Characterization of the Human Bitter Taste Receptor Response to Sesquiterpene Lactones from Edible Asteraceae Species and Suppression of Bitterness through pH Control

[Image: see text] Vegetables are important sources of nutrients and bioactive compounds; however, their consumption is often insufficient, partly because of unpleasant taste characteristics. This study aimed to investigate the mechanisms underlying bitter taste reception and to develop methods to suppress bitterness. We focused on sesquiterpene lactones found in edible Asteraceae species. HEK293T cells that heterologously expressed human bitter taste receptors (including TAS2R46) together with a chimeric G protein were analyzed using calcium imaging, and cellular responses to four sesquiterpene lactones contained in lettuce were examined. We found that TAS2R46-expressing cells responded most strongly to bitter compounds. The EC(50) value of 11β,13-dihydrolactucopicrin was 2.0 ± 0.6 μM, in agreement with the previously reported bitterness threshold of the compound. Adjustment of pH from neutral to weak acidic conditions reduced the response of TAS2R46-expressing cells to sesquiterpene lactones. We demonstrate the possibility of regulating the bitterness of Asteraceae species by controlling the pH.