Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation

Pharmacol Res. 2010 Jun;61(6):519-24. doi: 10.1016/j.phrs.2010.02.007. Epub 2010 Feb 24.


Eleven authenticated botanicals used in the traditional Chinese medicine Huo-Luo-Xiao-Ling Dan were screened for ligands to cyclooxygenase (COX) using pulsed ultrafiltration liquid chromatography-mass spectrometry, and a mass spectrometry-based enzyme assay was used to determine the concentration of each of 17 ligands that inhibited COX-1 or COX-2 by 50% (IC(50)). Acetyl-11-keto-beta-boswellic acid, beta-boswellic acid, acetyl-alpha-boswellic acid, acetyl-beta-boswellic acid, and betulinic acid were COX-1 selective inhibitors with IC(50) values of approximately 10 microM. Senkyunolide O and cryptotanshinone were COX-2 selective inhibitors with IC(50) values of 5 microM and 22 microM, respectively. Roburic acid and phenethyl-trans-ferulate inhibited COX-1 and COX-2 equally. COX inhibition and the IC(50) values of most of these natural product ligands have not been reported previously.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Cyclooxygenase 1 / metabolism
  • Cyclooxygenase 2 / metabolism
  • Cyclooxygenase Inhibitors / pharmacology*
  • Drugs, Chinese Herbal / pharmacology*
  • Humans


  • Anti-Inflammatory Agents
  • Cyclooxygenase Inhibitors
  • Drugs, Chinese Herbal
  • huo luo xiao ling dan
  • Cyclooxygenase 1
  • Cyclooxygenase 2