The number and variety of bitter compounds originating from plants are vast. Whereas some bitter chemicals are toxic and should not be ingested, other compounds exhibit health beneficial effects, which is manifest in the cross‐cultural believe that the bitterness of medicine is correlated with the desired medicinal activity. The bitter taste receptors in the oral cavity serve as sensors for bitter compounds and, as they are expressed in numerous extraoral tissues throughout the body, may also be responsible for some physiological effects exerted by bitter compounds. Chinese herbal medicine uses bitter herbs since ancient times for the treatment of various diseases; however, the routes by which these herbs modify physiology are frequently not well understood. We therefore screened 26 bitter substances extracted from medical herbs for the activation of the 25 human bitter taste receptors. We identified six receptors activated by in total 17 different bitter compounds. Interestingly, we observed a bias in bitter taste receptor activation with 10 newly identified agonists for the broadly tuned receptor TAS2R46, seven agonists activating the TAS2R14 and two compounds activating narrowly tuned receptors, suggesting that these receptors play dominant roles in the evaluation and perhaps physiological activities of Chinese herbal medicines.

中文翻译：

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来自中药的植物中的苦味物质对人的苦味受体产生偏激的激活作用

源自植物的苦味化合物的数量和种类繁多。尽管某些苦味化学物质有毒且不应摄入，但其他化合物却显示出有益于健康的作用，这在跨文化背景中得到了证明，即药物的苦味与所需的药物活性相关。口腔中的苦味感受器可作为苦味化合物的传感器，并且由于它们在体内的众多口腔外组织中表达，也可能与苦味化合物产生的某些生理作用有关。中草药自古以来就使用苦草药来治疗各种疾病。然而，这些草药改变生理状态的途径通常并不为人所知。因此，我们筛选了从草药中提取的26种苦味物质，以激活25种人类苦味受体。我们鉴定了总共17种不同苦味化合物激活的6种受体。有趣的是，我们观察到苦味受体激活存在偏见，其中有10种新近确定的针对广泛调节的受体TAS2R46的激动剂，7种激活TAS2R14的激动剂和两种化合物对狭窄的受体进行激活，这表明这些受体在评估和生理活动中起主要作用中草药。