title: Kaempferol Is an Anti-Inflammatory Compound with Activity towards NF-κB Pathway Proteins.
abstract: 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.
  
  
  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.
  
  
  CONCLUSIONS
  We conclude that kaempferol possesses anti-inflammatory activity.
authors.affiliation: Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Mainz, Germany.
authors.forename: Onat
authors.initials: O
authors.lastname: Kadioglu
authors.affiliation: Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Mainz, Germany.
authors.forename: Janine
authors.initials: J
authors.lastname: Nass
authors.affiliation: Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Mainz, Germany.
authors.forename: Mohamed E M
authors.initials: ME
authors.lastname: Saeed
authors.affiliation: Department of Pharmaceutical Biology and Biotechnology, Institute of Pharmaceutical Sciences, Albert-Ludwigs-University Freiburg, Freiburg, Germany.
authors.forename: Barbara
authors.initials: B
authors.lastname: Schuler
authors.affiliation: Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, Johannes Gutenberg University, Mainz, Germany efferth@uni-mainz.de.
authors.forename: Thomas
authors.initials: T
authors.lastname: Efferth
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D063646:Carcinogenesis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D051550:I-kappa B Kinase / Q000737:chemistry / Q000235:genetics; D007249:Inflammation / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D019169:Jurkat Cells; D044949:Kaempferols / Q000008:administration & dosage*; D007938:Leukemia / Q000188:drug therapy* / Q000235:genetics / Q000473:pathology; D062105:Molecular Docking Simulation; D016328:NF-kappa B / Q000737:chemistry / Q000235:genetics*; D010766:Phosphorylation; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D044949:Kaempferols; D016328:NF-kappa B; C006552:kaempferol; D051550:I-kappa B Kinase
keywords: NF-κB pathway; inflammation; leukemia; molecular docking