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Human Bitter Taste Receptors Are Activated by Different Classes of Polyphenols

Journal name:Journal of Agricultural and Food Chemistry
Literature No.:
Literature Url: https://pubs.acs.org/doi/abs/10.1021/acs.jafc.8b03569
Date publication:July 28, 2018
Polyphenols may contribute directly to plant-based foodstuffs flavor, in particular to astringency and bitterness. In this work, the bitterness of a small library of polyphenols from different classes [procyanidin dimers type B, ellagitannins (punicalagin, castalagin, and vescalagin) and phenolic acid ethyl esters (protocatechuic, ferulic, and vanillic acid ethyl esters] was studied by a cell-based assay. The bitter taste receptors (TAS2Rs) activated by these polyphenols and the half-maximum effective concentrations (EC50) of each agonist–TAS2Rs pair were determined. Computational methodologies were used to understand the polyphenol molecular region responsible for receptor activation and to get insights into the type of bonds established in the agonist–TAS2Rs pairs. The results show the combinatorial pattern of TAS2Rs activation. TAS2R5 seems to be the only receptor exhibiting a bias toward the activation by condensed tannins, while TAS2R7 seems more tuned for hydrolyzable (ellagi)tannins. Additionally, at the concentrations usually found for these compounds in foodstuffs, they can actively contribute to bitter taste, especially ellagitannins.
… 6 MATERIAL AND METHODS 73 Reagents. All reagents used were of analytical grade. Toyopearl HW-40(s) gel was purchased from 74 Tosoh
(Tokyo, Japan). Epigallocatechin gallate (EGCG) was acquired from Biopurify …
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