug effects*
  • Proto-Oncogene Proteins c-akt / metabolism
  • Rats
  • Signal Transduction / drug effects
  • Tumor Necrosis Factor-alpha / biosynthesis

Substances

  • Flavones
  • Interleukin-1beta
  • Interleukin-6
  • Tumor Necrosis Factor-alpha
  • nobiletin
  • Glycogen Synthase Kinase 3 beta
  • Proto-Oncogene Proteins c-akt