A novel histone deacetylase 6-selective inhibitor suppresses synovial inflammation and joint destruction in a collagen antibody-induced arthritis mouse model

Int J Rheum Dis. 2015 Jun;18(5):514-23. doi: 10.1111/1756-185X.12501. Epub 2014 Dec 20.

Abstract

Aim: To investigate the effects of Tubastatin A, a selective histone deacetylase-6 inhibitor, on synovial inflammation and joint destruction in a collagen antibody-induced arthritis (CAIA) mouse model.

Methods: Collagen antibody-induced arthritis mice were given daily intraperitoneal injections of various concentrations of Tubastatin A (0, 10, 50, 100 mg/kg). The clinical score and paw thickness were measured. Mice were sacrificed on day 15, and the expression of tumor necrosis factor (TNF)-α, interleukin (IL)-1 and IL-6 in the serum were analyzed using enyme-linked immunosorbent assay (ELISA). Two pathologists independently measured the synovitis score. Micro-computed tomography (CT) scans of the joints were performed to quantify joint destruction. The expression of IL-6 from human fibroblast-like synoviocytes (FLSs) after incubation with various doses of Tubastatin A (0, 0.75, 1.5, 3 μmol/L) was measured using ELISA.

Results: The clinical arthritis score was significantly attenuated and paw thickness was lower in the group treated with 100 mg/kg Tubastatin A compared with those treated with vehicle alone. The synovitis score was significantly reduced in the 100 mg/kg Tubastatin A-treated group compared with the control group. Micro-CT showed that quantitative measures of joint destruction were significantly attenuated in the 100 mg/kg Tubastatin A-treated group compared with the control. The expression of IL-6 in the sera was lower in the mice treated with Tubastatin A compared with the control. The expression of IL-6 in human FLSs decreased dose-dependently after incubation with Tubastatin A without affecting cell viability.

Conclusions: Tubastatin A successfully ameliorated synovial inflammation and protected against joint destruction in CAIA mice, at least in part, by modulating IL-6 expression.

Keywords: collagen antibody-induced arthritis; erosion; rheumatoid arthritis; tubastatin.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arthritis, Experimental / diagnostic imaging
  • Arthritis, Experimental / pathology
  • Arthritis, Experimental / prevention & control*
  • Arthrography
  • Cells, Cultured
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use
  • Histone Deacetylase 6
  • Histone Deacetylases / drug effects*
  • Histone Deacetylases / metabolism
  • Humans
  • Hydroxamic Acids / pharmacology*
  • Hydroxamic Acids / therapeutic use*
  • Indoles / pharmacology*
  • Indoles / therapeutic use*
  • Interleukin-1 / metabolism
  • Interleukin-6 / metabolism
  • Joints / drug effects
  • Joints / pathology*
  • Male
  • Mice
  • Mice, Inbred DBA
  • Synovial Membrane / drug effects
  • Synovial Membrane / metabolism
  • Synovial Membrane / pathology
  • Synovitis / diagnostic imaging
  • Synovitis / pathology
  • Synovitis / prevention & control*
  • Tomography, X-Ray Computed

Substances

  • Enzyme Inhibitors
  • Hydroxamic Acids
  • Indoles
  • Interleukin-1
  • Interleukin-6
  • tubastatin A
  • Hdac6 protein, mouse
  • Histone Deacetylase 6
  • Histone Deacetylases