Differential effects of selective HDAC inhibitors on macrophage inflammatory responses to the Toll-like receptor 4 agonist LPS

J Leukoc Biol. 2010 Jun;87(6):1103-14. doi: 10.1189/jlb.0509363. Epub 2010 Mar 3.

Abstract

Broad-spectrum inhibitors of HDACs are therapeutic in many inflammatory disease models but exacerbated disease in a mouse model of atherosclerosis. HDAC inhibitors have anti- and proinflammatory effects on macrophages in vitro. We report here that several broad-spectrum HDAC inhibitors, including TSA and SAHA, suppressed the LPS-induced mRNA expression of the proinflammatory mediators Edn-1, Ccl-7/MCP-3, and Il-12p40 but amplified the expression of the proatherogenic factors Cox-2 and Pai-1/serpine1 in primary mouse BMM. Similar effects were also apparent in LPS-stimulated TEPM and HMDM. The pro- and anti-inflammatory effects of TSA were separable over a concentration range, implying that individual HDACs have differential effects on macrophage inflammatory responses. The HDAC1-selective inhibitor, MS-275, retained proinflammatory effects (amplification of LPS-induced expression of Cox-2 and Pai-1 in BMM) but suppressed only some inflammatory responses. In contrast, 17a (a reportedly HDAC6-selective inhibitor) retained anti-inflammatory but not proinflammatory properties. Despite this, HDAC6(-/-) macrophages showed normal LPS-induced expression of HDAC-dependent inflammatory genes, arguing that the anti-inflammatory effects of 17a are not a result of inhibition of HDAC6 alone. Thus, 17a provides a tool to identify individual HDACs with proinflammatory properties.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • Chromatin Immunoprecipitation
  • Cyclooxygenase 2 / genetics
  • Cyclooxygenase 2 / metabolism
  • Enzyme-Linked Immunosorbent Assay
  • Histone Deacetylase 6
  • Histone Deacetylase Inhibitors / pharmacology*
  • Histone Deacetylases / chemistry*
  • Histone Deacetylases / physiology
  • Hydroxamic Acids / pharmacology
  • Inflammation / immunology*
  • Inflammation / metabolism
  • Inflammation / pathology
  • Inflammation Mediators / metabolism
  • Interleukin-12 Subunit p40 / genetics
  • Interleukin-12 Subunit p40 / metabolism
  • Lipopolysaccharides / pharmacology*
  • Luciferases / metabolism
  • Macrophages / cytology
  • Macrophages / drug effects*
  • Macrophages / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Plasminogen Activator Inhibitor 1 / genetics
  • Plasminogen Activator Inhibitor 1 / metabolism
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Reverse Transcriptase Polymerase Chain Reaction
  • Toll-Like Receptor 4 / agonists*
  • Toll-Like Receptor 4 / metabolism
  • Vorinostat

Substances

  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Inflammation Mediators
  • Interleukin-12 Subunit p40
  • Lipopolysaccharides
  • Plasminogen Activator Inhibitor 1
  • RNA, Messenger
  • Toll-Like Receptor 4
  • trichostatin A
  • Vorinostat
  • Luciferases
  • Ptgs2 protein, mouse
  • Cyclooxygenase 2
  • Hdac6 protein, mouse
  • Histone Deacetylase 6
  • Histone Deacetylases