Title |
6-Methoxyflavanones as Bitter Taste Receptor Blockers for hTAS2R39
|
---|---|
Published in |
PLOS ONE, April 2014
|
DOI | 10.1371/journal.pone.0094451 |
Pubmed ID | |
Authors |
Wibke S. U. Roland, Robin J. Gouka, Harry Gruppen, Marianne Driesse, Leo van Buren, Gerrit Smit, Jean-Paul Vincken |
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. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Spain | 1 | 1% |
Unknown | 91 | 99% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 15 | 16% |
Researcher | 13 | 14% |
Student > Master | 12 | 13% |
Professor > Associate Professor | 8 | 9% |
Professor | 6 | 7% |
Other | 18 | 20% |
Unknown | 20 | 22% |
Readers by discipline | Count | As % |
---|---|---|
Agricultural and Biological Sciences | 20 | 22% |
Biochemistry, Genetics and Molecular Biology | 11 | 12% |
Chemistry | 9 | 10% |
Pharmacology, Toxicology and Pharmaceutical Science | 4 | 4% |
Medicine and Dentistry | 4 | 4% |
Other | 16 | 17% |
Unknown | 28 | 30% |