German Institute of Human Nutrition Potsdam-Rehbruecke, 14558 Nuthetal, Germany.
J Neurosci. 2011 Oct 12;31(41):14775-82. doi: 10.1523/JNEUROSCI.2923-11.2011.
Food contains complex blends of structurally diverse bitter compounds that trigger bitterness through activation of one or more of the ∼25 human TAS2 bitter taste receptors. It remains unsolved, however, whether the perceived bitterness of binary bitter-compound mixtures can be considered an additive function of all bitter-inducing chemicals in the mouth, suggesting that little mutual interaction takes place among bitter substances or if mixture suppression and synergism occurs. Here we report on two natural sesquiterpene lactones from edible plants, which stimulate distinct sets of hTAS2Rs in transfected cells. Both chemicals also robustly inhibit different but overlapping subsets of agonist-activated hTAS2Rs. These findings demonstrate that mixtures of bitter compounds, because they normally occur in human foodstuff, likely elicit bitter perception in a complex and not in a merely additive manner. An unexpected implication of this discovery is that, during evolution, the naturally occurring bitter taste receptor antagonists have shaped some of the pharmacological properties of the receptors, such as overlapping recognition profiles and breadth of tuning.
食物中含有复杂的混合结构不同的苦味化合物，通过激活一个或多个约 25 个人类 TAS2 苦味受体来引发苦味。然而，尚未解决的问题是，二元苦味化合物混合物的感知苦味是否可以被认为是口中所有引起苦味的化学物质的加性函数，这表明苦味物质之间几乎没有相互作用，或者是否发生混合物抑制和协同作用。在这里，我们报告了两种来自食用植物的天然倍半萜内酯，它们在转染细胞中刺激不同的 hTAS2R 集。这两种化学物质还强烈抑制不同但重叠的激动剂激活 hTAS2R 亚集。这些发现表明，由于苦味化合物混合物通常存在于人类食物中，因此它们可能以复杂的方式而不是简单的加性方式引起苦味感知。这一发现的一个意外含义是，在进化过程中，天然存在的苦味受体拮抗剂塑造了受体的一些药理学特性，例如重叠的识别谱和调谐的广度。
