苦味受体（type 2 bitter taste receptor，TAS2Rs）属于G蛋白偶联受体亚家族，共有25个受体成员，除表达于味蕾以感知苦味外，还广泛分布于呼吸、消化、免疫等系统，参与调控气道防御、胃肠运动、炎症反应等生理过程。在中医药理论中，苦味中药具有“能泄、能燥、能坚”的特性，其功效物质既是苦味感知的呈味分子，又是发挥苦味药性和药效的关键成分，可能通过激活在不同组织器官表达的TAS2Rs，发挥调节糖脂代谢、调控炎症反应等药理作用。通过系统阐述苦味中药药效与TAS2Rs受体功能之间的关联，及TAS2Rs的组织分布、生理功能、结构特征及信号转导机制等，分析苦味中药与TAS2Rs受体药理学研究面临的问题与挑战，以期揭示苦味中药“性-效-物”关联的科学内涵。

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.

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组分中药国家重点实验面上项目（CBCM2024107）；四川省杰出青年科技人才项目（2025NSFJQ0032）；成都中医药大学引进人才项目（030040043）；国家自然科学基金资助项目（82574615）；国家自然科学基金资助项目（32200576）；四川省岐黄学者能力提升项目