Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation

被引：105

作者：

Cao, Hongmei ^{[1
]}

Yu, Rui ^{[1
]}

Choi, Yongsoo ^{[1
]}

Ma, Zhong-Ze ^{[2
]}

Zhang, Hongjie ^{[1
]}

Xiang, Wei ^{[1
]}

Lee, David Yue-Wei ^{[2
]}

Berman, Brian M. ^{[3
]}

Moudgil, Kamal D. ^{[4
]}

Fong, Harry H. S. ^{[1
]}

van Breemen, Richard B. ^{[1
]}

机构：

[1] Univ Illinois, Coll Pharm, Dept Med Chem & Pharmacognosy, Chicago, IL 60680 USA

[2] Harvard Univ, McLean Hosp, Sch Med, Belmont, MA 02178 USA

[3] Univ Maryland, Sch Med, Ctr Integrat Med, James Kernan Hosp Mans, Baltimore, MD 21201 USA

[4] Univ Maryland, Sch Med, Dept Microbiol & Immunol, Baltimore, MD 21201 USA

来源：

PHARMACOLOGICAL RESEARCH | 2010年 / 61卷 / 06期

基金：

美国国家卫生研究院;

关键词：

Cyclooxygenase; COX-2; Drug discovery; Botanical dietary supplements; Senkyunolide O; Cryptotanshinone; ULTRAFILTRATION MASS-SPECTROMETRY; PULSED ULTRAFILTRATION; COMBINATORIAL LIBRARIES; BIOLOGICAL EVALUATION; BETULINIC ACID; IDENTIFICATION; CONSTITUENTS;

D O I：

10.1016/j.phrs.2010.02.007

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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-beta-boswellic acid, beta-boswellic acid, acetyl-alpha-boswellic acid, acetyl-beta-boswellic acid, and betulinic acid were COX-1 selective inhibitors with IC50 values of approximately 10 mu M. Senkyunolide 0 and cryptotanshinone were COX-2 selective inhibitors with IC50 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 IC50 values of most of these natural product ligands have not been reported previously. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：519 / 524

页数：6

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