Warfarin and flavonoids do not share the same binding region in binding to the IIA subdomain of human serum albumin (CROSBI ID 240686)
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Podaci o odgovornosti
Rimac, Hrvoje ; Dufour, Claire ; Debeljak, Željko ; Zorc, Branka ; Bojić, Mirza
engleski
Warfarin and flavonoids do not share the same binding region in binding to the IIA subdomain of human serum albumin
Human serum albumin (HSA) binds a variety of xenobiotics, including flavonoids and warfarin. Binding of another ligand to the IIA binding site on HSA can cause warfarin displacement and potentially elevation of its free concentration in blood. Studies dealing with flavonoid- induced warfarin displacement from HSA provided controversial results: estimated risk of displacement ranged from none to serious. To resolve these controversies, in vitro study of simultaneous binding of warfarin and 8 different flavonoid aglycons and glycosides to HSA was carried out by fluorescence spectroscopy as well as molecular docking. Results show that warfarin and flavonoids do not share the same binding region in binding to HSA. Interactions were only observed at high warfarin concentrations, not attainable under recommended dosing regimes. Docking experiments show that flavonoid aglycons and glycosides do not bind at warfarin high affinity site, but rather to different regions within the IIA HSA subdomain. Thus, the risk of clinically significant warfarin–flavonoid interaction in binding to HSA should be regarded as negligible.
Flavonoids ; HSA binding ; subdomain IIA ; fluorimetry ; docking ; molecular modeling
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nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano
nije evidentirano