Blood-retinal barrier protection against high glucose damage: The role of P2X7 receptor

Biochem Pharmacol. 2019 Oct:168:249-258. doi: 10.1016/j.bcp.2019.07.010. Epub 2019 Jul 11.

Abstract

Blood retinal barrier (BRB) breakdown is a hallmark of diabetic retinopathy, whose occurrence in early or later phases of the disease has not yet been completely clarified. Recent evidence suggests that hyperglycemia induces activation of the P2X7 receptor (P2X7R) leading to pericyte cell death. We herein investigated the role of P2X7R on retinal endothelial cells viability and expression of tight- and adherens-junctions following high glucose (HG) exposure. We found that HG elicited P2X7R activation and expression and release of the pro-inflammatory cytokine IL-1β in human retinal endothelial cells (HRECs). Furthermore, HG exposure caused a decrease in HRECs viability and a damage of the BRB. JNJ47965567, a P2X7R antagonist, protected HRECs from HG-induced damage (LDH release) and preserved the BRB, as shown by transendothelial electrical resistance and cell junction morphology (ZO-1, claudin-5 and VE-cadherin). Moreover, JNJ47965567 treatment significantly decreased IL-1β expression and release, elicited by HG. These data indicate that P2X7R plays an important role to regulate BRB integrity, in particular the block of this receptor was useful to counteract the damage elicited by HG in HRECs, and warranting further clinical evaluation of P2X7R antagonists for the treatment of diabetic macular edema.

Keywords: Blood retinal barrier; Diabetic retinopathy; Interleukin-1; P2X7 receptor antagonist; Purinergic receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Blood-Retinal Barrier / drug effects
  • Blood-Retinal Barrier / metabolism*
  • Cell Line
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism*
  • Glucose / toxicity*
  • Humans
  • Niacinamide / analogs & derivatives
  • Niacinamide / pharmacology
  • Piperazines / pharmacology
  • Receptors, Purinergic P2X7 / physiology*
  • Retina / cytology
  • Retina / drug effects
  • Retina / metabolism*
  • Tight Junctions / drug effects
  • Tight Junctions / metabolism

Substances

  • JNJ-47965567
  • P2RX7 protein, human
  • Piperazines
  • Receptors, Purinergic P2X7
  • Niacinamide
  • Glucose