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Discovery of Cyclooxygenase Inhibitors From Medicinal Plants Used to Treat Inflammation

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

Pharmacol Res. 2010 Jun;61(6):519-24.

PMID: 20188172

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP6812813	Roburic acid		6812-81-3	Price

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