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. 2020 Jun 2;25(11):2590. doi: 10.3390/molecules25112590

Table 1.

Summary of studies on human bitter taste receptors (TAS2Rs) screening for activation by polyphenol agonists. EC50-Half-maximum effective concentration.

Hydrolyzable Tannins Grandinin Castalagin Punicalagin Vescalagin PGG
Structure graphic file with name molecules-25-02590-i001.jpg graphic file with name molecules-25-02590-i002.jpg graphic file with name molecules-25-02590-i003.jpg graphic file with name molecules-25-02590-i004.jpg graphic file with name molecules-25-02590-i005.jpg
EC50 (μM) 2.43 4.44 40.23; 3.95 7.26 8.5; 6.6
Activated TAS2Rs 7 7 5 and 7 7 5 and 7
Transfected cells HEK293T
Reference [30] [29]
Condensed Tannins (−)-Epicatechin (+)-Catechin ECG EGCG EGC Procyanidins
B1 B4 B2g B7 C2
Structure Inline graphic
(−)-Epicatechin R1 = H, R2 = OH
(−)-Catechin R1 = OH, R2 = H		 Inline graphic
(−)-ECG R = H
(−)-EGCG R = OH		 graphic file with name molecules-25-02590-i008.jpg Inline graphic
B1: R1 = OH; R2 = H; R3 = H; R4 = OH
B4: R1 = H; R2 = OH; R3 = OH; R4 = H
B2g: R1 = O-Galloyl; R2, R3 = H; R4 = OH		 graphic file with name molecules-25-02590-i010.jpg graphic file with name molecules-25-02590-i011.jpg
EC50 (μM) 30151.0; 3210.0; nd; 3800 nd; nd 70; nd; nd; 151 nd; 12.30; 34; nd; 8.50-161; 16.72 nd; nd 119.34; 123.95 nd 6.29; 9.11 nd 35.6
Activated TAS2Rs 4, 5, 14, 39 14 and 39 14, 30, 38, 39 4, 5, 14, 30, 39, 43 14 and 39 5 and 7 5 5 and 39 5 5
Transfected cells HEK293 and HEK293T HEK293 HEK293 and HEK293T HEK293T
Reference [29,31,33] [33] [31,32,33] [30,31,33] [31,32,33] [30] [29]

nd: non determined; ECG: epicatechin gallate, EGCG: epigallocatechin gallate; EGC: epigallocatechin.