Anti-Vascular Endothelial Growth Factors Protect Retinal Pigment Epithelium Cells Against Oxidation by Modulating Nitric Oxide Release and Autophagy

Cell Physiol Biochem. 2017;42(5):1725-1738. doi: 10.1159/000479441. Epub 2017 Jul 25.

Abstract

Background/aims: the anti-vascular endothelial growth factors (VEGF), Aflibercept and Ranibizumab, are used for the treatment of macular degeneration. Here we examined the involvement of nitric oxide (NO), mitochondria function and of apoptosis/autophagy in their antioxidant effects in human retinal pigment epithelium cells (RPE).

Methods: RPE were exposed to Ranibizumab/Aflibercept in the absence or presence of NO synthase (NOS) inhibitor and of autophagy activator/blocker, rapamicyn/3-methyladenine. Specific kits were used for cell viability, NO and reactive oxygen species detection and mitochondrial membrane potential measurement, whereas Western Blot was performed for apoptosis/ autophagy markers and other kinases detection.

Results: In RPE cultured in physiological conditions, Aflibercept/Ranibizumab increased NO release in a dose and time-dependent way. Opposite results were obtained in RPE pretreated with hydrogen peroxide. Moreover, both the anti-VEGF agents were able to prevent the fall of cell viability and of mitochondrial membrane potential. Those effects were reduced by the NOS inhibitor and 3-methyladenine and were potentiated by rapamycin. Finally, Aflibercept and Ranibizumab counteracted the changes of apoptosis/autophagy markers, NOS, Phosphatidylinositol-3-Kinase/Protein Kinase B and Extracellular signal-regulated kinases 1/2 caused by peroxidation.

Conclusion: Aflibercept and Ranibizumab protect RPE against peroxidation through the modulation of NO release, apoptosis and autophagy.

Keywords: Anti-VEGF; Cell viability; Mitochondria; Peroxidation.

MeSH terms

  • Adenine / analogs & derivatives
  • Adenine / toxicity
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Apoptosis / drug effects
  • Autophagy / drug effects*
  • Cell Line
  • Cell Proliferation / drug effects
  • Hydrogen Peroxide / toxicity
  • Membrane Potential, Mitochondrial / drug effects
  • Nitric Oxide / metabolism*
  • Nitric Oxide Synthase / antagonists & inhibitors
  • Nitric Oxide Synthase / genetics
  • Nitric Oxide Synthase / metabolism
  • Oxidative Stress / drug effects
  • Proto-Oncogene Proteins c-akt / metabolism
  • Ranibizumab / pharmacology*
  • Reactive Oxygen Species / metabolism
  • Receptors, Vascular Endothelial Growth Factor
  • Recombinant Fusion Proteins / pharmacology*
  • Retinal Pigment Epithelium / cytology
  • Retinal Pigment Epithelium / drug effects
  • Retinal Pigment Epithelium / metabolism
  • Sirolimus / toxicity
  • Swine

Substances

  • Angiogenesis Inhibitors
  • Reactive Oxygen Species
  • Recombinant Fusion Proteins
  • aflibercept
  • Nitric Oxide
  • 3-methyladenine
  • Hydrogen Peroxide
  • Nitric Oxide Synthase
  • Receptors, Vascular Endothelial Growth Factor
  • Proto-Oncogene Proteins c-akt
  • Adenine
  • Sirolimus
  • Ranibizumab