Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation.

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% (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.

• Authors: 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
• Journal: Pharmacological research (Pharmacol Res) Vol. 61 Issue 6 Pg. 519-24 (Jun 2010) ISSN: 1096-1186 [Electronic] Netherlands
• PMID: 20188172 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
• Copyright: (c) 2010 Elsevier Ltd. All rights reserved.

Chemical References

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

Topics

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