Organic anion transporting polypeptides and organic cation transporter 1 contribute to the cellular uptake of the flavonoid quercetin

  title={Organic anion transporting polypeptides and organic cation transporter 1 contribute to the cellular uptake of the flavonoid quercetin},
  author={Hartmut Glaeser and Krystyna Bujok and Ingrid Schmidt and Martin F. Fromm and Kathrin Mandery},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
Flavonoids such as quercetin and kaempferol mediate several health protective effects, e.g., anticancer effects. They are inhibitors of organic anion transporting polypeptides (OATP) and organic cation transporters (e.g., OCT2). However, little is known whether such transporters contribute to the cellular uptake of flavonoids. Therefore, we investigated the cellular uptake of kaempferol and quercetin using HEK293 cell lines stably expressing different human OATPs or OCT1. Kaempferol was not a… 
Involvement of organic anion-transporting polypeptides and organic cation transporter in the hepatic uptake of jatrorrhizine
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Organic anion-transporting polypeptide (OATP) 2B1 contributes to the cellular uptake of theaflavin.
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Transport of Drugs and Endogenous Compounds Mediated by Human OCT1: Studies in Single- and Double-Transfected Cell Models
In vitro cell systems are important for the determination of the substrate spectrum of OCT1, the understanding of the molecular mechanisms of polarized transport, and the investigation of potential drug-drug interactions in vitro.
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A critical analysis of published data on the role of OATPs in ADME and in drug–drug interactions is offered, especially focusing on OATP1A2, 1B1,1B3 and 2B1.
Dissecting the Contribution of OATP1B1 to Hepatic Uptake of Statins Using the OATP1B1 Selective Inhibitor Estropipate.
The results suggest that EPP is an appropriate OATP1B1-selective inhibitor to establish the relative contribution of OatP1 B1 to hepatic uptake in vitro and to discern the role of OATp1B 1 in hepatic disposition in vivo.
Organic anion transporting polypeptide 1A2 mediates fentanyl uptake in cultured cells.
The present study established a 293 cell line stably overexpressing OATP1A2, and investigated the transport function of the organic anion transporting polypeptide (OATP) at the blood‑brain barrier (BBB) in Sprague‑Dawley rats to determine whether OatP1 a2 is able to transport fentanyl across the plasma membrane.
Introduction to the Cellular Transport of Organic Cations
The data show that OCTs play an important physiological role for neurotransmitter balance in the body and, considering their high expression in excretory organs, together with MATEs are responsible for drug excretion.


Inhibition of hepatic uptake transporters by flavonoids.
Mechanisms of pH-gradient driven transport mediated by organic anion polypeptide transporters.
It is concluded that the pH dependency of OATPs/Oatps may lead to a stimulation of substrate transport in an acidic microenvironment and that the OATP/ Oatp-mediated substrate transport into cells is generally compensated or accompanied by bicarbonate efflux.
Differential Role of Organic Anion-Transporting Polypeptides in Estrone-3-Sulphate Uptake by Breast Epithelial Cells and Breast Cancer Cells
Transport kinetics of E3S uptake demonstrates transport efficiency that is 10 times greater in the MCF7 cells than in the hormone-independent cells, suggesting that OATPs could be a novel therapeutic target for hormone-dependent breast cancers, particularly in postmenopausal patients.
Expression and localization of the uptake transporters OATP2B1, OATP3A1 and OATP5A1 in non-malignant and malignant breast tissue
The results indicate the possibility of OATP-mediated uptake of hormones during breast cancer development and an impact of certain OATPs on chemotherapeutic cancer treatment.
Involvement of Human Organic Anion Transporting Polypeptide OATP-B (SLC21A9) in pH-Dependent Transport across Intestinal Apical Membrane
OATP-B plays a role in the absorption of anionic compounds across the apical membrane of human intestinal epithelial cells, although it cannot be decisively concluded that pH-dependent absorption of pravastatin is determined by OATPB alone.
A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane.
The results indicate that OATP2 is important for the uptake of organic anions, including bilirubin conjugates and sulfobromophthalein, in human liver.
OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine.
OATP transporters and P-gp colocalize in organs of importance to drug disposition such as the liver, their activity provides an explanation for the heretofore unknown mechanism(s) responsible for fexofenadine's disposition and suggests potentially similar roles in the disposition of other xenobiotics.
Organic cation transporters (OCTs, MATEs), in vitro and in vivo evidence for the importance in drug therapy.
A comprehensive overview is given on currently known genotype-phenotype correlations for variants in OCTs and MATE1 related to protein expression, pharmacokinetics/-dynamics of transporter substrates, treatment outcome, and disease susceptibility.