Methylene blue inhibits NLRP3, NLRC4, AIM2, and non-canonical inflammasome activation

Sci Rep. 2017 Sep 29;7(1):12409. doi: 10.1038/s41598-017-12635-6.

Abstract

Methylene blue (MB), which has antioxidant, anti-inflammatory, neuroprotective, and mitochondria protective effects, has been widely used as a dye and medication. However, the effect of MB on inflammasome activation has not yet been studied. Inflammasomes are multi-protein complexes that induce maturation of interleukins (ILs)-1β and -18 as well as caspase-1-mediated cell death, known as pyroptosis. Dysregulation of inflammasomes causes several diseases such as type 2 diabetes, Alzheimer's disease, and gout. In this study, we assess the effect of MB on inflammasome activation in macrophages. As the result, MB attenuated activation of canonical inflammasomes such as NLRP3, NLRC4, and AIM2 as well as non-canonical inflammasome activation. In addition, MB inhibited upstream signals such as inflammasome assembly, phagocytosis, and gene expression of inflammasome components via inhibition of NF-κB signaling. Furthermore, MB reduced the activity of caspase-1. The anti-inflammasome properties of MB were further confirmed in mice models. Thus, we suggest that MB is a broad-spectrum anti-inflammasome candidate molecule.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis Regulatory Proteins / antagonists & inhibitors
  • CARD Signaling Adaptor Proteins / antagonists & inhibitors
  • Calcium-Binding Proteins / antagonists & inhibitors
  • DNA-Binding Proteins / antagonists & inhibitors
  • Gene Expression / drug effects
  • Humans
  • Inflammasomes / drug effects*
  • Inflammasomes / metabolism
  • Macrophages / drug effects*
  • Macrophages / metabolism
  • Methylene Blue / pharmacology*
  • Mice
  • Mice, Inbred C57BL
  • NF-kappa B / metabolism
  • NLR Family, Pyrin Domain-Containing 3 Protein / antagonists & inhibitors
  • Phagocytosis / drug effects
  • Pyroptosis / drug effects
  • RAW 264.7 Cells
  • THP-1 Cells

Substances

  • AIM2 protein, human
  • Aim2 protein, mouse
  • Apoptosis Regulatory Proteins
  • CARD Signaling Adaptor Proteins
  • Calcium-Binding Proteins
  • DNA-Binding Proteins
  • Inflammasomes
  • Ipaf protein, mouse
  • NF-kappa B
  • NLR Family, Pyrin Domain-Containing 3 Protein
  • NLRC4 protein, human
  • NLRP3 protein, human
  • Nlrp3 protein, mouse
  • Methylene Blue