EMAIL THIS PAGE TO A FRIEND

PloS one

6-methoxyflavanones as bitter taste receptor blockers for hTAS2R39.


PMID 24722342

Abstract

Many (dietary) bitter compounds, e.g. flavonoids, activate bitter receptor hTAS2R39 in cell-based assays. Several flavonoids, amongst which some flavanones, are known not to activate this receptor. As certain flavanones are known to mask bitter taste sensorially, flavanones might act as bitter receptor antagonists. Fourteen flavanones were investigated for their potential to reduce activation of hTAS2R39 by epicatechin gallate (ECG), one of the main bitter compounds occurring in green tea. Three flavanones showed inhibitory behavior towards the activation of hTAS2R39 by ECG: 4'-fluoro-6-methoxyflavanone, 6,3'-dimethoxyflavanone, and 6-methoxyflavanone (in order of decreasing potency). The 6-methoxyflavanones also inhibited activation of hTAS2R14 (another bitter receptor activated by ECG), though to a lesser extent. Dose-response curves of ECG at various concentrations of the full antagonist 4'-fluoro-6-methoxyflavanone and wash-out experiments indicated reversible insurmountable antagonism. The same effect was observed for the structurally different agonist denatonium benzoate.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

T3258
Tetracycline, ≥88.0% (HPLC)
C22H24N2O8 · xH2O
87128
Tetracycline, ≥98.0% (NT)
C22H24N2O8 · xH2O
93595
Trypan Blue solution, 0.4%, for microscopy
C34H24N6Na4O14S4