Cordycepin inhibits LPS-induced inflammatory responses by modulating NOD-Like Receptor Protein 3 inflammasome activation

Biomed Pharmacother. 2017 Nov:95:1777-1788. doi: 10.1016/j.biopha.2017.09.103. Epub 2017 Oct 6.

Abstract

Aim: The aim of this study is to examine the effects of cordycepin (CRD) on LPS-induced inflammatory response in macrophages and further investigate the underlying molecular mechanisms.

Methods: Cultured mouse RAW264.7 macrophages and human THP-1-derived macrophages were used in this study. The mRNA and protein expression levels of cytokine IL-1β, IL-6, TNF-α, and MCP-1 were detected by real time RT-PCR, ELISA and Western blot, respectively. The activation of NOD-Like Receptor Protein 3 (NLRP3) inflammasome was analyzed with Western blot analysis and immunofluorescence staining. The ERK1/2 activation was assessed by Western blot analysis.

Results: The results demonstrated that pretreatment with CRD (6.25, 12.5, 25, 50μmol/L) dose-dependently inhibited LPS-induced expression of proinflammatory cytokines (IL-1β, IL-6, TNF-α, MCP-1) and cyclooxygenase 2 (COX-2) in mouse RAW264.7 cells. Similar results were obtained in human THP-1-derived macrophages with CRD. Furthermore, CRD remarkably inhibited LPS-induced activation of the NLRP3 inflammasome and ERK1/2 signaling pathway in RAW264.7 cells.

Conclusion: CRD exerts anti-inflammatory effects in LPS-induced murine and human macrophages at least in part by inhibiting the activation of NLRP3 inflammasome and ERK1/2 signaling pathway as well as inhibition of COX2-mediated inflammatory response.

Keywords: Cordycepin; ERK; Inflammatory cytokines; NOD-Like Receptor Protein 3 inflammasome.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / pharmacology
  • Blotting, Western
  • Cyclooxygenase 2 / drug effects
  • Cyclooxygenase 2 / metabolism
  • Cytokines / metabolism
  • Deoxyadenosines / administration & dosage
  • Deoxyadenosines / pharmacology*
  • Dose-Response Relationship, Drug
  • Humans
  • Inflammasomes / drug effects*
  • Inflammasomes / metabolism
  • Inflammation / prevention & control*
  • Lipopolysaccharides
  • MAP Kinase Signaling System / drug effects
  • Macrophages / metabolism
  • Mice
  • NLR Family, Pyrin Domain-Containing 3 Protein / metabolism*
  • RAW 264.7 Cells
  • Real-Time Polymerase Chain Reaction
  • Signal Transduction / drug effects

Substances

  • Anti-Inflammatory Agents
  • Cytokines
  • Deoxyadenosines
  • Inflammasomes
  • Lipopolysaccharides
  • NLR Family, Pyrin Domain-Containing 3 Protein
  • Cyclooxygenase 2
  • cordycepin