Indirubin Inhibits LPS-Induced Inflammation via TLR4 Abrogation Mediated by the NF-kB and MAPK Signaling Pathways

Inflammation. 2017 Feb;40(1):1-12. doi: 10.1007/s10753-016-0447-7.

Abstract

Indirubin plays an important role in the treatment of many chronic diseases and exhibits strong anti-inflammatory activity. However, the molecular mode of action during mastitis prophylaxis remains poorly understood. In this study, a lipopolysaccharide (LPS)-induced mastitis mouse model showed that indirubin attenuated histopathological changes in the mammary gland, local tissue necrosis, and neutrophil infiltration. Moreover, indirubin significantly downregulated the production of interleukin (IL)-1β, IL-6, and tumor necrosis factor-α (TNF-α). We explored the mechanism whereby indirubin exerts protective effects against LPS-induced inflammation of mouse mammary epithelial cells (MMECs). The addition of different concentrations of indirubin before exposure of cells to LPS for 1 h significantly attenuated inflammation and reduced the concentrations of the three inflammatory cytokines in a dose-dependent manner. Indirubin downregulated LPS-induced cyclooxygenase-2 (COX-2) and Toll-like receptor 4 (TLR4) expression, inhibited phosphorylation of the LPS-induced nuclear transcription factor-kappa B (NF-kB) P65 protein and its inhibitor IkBα of the NF-kB signaling pathway. Furthermore, indirubin suppressed phosphorylation of P38, extracellular signal-regulated kinase (ERK), and c-Jun NH2-terminal kinase (JNK) of the mitogen-activated protein kinase (MAPK) signal pathways. Thus, indirubin effectively suppressed LPS-induced inflammation via TLR4 abrogation mediated by the NF-kB and MAPK signaling pathways and may be useful for mastitis prophylaxis.

Keywords: MAPK; NF-kB; TLR4; indirubin; inflammation; lipopolysaccharide (LPS).

MeSH terms

  • Animals
  • Cytokines / drug effects
  • Cytokines / metabolism
  • Dose-Response Relationship, Drug
  • Female
  • Indoles / pharmacology
  • Indoles / therapeutic use
  • Inflammation / drug therapy*
  • Inflammation Mediators / metabolism
  • Lipopolysaccharides
  • MAP Kinase Signaling System / drug effects*
  • Mastitis / drug therapy
  • Mice
  • NF-kappa B / metabolism*
  • Signal Transduction / drug effects
  • Toll-Like Receptor 4 / physiology*

Substances

  • Cytokines
  • Indoles
  • Inflammation Mediators
  • Lipopolysaccharides
  • NF-kappa B
  • Tlr4 protein, mouse
  • Toll-Like Receptor 4
  • indirubin