Bitter substances from plants used in traditional Chinese medicine exert biased activation of human bitter taste receptors
Bitter substances from plants used in traditional Chinese medicine exert biased activation of human bitter taste receptors
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DOI：
10.1111/cbdd.13089
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发表时间：
2018-02-01
影响因子：
3
通讯作者：
Meyerhof, Wolfgang
中科院分区：
文献类型：
--
作者：
Behrens, Maik;Gu, Ming;Meyerhof, Wolfgang
来源于植物的苦味化合物的数量和种类是巨大的。虽然一些苦味化学物质是有毒的，不应该被摄入，但其他化合物表现出有益健康的效果，这体现在跨文化的信念中，即药物的苦味与所需的药物活性相关。口腔中的苦味受体充当苦味化合物的传感器，并且由于它们在整个身体的许多口外组织中表达，因此也可能是由苦味化合物施加的一些生理效应的原因。中草药自古以来就使用苦味草药治疗各种疾病;然而，这些草药改变生理的途径往往不太清楚。因此，我们筛选了26种从草药中提取的苦味物质，用于激活25种人类苦味受体。我们确定了总共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的偏见与10个新鉴定的激动剂广泛调谐受体TAS 2 R46，7激动剂激活TAS 2 R14和两个化合物激活窄调谐受体，这表明这些受体中发挥主导作用的评价，也许中草药的生理活性。
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.