Effect of quercetin on CYP3A activity in Chinese healthy participants
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 (AUC(0-12 h)) of midazolam (160.88 ± 45.58 ng·h/mL vs 188.07 ± 65.75 ng·h/mL, P < .05), significantly decreased the AUC(0-∞) of midazolam (165.46 ± 47.15 ng·h/mL vs 211.84 ± 75.80 ng·h/mL, P < .01), shortened t(1/2) (2.06 ± 0.51 h vs 2.75 ± 0.89 h, P < .01), and decreased t(max) 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.
How strong is the evidence?
Evidence Hub reads this as a randomized trial, done in people. Its evidence level is 2 of 5 (High · randomized trial). Randomized trials of a reasonable size are the strongest single-study design. Reported size: 165 participants or records.
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