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. © 2006 Elsevier Masson SAS. All rights reserved.
Flavonoids inhibit the amidolytic activity of human thrombin / Mozzicafreddo, M.; Cuccioloni, M.; Eleuteri, A. M.; Fioretti, E.; Angeletti, M.. - In: BIOCHIMIE. - ISSN 0300-9084. - 88:9(2006), pp. 1297-1306. [10.1016/j.biochi.2006.04.007]
Flavonoids inhibit the amidolytic activity of human thrombin
Mozzicafreddo M.;
2006-01-01
Abstract
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. © 2006 Elsevier Masson SAS. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
