Phytochemicals from Ruta graveolens Activate TAS2R Bitter Taste Receptors and TRP Channels Involved in Gustation and Nociception.
Ruta graveolens (rue) is a spontaneous plant in the Mediterranean area with a strong aroma and a very intense bitter taste, used in gastronomy and in folk medicine. From the leaves, stems and fruits of rue, we isolated rutin, rutamarin, three furanocoumarins, two quinolinic alkaloids, a dicoumarin and two long chain ketones. Bitter taste and chemesthetic properties have been evaluated by in vitro assays with twenty receptors of the TAS2R family and four TRP ion channels involved in gustation and nociception. Among the alkaloids, skimmianine was active as a specific agonist of T2R14, whereas kokusaginin did not activate any of the tested receptors. The furanocoumarins activates TAS2R10, 14, and 49 with different degrees of selectivity, as well as the TRPA1 somatosensory ion channel. Rutamarin is an agonist of TRPM5 and TRPV1 and a strong antagonist of TRPM8 ion channels.
DeFENS-Department of Food, Environmental and Nutritional Sciences, University of Milan, via Celoria 2, Milano I-20133, Italy. manq.hsp@libero.it.
Giuseppe
G
Mancuso
DeFENS-Department of Food, Environmental and Nutritional Sciences, University of Milan, via Celoria 2, Milano I-20133, Italy. gigliola.borgonovo@unimi.it.
Gigliola
G
Borgonovo
DeFENS-Department of Food, Environmental and Nutritional Sciences, University of Milan, via Celoria 2, Milano I-20133, Italy. leonardo.scaglioni@unimi.it.
Leonardo
L
Scaglioni
DeFENS-Department of Food, Environmental and Nutritional Sciences, University of Milan, via Celoria 2, Milano I-20133, Italy. angela.bassoli@unimi.it.
Angela
A
Bassoli
D020013:Calcium Signaling; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D059225:Nociception; D009822:Oils, Volatile / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010938:Plant Oils / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D043562:Receptors, G-Protein-Coupled / Q000819:agonists; D032105:Ruta / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013649:Taste; D050051:Transient Receptor Potential Channels / Q000819:agonists*; D000098706:Taste Receptors, Type 2
D009822:Oils, Volatile; D010936:Plant Extracts; D010938:Plant Oils; D043562:Receptors, G-Protein-Coupled; D050051:Transient Receptor Potential Channels; D000098706:Taste Receptors, Type 2
Ruta graveolens; TAS2Rs receptors; TRP channels; bitter taste; chemesthesis