Prevention of LPS-induced microglia activation, cytokine production and sickness behavior with TLR4 receptor interfering peptides

PLoS One. 2013;8(3):e60388. doi: 10.1371/journal.pone.0060388. Epub 2013 Mar 28.

Abstract

The innate immune receptor Toll-like 4 (TLR4) is the receptor activated by lipopolysaccharide (LPS), and TLR4-LPS interaction is well known to induce an innate immune response, triggering sickness behavior. Within the brain, TLR4 is highly expressed in brain microglia, and excessive inflammation resulting from activation of this pathway in the brain has been implicated in depressive disorders and neurodegenerative pathologies. We hypothesized that blocking LPS-induced activation of TLR4 would prevent downstream immune signaling in the brain and suppress the induction of sickness behavior. We used interfering peptides to block TLR4 activation and confirmed their efficacy in preventing second messenger activation and cytokine production normally induced by LPS treatment. Further, these peptides blocked morphological changes in microglia that are typically induced by LPS. We also demonstrated that intraperitoneal (i.p.) injection of Tat-TLR4 interfering peptides prevented LPS-induced sickness behavior, as assessed in home cage behavior and with the intracranial self-stimulation paradigm. These newly synthesised peptides inhibit TLR4 signaling thereby preventing changes in behavior and motivation caused by inflammatory stimuli. These peptides highlight the roll of TLR4 and microglia morphology changes in sickness behavior, and thus may be of therapeutic value in limiting the deleterious impact of excessive inflammation in specific CNS pathologies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Brain / drug effects
  • Brain / immunology
  • Brain / pathology
  • Cytokines / immunology*
  • Humans
  • Illness Behavior / drug effects*
  • Immunity, Innate / drug effects
  • Lipopolysaccharides / immunology*
  • Mice
  • Microglia / drug effects*
  • Microglia / immunology
  • Microglia / pathology
  • Molecular Sequence Data
  • Peptides / chemistry
  • Peptides / pharmacology*
  • Signal Transduction / drug effects
  • Toll-Like Receptor 4 / antagonists & inhibitors*
  • Toll-Like Receptor 4 / immunology*

Substances

  • Cytokines
  • Lipopolysaccharides
  • Peptides
  • Toll-Like Receptor 4