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. 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.

journal_name

Anticancer Res

journal_title

Anticancer research

authors

Kadioglu O,Nass J,Saeed ME,Schuler B,Efferth T

subject

Has Abstract

pub_date

2015-05-01 00:00:00

pages

2645-50

issue

5

eissn

0250-7005

issn

1791-7530

pii

35/5/2645

journal_volume

35

pub_type

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