search button
Open Access

Quercetin‑3‑O‑β‑D‑glucoside decreases the bioavailability of cyclosporin A through regulation of drug metabolizing enzymes, transporters and nuclear receptors in rats

  • Authors:
    • Tingyu Yang
    • Yani Liu
    • Xixi Huang
    • Rui Zhang
    • Chunxiao Yang
    • Jiali Zhou
    • Yu Zhang
    • Jing Wan
    • Shaojun Shi

  • View Affiliations

  • Published online on: July 3, 2018     https://doi.org/10.3892/mmr.2018.9249
  • Pages: 2599-2612

  • Copyright: © Yang et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

Metrics: Total Views: 0 (Spandidos Publications: | PMC Statistics: )
Total PDF Downloads: 0 (Spandidos Publications: | PMC Statistics: )


Abstract

Quercetin is a flavonoid compound that is widely present in food and drink. Quercetin‑3‑O‑β‑D‑glucoside (Q3GA) is a major metabolite of quercetin. The aim of the present study was to investigate the effect of Q3GA on the pharmacokinetics of orally and intravenously administered cyclosporin A (CsA) in rats, and to assess the effect of Q3GA on drug‑metabolizing enzymes (DMEs), drug transporters (DTs) and nuclear receptors (NRs). The pharmacokinetic parameters of CsA were measured following oral (10 mg/kg) and intravenous (2.5 mg/kg) administration of CsA in the presence or absence of Q3GA. The mRNA and protein expression levels of DMEs, DTs and NRs in the liver and small intestine were detected by quantitative polymerase chain reaction and western blot analysis. The results indicated that the intravenous administration of Q3GA (2.5, 5 or 10 mg/kg) for 7 consecutive days reduced the bioavailability of oral CsA. By contrast, the pharmacokinetics of the intravenous administration of CsA were not affected by Q3GA. However, the mRNA and protein expression levels of DMEs and DTs were inhibited by Q3GA. The activation of DMEs and DTs by NRs, and the interplay between DMEs and DTs, may explain these results. The present study identified a novel flavonoid‑drug interaction, which may have implications for patients taking CsA and quercetin supplements or on a quercetin‑containing diet.
View Figures
View References

Related Articles

Journal Cover

September-2018
Volume 18 Issue 3

Print ISSN: 1791-2997
Online ISSN:1791-3004

Sign up for eToc alerts

Recommend to Library

  • Journal Metrics
  • Impact Factor: 3.4
  • Ranked Medicine Research and Experimental
    (total number of cites)
  • CiteScore: 7.6
  • CiteScore Rank: Q1: #82/347 Biochemistry, Genetics and Molecular Biology
  • Source Normalized Impact per Paper (SNIP): 0.647
  • SCImago Journal Rank (SJR): 0.781
International Symposium on Molecular Medicine Conference Banner
The Cancer Story
World Congress on Advances in Oncology and International Symposium on Molecular Medicine Conference Banner
World Academy Of Sciences Banner
Heyday Road Banner

0

Copy and paste a formatted citation
x
Spandidos Publications style
Yang T, Liu Y, Huang X, Zhang R, Yang C, Zhou J, Zhang Y, Wan J and Shi S: Quercetin‑3‑O‑β‑D‑glucoside decreases the bioavailability of cyclosporin A through regulation of drug metabolizing enzymes, transporters and nuclear receptors in rats. Mol Med Rep 18: 2599-2612, 2018.
APA
Yang, T., Liu, Y., Huang, X., Zhang, R., Yang, C., Zhou, J. ... Shi, S. (2018). Quercetin‑3‑O‑β‑D‑glucoside decreases the bioavailability of cyclosporin A through regulation of drug metabolizing enzymes, transporters and nuclear receptors in rats. Molecular Medicine Reports, 18, 2599-2612. https://doi.org/10.3892/mmr.2018.9249
MLA
Yang, T., Liu, Y., Huang, X., Zhang, R., Yang, C., Zhou, J., Zhang, Y., Wan, J., Shi, S."Quercetin‑3‑O‑β‑D‑glucoside decreases the bioavailability of cyclosporin A through regulation of drug metabolizing enzymes, transporters and nuclear receptors in rats". Molecular Medicine Reports 18.3 (2018): 2599-2612.
Chicago
Yang, T., Liu, Y., Huang, X., Zhang, R., Yang, C., Zhou, J., Zhang, Y., Wan, J., Shi, S."Quercetin‑3‑O‑β‑D‑glucoside decreases the bioavailability of cyclosporin A through regulation of drug metabolizing enzymes, transporters and nuclear receptors in rats". Molecular Medicine Reports 18, no. 3 (2018): 2599-2612. https://doi.org/10.3892/mmr.2018.9249