期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 20, 页码 9101-9105出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.09.028
关键词
carbonic anhydrase; salicylic acid derivatives; inhibition; hCA I; hCA II; enzyme inhibitor
资金
- 6th Framework programme
- DeZnIT project
- Scientific and Technological Research Council of Turkey [107T882 TBAG-HD/328]
The inhibition of two human cytosolic carbonic anhydrase ( hCA, EC 4.2.1.1) isozymes, hCA I and II, with a series of salicylic acid derivatives was investigated by using the esterase method with 4-nitrophenyl acetate as substrate. IC50 values for sulfasalazine, diflunisal, 5-chlorosalicylic acid, dinitrosalicylic acid, 4-aminosalicylic acid, 4-sulfosalicylic acid, 5-sulfosalicylic acid, salicylic acid, acetylsalicylic acid ( aspirin) and 3-metylsalicylic acid were of 3.04 mu M, 3.38 mu M, 4.07 mu M, 7.64 mu M, 0.13 mM, 0.29 mM, 0.42 mM, 0.56 mM, 2.71 mM and 3.07 mM for hCA I and of 4.49 mu M, 2.70 mu M, 0.72 mu M, 2.80 mu M, 0.75 mM, 0.72 mM, 0.29 mM, 0.68 mM, 1.16 mM and 4.70 mM for hCA II, respectively. Lineweaver-Burk plots were also used for the determination of the inhibition mechanism of these substituted phenols, most of which were noncompetitive inhibitors with this substrate. Some salicylic acid derivatives investigated here showed effective hCA I and II inhibitory activity, and might be used as leads for generating enzyme inhibitors eventually targeting other isoforms which have not been assayed yet for their interactions with such agents. (C) 2008 Elsevier Ltd. All rights reserved.
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