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• W2615458027 endingPage "2936" @default.
• W2615458027 startingPage "2930" @default.
• W2615458027 abstract "Monocarboxylate transporter 6 (MCT6; SLC16A5) has been recognized for its role as a xenobiotic transporter, with characterized substrates probenecid, bumetanide, and nateglinide. To date, the impact of commonly ingested dietary compounds on MCT6 function has not been investigated, and therefore, the objective of this study was to evaluate a variety of flavonoids for their potential MCT6-specific interactions. Flavonoids are a large group of polyphenolic phytochemicals found in commonly consumed plant-based products that have been recognized for their dietary health benefits. The uptake of bumetanide in human MCT6 gene-transfected Xenopus laevis oocytes was significantly decreased in the presence of a variety of flavonoids (e.g., quercetin, luteolin, phloretin, and morin), but was not significantly affected by flavonoid glycosides (e.g., naringin, rutin, phlorizin). The IC50 values of quercetin, phloretin, and morin were determined to be 25.3 ± 3.36, 17.3 ± 2.37, and 33.1 ± 3.29 μM, respectively. The mechanism of inhibition of phloretin was reversible and competitive, with a Ki value of 22.8 μM. Furthermore, typical MCT substrates were also investigated for their potential interactions with MCT6. Substrates of MCTs 1, 2, 4, 8, and 10 did not cause any significant decrease in MCT6-mediated bumetanide uptake, suggesting that MCT6 has distinct compound selectivity. In summary, these results suggest that dietary aglycon flavonoids may significantly alter the pharmacokinetics and pharmacodynamics of bumetanide and other MCT6-specific substrates, and may represent potential substrates for MCT6." @default.
• W2615458027 created "2017-05-26" @default.
• W2615458027 creator A5013913541 @default.
• W2615458027 creator A5050416801 @default.
• W2615458027 creator A5051769144 @default.
• W2615458027 date "2017-05-31" @default.
• W2615458027 modified "2023-10-09" @default.
• W2615458027 title "Quercetin, Morin, Luteolin, and Phloretin Are Dietary Flavonoid Inhibitors of Monocarboxylate Transporter 6" @default.
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• W2615458027 doi "https://doi.org/10.1021/acs.molpharmaceut.7b00264" @default.
• W2615458027 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5585036" @default.
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• W2615458027 hasPublicationYear "2017" @default.
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