KATP Channel Blocker Glibenclamide Prevents Radiation-Induced Lung Injury and Inhibits Radiation-Induced Apoptosis of Vascular Endothelial Cells by Increased Ca2+ Influx and Subsequent PKC Activation

Radiat Res. 2020 Feb;193(2):171-185. doi: 10.1667/RR15381.1. Epub 2019 Dec 26.

Abstract

Radiation-induced lung injury (RILI) is a common and severe side effect of thoracic radiotherapy, which compromises patients' quality of life. Recent studies revealed that early vascular injury, especially microvascular damage, played a central role in the development of RILI. For this reason, early vascular protection is essential for RILI therapy. The ATP-sensitive K+ (KATP) channel is an ATP-dependent K+ channel with multiple subunits. The protective role of the KATP channel in vascular injury has been demonstrated in some published studies. In this work, we investigated the effect of KATP channel on RILI. Our findings confirmed that the KATP channel blocker glibenclamide, rather than the KATP channel opener pinacidil, remitted RILI, and in particular, provided protection against radiation-induced vascular injury. Cytology experiments verified that glibenclamide enhanced cell viability, increased the potential of proliferation after irradiation and attenuated radiation-induced apoptosis. Involved mechanisms included increased Ca2+ influx and PKC activation, which were induced by glibenclamide pretreatment. In conclusion, the KATP channel blocker glibenclamide remitted RILI and inhibited the radiation-induced apoptosis of vascular endothelial cells by increased Ca2+ influx and subsequent PKC activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Apoptosis / radiation effects
  • Biological Transport / drug effects
  • Biological Transport / radiation effects
  • Calcium / metabolism*
  • Enzyme Activation / drug effects
  • Enzyme Activation / radiation effects
  • Gene Expression Regulation / drug effects
  • Gene Expression Regulation / radiation effects
  • Glyburide / pharmacology*
  • Human Umbilical Vein Endothelial Cells / cytology
  • Human Umbilical Vein Endothelial Cells / drug effects
  • Human Umbilical Vein Endothelial Cells / radiation effects
  • Humans
  • KATP Channels / antagonists & inhibitors*
  • Lung Injury / etiology
  • Lung Injury / metabolism
  • Lung Injury / pathology
  • Lung Injury / prevention & control*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Phosphorylation / drug effects
  • Phosphorylation / radiation effects
  • Potassium Channel Blockers / pharmacology
  • Protein Kinase C / metabolism*
  • Radiation Injuries, Experimental / metabolism
  • Radiation Injuries, Experimental / pathology
  • Radiation Injuries, Experimental / prevention & control*
  • Radiation Pneumonitis / prevention & control

Substances

  • KATP Channels
  • Potassium Channel Blockers
  • Protein Kinase C
  • Glyburide
  • Calcium