Antifibrotic activity of bevacizumab on human Tenon's fibroblasts in vitro

Invest Ophthalmol Vis Sci. 2010 Dec;51(12):6524-32. doi: 10.1167/iovs.10-5669. Epub 2010 Jun 23.

Abstract

Purpose: To evaluate the effect of the anti-VEGF-A monoclonal antibody bevacizumab on primary human Tenon's capsule fibroblasts (HTFs) in an in vitro model of wound healing.

Methods: Fibroblasts were cultured in RPMI media, and bevacizumab was administered at a concentration ranging from 0.25 to 12.5 mg/mL. Fibroblast viability and cell death were assessed using the MTT colorimetric assay, lactate dehydrogenase assay, BrdU assay, and live/dead assay. Fibroblast contractility was assessed in floating collagen gels. Morphologic changes were assessed by transmission electron microscopy. Antifibrosis activities were compared with 5-fluorouracil.

Results: Bevacizumab induced a significant dose-related reduction of HTF cell number at 12.5 mg/mL at 72 hours (P < 0.05). Under serum-free conditions, bevacizumab induced significant fibroblast cell death at concentrations greater than 7.5 mg/mL (P < 0.05). Bevacizumab caused a moderate inhibition of fibroblast gel contraction from baseline (P < 0.05). Scanning electron microscopy revealed marked vacuolization in bevacizumab-treated fibroblasts.

Conclusions: Bevacizumab disrupted fibroblast proliferation, inhibited collagen gel contraction ability, and induced fibroblast cell death at concentrations greater than 7.5 mg/mL in serum-free conditions. These results demonstrated that bevacizumab inhibited a number of fibrosis activities in culture. These activities may underpin the antifibrosis effect proposed in vivo.

MeSH terms

  • Angiogenesis Inhibitors / pharmacology*
  • Antibodies, Monoclonal / pharmacology*
  • Antibodies, Monoclonal, Humanized
  • Apoptosis / drug effects*
  • Bevacizumab
  • Cell Count
  • Cell Proliferation / drug effects*
  • Cells, Cultured
  • DNA / biosynthesis
  • Dose-Response Relationship, Drug
  • Fibroblasts / drug effects*
  • Fibroblasts / ultrastructure
  • Humans
  • L-Lactate Dehydrogenase / metabolism
  • Microscopy, Electron
  • Microscopy, Fluorescence
  • Tenon Capsule / drug effects*
  • Tenon Capsule / ultrastructure
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors*
  • Wound Healing / drug effects

Substances

  • Angiogenesis Inhibitors
  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • VEGFA protein, human
  • Vascular Endothelial Growth Factor A
  • Bevacizumab
  • DNA
  • L-Lactate Dehydrogenase