Vericiguat attenuates doxorubicin-induced cardiotoxicity through the PRKG1/PINK1/STING axis

Transl Res. 2024 Nov:273:90-103. doi: 10.1016/j.trsl.2024.07.005. Epub 2024 Jul 24.

Abstract

Doxorubicin (DOX) is restricted due to its severe cardiotoxicity. There is still a lack of viable and effective drugs to prevent or treat DOX-induced cardiotoxicity(DIC). Vericiguat is widely used to treat heart failure with reduced ejection fraction. However, it is not clear whether vericiguat can improve DIC. In the present study, we constructed a DIC model using mice and neonatal rat cardiomyocytes and found that vericiguat ameliorated DOX-induced cardiac insufficiency in mice, restored DOX-induced mitochondrial dysfunction in neonatal rat cardiomyocytes, and inhibited the expression of inflammatory factors. Further studies showed that vericiguat improved mitochondrial dysfunction and reduced mtDNA leakage into the cytoplasm by up-regulating PRKG1, which activated PINK1 and then inhibited the STING/IRF3 pathway to alleviate DIC. These findings demonstrate for the first time that vericiguat has therapeutic potential for the treatment of DIC.

Keywords: Cardiotoxicity; Doxorubicin; Inflammation; Mitochondrial dysfunction; Vericiguat.

MeSH terms

  • Animals
  • Cardiotoxicity* / etiology
  • Cardiotoxicity* / prevention & control
  • Doxorubicin* / adverse effects
  • Doxorubicin* / toxicity
  • Male
  • Membrane Proteins* / genetics
  • Membrane Proteins* / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Myocytes, Cardiac* / drug effects
  • Myocytes, Cardiac* / metabolism
  • Myocytes, Cardiac* / pathology
  • Protein Kinases* / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Signal Transduction / drug effects

Substances

  • Doxorubicin
  • PTEN-induced putative kinase
  • Membrane Proteins
  • Protein Kinases
  • Sting1 protein, mouse