PDF(Pubmed)
Abstract：
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.
摘要：
Cornelian樱桃果实含有广泛的酚酸，黄酮类化合物，和其他次生代谢产物。选择的类黄酮可以抑制苦味的感知，然而,所有TAS2R苦味受体的完整机制尚不清楚。该研究的目的是通过功能性体外测定和偶联研究来确定山茱萸酚类对苦味受体TAS2R13和TAS2R3的抑制作用。通过分析用测试的矢车菊樱桃提取物处理的细胞中受体活性的抑制来验证总体效果。与两种TAS2R受体相互作用的强度在具有不同结合亲和力的研究化合物之间变化。大多数化合物通过与Trp89A和酚类和色氨酸芳环之间的π-π轨道重叠的长距离疏水相互作用与TAS2R3受体键合。对于TAS2R13,观察到与化合物相互作用的各种机制。尽管如此，柚皮苷和槲皮素与受体的模型激动剂-氯喹和地那铵具有最相似的结合亲和力。
