Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation

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

来源：Pharmacological Research, 2010, 61(6): 519-524.

DOI：10.1016/j.phrs.2010.02.007

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

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 mu M. Senkyunolide 0 and cryptotanshinone were COX-2 selective inhibitors with IC(50) values of 5 mu M and 22 mu M, 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.

• 出版日期2010-6