A Novel Platelet-Activating Factor Receptor Antagonist Inhibits Choroidal Neovascularization and Subretinal Fibrosis

PLoS One. 2013 Jun 27;8(6):e68173. doi: 10.1371/journal.pone.0068173. Print 2013.

Abstract

Choroidal neovascularization (CNV) is a critical pathogenesis in age-related macular degeneration (AMD), the most common cause of blindness in developed countries. To date, the precise molecular and cellular mechanisms underlying CNV have not been elucidated. Platelet-activating factor (PAF) has been previously implicated in angiogenesis; however, the roles of PAF and its receptor (PAF-R) in CNV have not been addressed. The present study reveals several important findings concerning the relationship of the PAF-R signaling with CNV. PAF-R was detected in a mouse model of laser-induced CNV and was upregulated during CNV development. Experimental CNV was suppressed by administering WEB2086, a novel PAF-R antagonist. WEB2086-dependent suppression of CNV occurred via the inhibition of macrophage infiltration and the expression of proangiogenic (vascular endothelial growth factor) and proinflammatory molecules (monocyte chemotactic protein-1 and IL-6) in the retinal pigment epithelium-choroid complex. Additionally, WEB2086-induced PAF-R blockage suppresses experimentally induced subretinal fibrosis, which resembles the fibrotic subretinal scarring observed in neovascular AMD. As optimal treatment modalities for neovascular AMD would target the multiple mechanisms of AMD-associated vision loss, including neovascularization, inflammation and fibrosis, our results suggest PAF-R as an attractive molecular target in the treatment of AMD.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Azepines / pharmacology*
  • Choroidal Neovascularization / drug therapy*
  • Choroidal Neovascularization / metabolism
  • Choroidal Neovascularization / pathology
  • Disease Models, Animal
  • Female
  • Fibrosis / drug therapy*
  • Fibrosis / metabolism
  • Fibrosis / pathology
  • Hematologic Agents / pharmacology*
  • Lasers
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Macrophages / pathology
  • Mice, Inbred C57BL
  • Platelet Membrane Glycoproteins / antagonists & inhibitors*
  • Platelet Membrane Glycoproteins / metabolism
  • RNA, Messenger / metabolism
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Receptors, G-Protein-Coupled / metabolism
  • Retinal Diseases / drug therapy*
  • Retinal Diseases / metabolism
  • Retinal Diseases / pathology
  • Triazoles / pharmacology*

Substances

  • Azepines
  • Hematologic Agents
  • Platelet Membrane Glycoproteins
  • RNA, Messenger
  • Receptors, G-Protein-Coupled
  • Triazoles
  • platelet activating factor receptor
  • WEB 2086

Grants and funding

This work was supported by grants C (K-H.S.) and grant-in-aid for Young Scientists (A) (A.T.) from the Ministry of Education, Science, Sports and Culture of Japan. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.