Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine

被引：8
|
作者：
Sethi, Kalyan K. [1 ]
Sahoo, Suvendu K. [1 ]
Pichikala, Jayaprakash N. [1 ]
Suresh, Padilam [1 ]
机构：
[1] GITAM Univ, GITAM Inst Pharm, Visakhapatnam 530045, Andhra Pradesh, India
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2012年 / 27卷 / 01期
关键词：
Carbonic anhydrase; enzyme inhibitor; natural product; caffeine; piperine; ISOZYME-II; HETEROCYCLIC SULFONAMIDES; THERAPEUTIC APPLICATIONS; SULFAMATE INHIBITORS; VIVO SELECTIVITY; SALICYLIC-ACID; CA I; TARGET; TRANSMEMBRANE; PHENOLS;
D O I：
10.3109/14756366.2011.578393
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Novel chemotypes with carbonic anhydrase (CA; EC 4.2.1.1) inhibitory action, in addition to the sulphonamide and sulphamate were discovered, many of which are based on natural products. Caffeine and piperine were extracted and tested for inhibition of the human (h) cytosolic isoforms hCA I and II. The IC50 values of caffeine against hCA I was of 55 mM, whereas that of piperine of 60 mM. The IC50 values of caffeine and piperine against hCA II were of 2 mM. Although these are quite weak inhibitors they may constitute leads for developing tighter binding compounds.
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收藏
页码：97 / 100
页数：4
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