Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation

被引：102
|
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
收藏
页码：519 / 524
页数：6
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