jf5b05833_si_001.pdf (115.74 kB)
Characterization and Modulation of the Bitterness of Polymethoxyflavones Using Sensory and Receptor-Based Methods
journal contribution
posted on 2016-03-02, 00:00 authored by A. Max Batenburg, Teun de Joode, Robin J. GoukaAn obstacle in the application of many “health ingredients”
is their alleged off-flavor. We used a combination of chemical, sensory,
and biological analyses to identify the bitter components in citrus
peel-derived polymethoxyflavone preparations, claimed to be functional
in the lowering of cholesterol. Nobiletin (56–81%) and tangeretin
(10–33%) were found to be the main bitter components. Using
in vitro receptor assays, hTAS2R14 was shown to be the main bitter
receptor involved in their perception, with EC50 values
of 14 and 63 μM, respectively. Our analysis provided several
routes for off-flavor reduction. Purification is an option because
a purified, single PMF species proved to be considerably less bitter
upon application in emulsified foods, due to limited solubility in
the aqueous phase. A second route, also demonstrated in vivo, is C5-specific
demethoxylation, in line with the finding that 5-desmethylnobiletin
does not activate hTAS2R14. A third route could be the use of TAS2R14
antagonists. As a proof of principle, several antagonists, with IC50 values ranging from 10 to 50 μM, were identified.