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<title lang=en>Inhibition of SLC drug transporter activities by environmental bisphenols</title>
<creator>Bruyere, A.</creator>
<creator>Hubert, C.</creator>
<creator>Le Vee, M.</creator>
<creator>Chedik, L.</creator>
<creator>Sayyed, K.</creator>
<creator>Stieger, B.</creator>
<creator>Denizot, C.</creator>
<creator>Parmentier, Y.</creator>
<creator>Fardel, O.</creator>
<contributor>Institut de recherche, santé, environnement et travail [Rennes] (Irset) ; Université d'Angers (UA) - Université des Antilles et de la Guyane (UAG) - Université de Rennes 1 (UR1) - École des Hautes Études en Santé Publique [EHESP] (EHESP) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>University hospital of Zurich [Zurich]</contributor>
<contributor>Technologie Servier ; Technologie Servier</contributor>
<contributor>Institut de biologie moléculaire des plantes (IBMP) ; Centre National de la Recherche Scientifique (CNRS)</contributor>
<contributor>CHU Pontchaillou [Rennes]</contributor>
<description>International audience</description>
<source>Toxicology in Vitro</source>
<identifier>hal-01467545</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01467545</identifier>
<source>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01467545</source>
<source>Toxicology in Vitro, 2017, 40, pp.34--44. 〈10.1016/j.tiv.2016.12.009〉</source>
<identifier>DOI : 10.1016/j.tiv.2016.12.009</identifier>
<relation>info:eu-repo/semantics/altIdentifier/doi/10.1016/j.tiv.2016.12.009</relation>
<identifier>PUBMED : 27989701</identifier>
<relation>info:eu-repo/semantics/altIdentifier/pmid/27989701</relation>
<language>en</language>
<subject>[SDV.EE] Life Sciences [q-bio]/Ecology, environment</subject>
<type>info:eu-repo/semantics/article</type>
<type>Journal articles</type>
<description lang=en>The plastic component bisphenol A (BPA) is suspected to exert deleterious effects towards human health and targets various cellular and molecular pathways, including activity of ATP-binding cassette drug transporters. The present study was designed to determine whether BPA and some derivatives, like its substitutes bisphenol F (BPF) and bisphenol S (BPS) and the flame retardant tetrabromobisphenol A (TBBPA), may additionally interact with solute carrier (SLC) drug transporters. Activities of the various following SLC transporters were inhibited in a major way (by > 60%) by 100 μM bisphenols: OCT1 and MATE1 (by BPA and TBBPA), OATP1B1 (by BPA, BPF and TBBPA), OATP1B3 and NTCP (by TBBPA) and OAT3 (by BPA, BPF, BPS and TBBPA); by contrast, activities of other transporters were not impacted (MATE2-K) or were stimulated (notably OCT1 by BPS and OCT2 by BPF). Transporter inhibitions due to bisphenols were concentrations-dependent, with half maximal inhibitory concentrations (IC50) ranging from 0.5 μM to 73.5 μM. BPA was finally shown to be not transported by OAT3, although inhibiting this transporter in a competitive manner. Taken together, these data indicate that bisphenols interact with SLC transporters, at concentration levels however rather higher than those occurring in humans in response to environmental exposure. © 2016 Elsevier B.V.</description>
<date>2017</date>
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