Tranexamic acid suppresses the release of mitochondrial DNA, protects the endothelial monolayer and enhances oxidative phosphorylation

J Cell Physiol. 2019 Nov;234(11):19121-19129. doi: 10.1002/jcp.28603. Epub 2019 Apr 2.

Abstract

Damage-associated molecular patterns, including mitochondrial DNA (mtDNA) are released during hemorrhage resulting in the development of endotheliopathy. Tranexamic acid (TXA), an antifibrinolytic drug used in hemorrhaging patients, enhances their survival despite the lack of a comprehensive understanding of its cellular mechanisms of action. The present study is aimed to elucidate these mechanisms, with a focus on mitochondria. We found that TXA inhibits the release of endogenous mtDNA from granulocytes and endothelial cells. Furthermore, TXA attenuates the loss of the endothelial monolayer integrity induced by exogenous mtDNA. Using the Seahorse XF technology, it was demonstrated that TXA strongly stimulates mitochondrial respiration. Studies using Mitotracker dye, cells derived from mito-QC mice, and the ActivSignal IPAD assay, indicate that TXA stimulates biogenesis of mitochondria and inhibits mitophagy. These findings open the potential for improvement of the strategies of TXA applications in trauma patients and the development of more efficient TXA derivatives.

Keywords: endothelial cell; mitochondria; mitochondrial DNA; mitophagy; tranexamic acid.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • DNA Damage / drug effects
  • DNA, Mitochondrial / drug effects*
  • Endothelial Cells / drug effects
  • Granulocytes / drug effects
  • Hemorrhage / drug therapy*
  • Hemorrhage / genetics
  • Hemorrhage / pathology
  • Humans
  • Mice
  • Mitochondria / drug effects
  • Mitophagy / drug effects
  • Oxidative Phosphorylation / drug effects
  • Tranexamic Acid / pharmacology*
  • Wounds and Injuries / drug therapy*
  • Wounds and Injuries / genetics
  • Wounds and Injuries / pathology

Substances

  • DNA, Mitochondrial
  • Tranexamic Acid