HDAC Inhibitor-Mediated Epigenetic Regulation of Glaucoma-Associated TGFβ2 in the Trabecular Meshwork

Invest Ophthalmol Vis Sci. 2016 Jul 1;57(8):3698-707. doi: 10.1167/iovs16-19446.

Abstract

Purpose: Elevated intraocular pressure (IOP) in primary open-angle glaucoma (POAG) results from glaucomatous damage to the trabecular meshwork (TM). The glaucoma-associated factor TGFβ2 is increased in aqueous humor and TM of POAG patients. We hypothesize that histone acetylation has a role in dysregulated TGFβ2 expression.

Methods: Protein acetylation was compared between nonglaucomatous TM (NTM) and glaucomatous TM (GTM) cells using Western immunoblotting (WB). Nonglaucomatous TM cells were treated with 10 nM thailandepsin-A (TDP-A), a potent histone deacetylase inhibitor for 4 days. Total and nuclear proteins, RNA, and nuclear protein-DNA complexes were harvested for WB, quantitative PCR (qPCR), and chromatin immunoprecipitation (ChIP) assays, respectively. Paired bovine eyes were perfused with TDP-A versus DMSO, or TDP-A versus TDP-A plus the TGFβ pathway inhibitor LY364947 for 5 to 9 days. Intraocular pressure, TM, and perfusate proteins were compared.

Results: We found increased acetylated histone 3 and total protein acetylation in the GTM cells and TDP-A treated NTM cells. Chromatin immunoprecipitation assays showed that TDP-A induced histone hyperacetylation associated with the TGFβ2 promoter. This change of acetylation significantly increased TGFβ2 mRNA and protein expression in NTM cells. In perfusion-cultured bovine eyes, TDP-A increased TGFβ2 in the perfusate as well as elevated IOP. Histologic and immunofluorescent analyses showed increased extracellular matrix and cytoskeletal proteins in the TM of TDP-A treated bovine eyes. Cotreatment with the TGFβ pathway inhibitor LY364947 blocked TDP-A-induced ocular hypertension.

Conclusions: Our results suggest that histone acetylation has an important role in increased expression of the glaucoma-associated factor TGFβ2. Histone hyperacetylation may be the initiator of glaucomatous damage to the TM.

MeSH terms

  • Acetylation
  • Animals
  • Cattle
  • Cells, Cultured
  • Epigenesis, Genetic / genetics*
  • Glaucoma, Open-Angle / genetics*
  • Histone Deacetylase Inhibitors / pharmacology*
  • Pyrazoles / pharmacology
  • Pyrroles / pharmacology
  • RNA, Messenger / metabolism
  • Trabecular Meshwork / physiology*
  • Transforming Growth Factor beta2 / genetics*

Substances

  • HTS 466284
  • Histone Deacetylase Inhibitors
  • Pyrazoles
  • Pyrroles
  • RNA, Messenger
  • Transforming Growth Factor beta2