Suppressive effects of the kahweol and cafestol on cyclooxygenase-2 expression in macrophages

FEBS Lett. 2004 Jul 2;569(1-3):321-6. doi: 10.1016/j.febslet.2004.05.070.


Inducible cyclooxygenase-2 (COX-2) has been suggested to play a role in the processes of inflammation and carcinogenesis. Recent studies have shown the chemoprotective effects of kahweol and cafestol, which are coffee-specific diterpenes. This study investigated the effects of kahweol and cafestol on the expression of COX-2 in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages. Kahweol and cafestol significantly suppressed the LPS-induced production of prostaglandin E(2), COX-2 protein and mRNA expression, and COX-2 promoter activity in a dose-dependent manner. Furthermore, kahweol blocked the LPS-induced activation of NF-kappaB by preventing IkappaB degradation and inhibiting IkappaB kinase activity. These results will provide new insights into the anti-inflammatory and anti-carcinogenic properties of kahweol and cafestol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Coffee*
  • Cyclooxygenase 2
  • Diterpenes / pharmacology*
  • I-kappa B Proteins / antagonists & inhibitors
  • Isoenzymes / genetics*
  • Lipopolysaccharides / pharmacology
  • Macrophages / drug effects
  • Macrophages / enzymology*
  • Mice
  • NF-KappaB Inhibitor alpha
  • NF-kappa B / antagonists & inhibitors
  • NF-kappa B / metabolism
  • Promoter Regions, Genetic / drug effects
  • Prostaglandin-Endoperoxide Synthases / genetics*
  • RNA, Messenger / genetics
  • Transcription, Genetic / drug effects


  • Coffee
  • Diterpenes
  • I-kappa B Proteins
  • Isoenzymes
  • Lipopolysaccharides
  • NF-kappa B
  • Nfkbia protein, mouse
  • RNA, Messenger
  • NF-KappaB Inhibitor alpha
  • kahweol
  • cafestol
  • Cyclooxygenase 2
  • Prostaglandin-Endoperoxide Synthases