Department of Gastronomy Science and Functional Foods, Poznań University of Life Sciences, ul. Wojska Polskiego 28, 60-637, Poznań, Poland.
Department of Biochemistry and Biotechnology, Poznań University of Life Sciences, ul. Dojazd 11, 60-132, Poznań, Poland.
Sci Rep. 2024 Jul 10;14(1):15983. doi: 10.1038/s41598-024-66861-w.
Cornelian cherry fruits contain a wide range of phenolic acids, flavonoids, and other secondary metabolites. Selected flavonoids may inhibit the perceiving of bitterness, however, the full mechanism with all TAS2R bitter taste receptors is not known. The aim of the study was to determine the inhibitory effect of Cornus mas phenolics against the bitterness receptors TAS2R13 and TAS2R3 through functional in vitro assays and coupling studies. The overall effect was validated by analysing the inhibition of the receptors activity in cells treated with tested cornelian cherry extracts. The strength of interaction with both TAS2R receptors varied between studied compounds with different binding affinity. Most compounds bonded with the TAS2R3 receptor through a long-distant hydrophobic interaction with Trp89A and π-π orbital overlapping-between phenolic and tryptophane aromatic rings. For TAS2R13 observed were various mechanisms of interaction with the compounds. Nonetheless, naringin and quercetin had most similar binding affinity to chloroquine and denatonium-the model agonists for the receptor.
欧李果实含有丰富的酚酸、类黄酮和其他次生代谢物。一些特定的类黄酮可能会抑制苦味感知，然而，完整的机制以及所有 TAS2R 苦味受体并不清楚。本研究的目的是通过体外功能测定和偶联研究来确定欧李酚类物质对苦味受体 TAS2R13 和 TAS2R3 的抑制作用。通过分析用测试的欧李提取物处理的细胞中受体活性的抑制来验证整体效果。研究化合物之间的相互作用强度因与两个 TAS2R 受体的结合亲和力不同而有所不同。大多数化合物通过与 Trp89A 的长距离疏水相互作用以及酚和色氨酸芳环之间的π-π轨道重叠与 TAS2R3 受体结合。对于 TAS2R13，观察到与化合物的各种相互作用机制。然而，柚皮苷和槲皮素与氯喹和苯甲地那铵（该受体的模型激动剂）具有最相似的结合亲和力。
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