Harmine is an inflammatory inhibitor through the suppression of NF-κB signaling

Biochem Biophys Res Commun. 2017 Jul 29;489(3):332-338. doi: 10.1016/j.bbrc.2017.05.126. Epub 2017 May 24.


Harmine is a major constituent in a hallucinogenic botanical mixture ayahuasca and medical plant Peganum harmala L. The plant is used for various illnesses and exhibits anti-inflammatory activity. However, the active constituents remain unclear. Here, we screened the seven alkaloids in P. harmala for their anti-inflammatory activity using an nuclear factor-κB (NF-κB) reporter assay. We found that harmine and harmol could inhibit NF-κB transactivity. As the most abundant compound, harmine inhibited tumor necrosis factor-α (TNF-α)- and lipopolysaccharides (LPS)-induced NF-κB transactivity and nuclear translocation in mouse macrophage RAW 264.7 cells. The mRNA and protein levels of NF-κB downstream inflammatory cytokines also reduced. In an LPS-challenged mouse model, harmine markedly averted inflammatory damage of the lung, and decreased serum TNF-α, interleukin-1β (IL-1β) and IL-6 levels. Our data indicate that harmine may exert the anti-inflammatory effect by inhibition of the NF-κB signaling pathway and harmine is probably responsible for the anti-inflammatory effects of P. harmala.

Keywords: Harmin; IL-1β; IL-6; Inflammation; NF-κB; Peganum harmala L.; TNF-α.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • HEK293 Cells
  • Harmine / chemistry
  • Harmine / pharmacology*
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / metabolism
  • Lipopolysaccharides / antagonists & inhibitors
  • Lipopolysaccharides / pharmacology
  • Mice
  • Molecular Structure
  • NF-kappa B / metabolism*
  • Nitric Oxide / biosynthesis
  • Protein Transport / drug effects
  • RAW 264.7 Cells
  • Signal Transduction / drug effects*
  • Structure-Activity Relationship
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors
  • Tumor Necrosis Factor-alpha / pharmacology


  • Anti-Inflammatory Agents
  • Lipopolysaccharides
  • NF-kappa B
  • Tumor Necrosis Factor-alpha
  • Nitric Oxide
  • Harmine