Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation

Hongmei Cao, Rui Yu, Yongsoo Choi, Zhong Ze Ma, Hongjie Zhang, Wei Xiang, David Yue Wei Lee, Brian M. Berman, Kamal D. Moudgil, Harry H.S. Fong, Richard B. van Breemen*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

97 Citations (Scopus)


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% (IC50). Acetyl-11-keto-β-boswellic acid, β-boswellic acid, acetyl-α-boswellic acid, acetyl-β-boswellic acid, and betulinic acid were COX-1 selective inhibitors with IC50 values of approximately 10μM. Senkyunolide O and cryptotanshinone were COX-2 selective inhibitors with IC50 values of 5μM and 22μM, respectively. Roburic acid and phenethyl-trans-ferulate inhibited COX-1 and COX-2 equally. COX inhibition and the IC50 values of most of these natural product ligands have not been reported previously.

Original languageEnglish
Pages (from-to)519-524
Number of pages6
JournalPharmacological Research
Issue number6
Publication statusPublished - Jun 2010

Scopus Subject Areas

  • Pharmacology

User-Defined Keywords

  • Botanical dietary supplements
  • COX-2
  • Cryptotanshinone
  • Cyclooxygenase
  • Drug discovery
  • Senkyunolide O


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