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
Tingyu YangShaojun Shi

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 ...Continue Reading

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Citations

Jan 23, 2021·Pharmaceutics·Maria D AuxteroAna I Fernandes
Jul 11, 2019·Mini Reviews in Medicinal Chemistry·Zehra CalisAbdülkerim Kasim Baltaci

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Methods Mentioned

BETA
Protein Concentration Assay
electrophoresis

Software Mentioned

Drug and Statistics ( DAS )
AlphaEaseFC
GraphPad Prism
GraphPad

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