Quercetin, Morin, Luteolin, and Phloretin Are Dietary Flavonoid Inhibitors of Monocarboxylate Transporter 6

Molecular Pharmaceutics
Robert S JonesMarilyn E Morris

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, a...Continue Reading

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Citations

May 16, 2018·The Journal of Pharmacy and Pharmacology·Clément ChaletPatrick Augustijns
Oct 28, 2018·Biotechnology and Bioengineering·Ana S NunesIlídio J Correia
Jun 27, 2020·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Robert S JonesMarilyn E Morris
Mar 21, 2019·CNS & Neurological Disorders Drug Targets·Fahad Ali, Yasir Hasan Siddique
Mar 8, 2020·Pharmacological Reviews·Melanie A FelmleeMarilyn E Morris

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