In vitro inhibition of quercetin and its glycosides on P450 enzyme activities / 中国药学杂志
Chinese Pharmaceutical Journal
; (24): 1051-1055, 2014.
Article
in Chinese
| WPRIM (Western Pacific)
| ID: wpr-859687
Responsible library:
WPRO
ABSTRACT
OBJECTIVE:
To evaluate inhibitory effect of the flavonoids, quercetin and its glycosides, on the activities of human liver microsomes isoforms CYP2C19, CYP2D6, CYP3A4 CYP2E1 and CYP2C9 in vitro for predicting prudential drug-drug interactions in clinical application.METHODS:
Human liver microsomes and five probes were incubated with tested flavonoids at 37°C, in presence of NADPH. The concentrations of produced metabolites in the reaction solution were determined by liquid chromatography/tandem mass spectrometry method, and compared for evaluating the activity of isoenzymes.RESULTS:
Quercetin inhibited CYP3A4 and CYP2C9 activities with IC50 values of 13.14 and 23.09 μmol·L-1, respectively. While, the quercetin glycosides, quercetin-3-O-glu-curonide, isoquercitrin, hyperoside and rutin were found no significant inhibition effects on the five tested enzymes, with IC50 values higher than 100 μmol·L-1.CONCLUSION:
Quercetin shows moderate inhibition on CYP3A4 and CYP2C9, there is very little inhibition on the other tested flavonoids because sufficiently high levels are not clinically achieved more than 100 μmol·L-1. The quercetin glycoside compounds are less likely to cause potential drug-drug interactions.
Full text:
Available
Database:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Chinese Pharmaceutical Journal
Year:
2014
Document type:
Article