Abstract
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 language | English |
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Pages (from-to) | 519-524 |
Number of pages | 6 |
Journal | Pharmacological Research |
Volume | 61 |
Issue number | 6 |
DOIs | |
Publication status | Published - Jun 2010 |
Scopus Subject Areas
- Pharmacology
User-Defined Keywords
- Botanical dietary supplements
- COX-2
- Cryptotanshinone
- Cyclooxygenase
- Drug discovery
- Senkyunolide O