Type 2 bitter taste receptors (TAS2Rs), a subfamily of G protein-coupled receptors, comprise 25 receptor-members. Besides being expressed on taste buds to perceive bitterness, TAS2Rs are also distributed in multiple systems, including the respiratory, digestive, immune systems, where they regulate various physiological processes such as airway defense, gastrointestinal motility, and inflammation regulation. In traditional Chinese medicines (TCMs) theory, the bitter TCMs are able to purge, dry and firm. Their functional substances often serve as both taste substances that evoke bitter perception and the key component responsible for the medicinal properties and efficacy of bitter herbs. These components may exert various pharmacological effects, such as regulating glucolipid metabolism and inflammatory responses, by activating TAS2Rs expressed in different tissues and organs. This article systematically expounds the association between the efficacy of bitter TCMs and the function of TAS2Rs, as well as the tissue distribution, physiological functions, structural characteristics and signal transduction mechanisms of TAS2Rs, and analyses the problems and challenges in research between bitter TCMs and TAS2Rs pharmacology. It’s expected to reveal the scientific essence of the “property-effect-substance” correlation of bitter TCMs.

bitter traditional Chinese medicines  /  bitter taste receptors  /  physiological function  /  structural characteristics  /  signal transduction  /  bitter components