Flavonoids inhibit the amidolytic activity of human thrombin

被引:55
作者
Mozzicafreddo, M. [1 ]
Cuccioloni, M. [1 ]
Eleuteri, A. M. [1 ]
Fioretti, E. [1 ]
Angeletti, M. [1 ]
机构
[1] Univ Camerino, MCAB Dept, I-62032 Camerino, MC, Italy
关键词
bioinformatics; biosensor; equilibrium studies; kinetics; polyphenols;
D O I
10.1016/j.biochi.2006.04.007
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 [生物化学与分子生物学]; 081704 [应用化学];
摘要
The effect of a group of natural flavonoids on human thrombin amidolytic activity was investigated using a spectrophotometric inhibition assay while information on the kinetics and thermodynamics was obtained using optical biosensor techniques. All the flavonoids tested acted as reversible inhibitors, and the quercetin-thrombin complex was found to be most stable at pH = 7.5. Docking analysis indicated that quercetin's inhibitory behavior could be related to its planar structure and low steric hindrance, and to its ability to form a critical H-bond with thrombin His57. (c) 2006 Elsevier SAS. All rights reserved.
引用
收藏
页码:1297 / 1306
页数:10
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