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Vitamins and plant ingredients

Effect of quercetin on P-glycoprotein transport ability in Chinese healthy subjects

Abstract

Objectives:

The aim of this study was to investigate the effect of quercetin on P-glycoprotein (P-gp) transport ability in vivo.

Subjects/Methods:

Genotype data were available from a total of 165 health volunteers. An open, randomized, two-period crossover clinical trial was performed in eighteen subjects with different MDR1 3435 C/T genotypes. All subjects took 500 mg quercetin or placebo daily from 1st to 13th day or from 43st to 55th day, and 100 mg talinolol was given at the 14th or 56th day. The washout period is 28 days.

Results:

In this study, we found the values of area under the curve (AUC)0–48h, AUC0–∞ and Cmax of talinolol in all subjects significantly decreased (6496.6±2389.9 vs 7809.5±2386.8 ng.h/ml, P=0.04), (8414.7±344.8 vs 10478.2±4195.4 ng.h/ml, P=0.03), (412.9±132.6 vs 543.3±97.9 ng.h/ml, P=0.01) after administration of quercetin, respectively. There were no significant differences in tmax and t1/2 of talinolol. The results also showed AUC0–48h (5598.6±2202.1 vs 8229.4±1491.7 ng.h/ml, P=0.02) and AUC0–∞ (7110.0±3437.0 vs 12681.2±4828.2 ng.h/ml, P=0.01) of talinolol to be significantly decreased in MDR1 3435 TT individuals administered of quercetin. The Cmax of talinolol in MDR1 3435 TT (382.4±149.1 vs 584.9±115.2 ng/ml, P=0.04) and MDR1 3435 CT (383.5±104.9 vs 554.6±80.6 ng/ml, P=0.01) individuals significantly decreased after the administration of quercetin.

Conclusions:

Quercetin significantly induced the activity of P-gp and this induced effect was more obvious in MDR1 3435 TT individuals.

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Acknowledgements

We thank these volunteers for their support in this study. We also thank the grants support of the National High-Tech R&D Program of China (863 Program; 2012AA02A517), National Natural Science Foundation of China (81173129), Program for Changjiang Scholars and Innovative Research Team in University of Ministry of Education of China (IRT0946), and supported by Hunan Provincial Natural Science Foundation of China (12JJ7006).

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Correspondence to Z-Q Liu.

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Wang, SY., Duan, KM., Li, Y. et al. Effect of quercetin on P-glycoprotein transport ability in Chinese healthy subjects. Eur J Clin Nutr 67, 390–394 (2013). https://doi.org/10.1038/ejcn.2013.5

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  • DOI: https://doi.org/10.1038/ejcn.2013.5

Keywords

  • quercetin
  • talinolol
  • MDR1
  • drug transporter
  • gene polymorphisms
  • pharmacokinetcs

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