Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation |
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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 HS Fong Richard B van Breemen |
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Institution: | 1. Cancer Biology Division, KIIT School of Biotechnology, KIIT University, Campus-11, Patia, Bhubaneswar, Orissa 751024, India;2. Institute of Life Sciences, Nalco Square, Bhubaneswar, Orissa 751023, India;3. Department of Biotechnology, Visva Bharati University, Santiniketan, West Bengal, India |
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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 10 μM. Senkyunolide O and cryptotanshinone were COX-2 selective inhibitors with IC50 values of 5 μM and 22 μM, 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. |
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