Kaempferol Is an Anti-Inflammatory Compound with Activity towards NF-κB Pathway Proteins

Anticancer Res. 2015 May;35(5):2645-50.


Background: The nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway is critical in inflammation, proliferation and carcinogenesis. There exist three main players in this pathway. The inhibitor of NF-κB (IκB), IκB kinase (IκK)- NF-κB essential modulator (NEMO) complex and NF-κB. The IkK-NEMO complex activates NF-κB via phosphorylation of Iκβ and, eventually, leads to its proteasomal degradation. This leads to nuclear translocation of NF-κB and activation of target genes, such as cyclooxygenases and interleukins. The identification of anti-inflammatory compounds might be an effective strategy to target inflammatory disorders and cancer.

Materials and methods: In the present investigation, kaempferol was investigated in terms of its effect on NF-κB activity with a SEAP-driven reporter cell line, NF-κB DNA binding with electromobility shift assay (EMSA) and translocation of NF-κB-p65 from cytosol to the nucleus with western blot in Jurkat cells.

Results: Kaempferol revealed anti-inflammatory activity, as shown in vitro and in silico. Molecular docking studies of kaempferol revealed comparable binding energies and similar docking poses on target proteins such as MG-132, a known NF-κB inhibitor.

Conclusion: We conclude that kaempferol possesses anti-inflammatory activity.

Keywords: NF-κB pathway; inflammation; leukemia; molecular docking.

MeSH terms

  • Apoptosis / drug effects
  • Carcinogenesis / drug effects
  • Cell Proliferation / drug effects*
  • Humans
  • I-kappa B Kinase / chemistry
  • I-kappa B Kinase / genetics
  • Inflammation / drug therapy*
  • Inflammation / genetics
  • Inflammation / pathology
  • Jurkat Cells
  • Kaempferols / administration & dosage*
  • Leukemia / drug therapy*
  • Leukemia / genetics
  • Leukemia / pathology
  • Molecular Docking Simulation
  • NF-kappa B / chemistry
  • NF-kappa B / genetics*
  • Phosphorylation
  • Signal Transduction / drug effects


  • Kaempferols
  • NF-kappa B
  • kaempferol
  • I-kappa B Kinase