Burkina, Viktoriia
- Jihočeská univerzita v Českých Budějovicích
Sammanfattning
Flavonoids are known to have effects on cytochrome P450 enzymatic activity. However, little effort has been made to examine species differences and the relevance of studies on mammalian and fish microsomes so that extrapolations can be made to humans. Therefore, the effects of several naturally occurring flavonoids on the activity of CYP3A-dependent 7-benzyloxy-4-trifluoromethylcoumarin O-debenzylase (BFCOD) were evaluated in human, pig, mouse, and juvenile rainbow trout sources of hepatic microsomes. Each was exposed to three concentrations (1, 10, and 100 mu M) of diosmin, naringin, and naringenin. Naringenin competitively inhibited BFCOD activity (K-i values were 24.6 mu M in human, 15.6 mu M in pig, and 19.6 mu M in mouse microsomes). In fish, BFCOD activity was inhibited in a noncompetitive manner (K-i = 7 mu M). Neither diosmin nor naringenin affected BFCOD activity in hepatic microsomes from the studied model organisms. These results suggest that dietary flavonoids potentially inhibit the metabolism of clinical drugs. (C) 2016 Elsevier Inc. All rights reserved.
Nyckelord
CYP3A; Inhibition; Diosmin; Naringin; Naringenin
Publicerad i
Biochemical Pharmacology
2016, volym: 110-111, sidor: 109-116
Utgivare: PERGAMON-ELSEVIER SCIENCE LTD
SLU författare
Zlabek, Vladimir
- Jihočeská univerzita v Českých Budějovicích
Zamaratskaia, Galia
- Institutionen för molekylära vetenskaper, Sveriges lantbruksuniversitet
- Jihočeská univerzita v Českých Budějovicích
- Institutionen för molekylära vetenskaper, Sveriges lantbruksuniversitet
UKÄ forskningsämne
Biokemi
Molekylärbiologi
Publikationens identifierare
- DOI: https://doi.org/10.1016/j.bcp.2016.04.011
Permanent länk till denna sida (URI)
https://res.slu.se/id/publ/77968