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- Title
Effect of Quercetin on CYP3A Activity in Chinese Healthy Participants.
- Authors
Duan, Kai-Ming; Wang, Sai-Ying; Ouyang, Wen; Mao, Yan-Mei; Yang, Li-Jun
- Abstract
The aims of this study were to investigate the effect of quercetin on CYP3A activity in vivo. An open, randomized, 2-period crossover experiment was performed in 18 healthy male volunteers. Genotyped data were available from a total of 165 participants. The allelic frequency was 52.5%. Every volunteer ingested orally 500 mg quercetin or placebo once a day for 13 consecutive days. On day 14, a single 7.5-mg midazolam tablet was administrated orally. The plasma concentrations of midazolam and 1-OH-midazolam were determined over 24 hours. The results showed that coadministration of quercetin in CYP3A5*1/*1 and CYP3A5*1/*3 individuals significantly decreased the area under the curve (AUC0-12 h) of midazolam (160.88 ± 45.58 ng·h/mL vs 188.07 ± 65.75 ng·h/mL, P < .05), significantly decreased the AUC0-∞ of midazolam (165.46 ± 47.15 ng·h/mL vs 211.84 ± 75.80 ng·h/mL, P < .01), shortened t1/2 (2.06 ± 0.51 h vs 2.75 ± 0.89 h, P < .01), and decreased tmax significantly (0.48 ± 0.36 h vs 1.06 ± 0.69 h, P < .01), respectively. In conclusion, quercetin significantly induced CYP3A activity to substrate midazolam, and the induction was partly related to the CYP3A5 genotype, being more prominent in CYP3A5*1/*1 and CYP3A5*1/*3 individuals.
- Subjects
CHINA; ANALYSIS of variance; BIOPHYSICS; CROSSOVER trials; GENES; HIGH performance liquid chromatography; MASS spectrometry; RESEARCH methodology; MIDAZOLAM; OXIDOREDUCTASES; POLYMERASE chain reaction; QUERCETIN; STATISTICAL sampling; T-test (Statistics); RANDOMIZED controlled trials; REPEATED measures design; DATA analysis software; DESCRIPTIVE statistics; THERAPEUTICS
- Publication
Journal of Clinical Pharmacology, 2012, Vol 52, Issue 6, p940
- ISSN
0091-2700
- Publication type
Article
- DOI
10.1177/0091270011406278