Eriodictyol and thymonin act as GPR35 agonists.
Eriodictyol and thymonin act as GPR35 agonists.
复制标题
圣草酚和胸腺素充当 GPR35 激动剂。
DOI：
10.1093/bbb/zbad125
复制
发表时间：
2023
期刊：
影响因子：
--
通讯作者：
T. Shibata
中科院分区：
文献类型：
--
作者：
Fumie Nakashima;Wei Qi Loh;Mayuka Wakabayashi;Sayako Shimomura;Hiroyuki Hattori;Masaki Kita;A. Inoue;Koji Uchida;T. Shibata
尽管草药和香料因其对健康的益处而被用于传统医学已有世纪之久，但相关的潜在机制仍不清楚。由于G蛋白偶联受体35（GPR35）与多种抗氧化和抗炎作用有关，我们筛选了19种不同的草药和香料，以了解GPR35依赖的草药和香料功能。在筛选的提取物中，百里香的乙酸乙酯提取物表现出显著的GPR35激动活性。活性导向分离使我们能够确定两个多酚植物化学物质，圣草酚和胸腺素，作为GPR35激动剂。圣草酚和胸腺素对GPR35均表现出强而特异的激动活性，半数最大有效浓度值分别为5.48和8.41 μM。这些发现表明，这些植物化学物质可能对GPR35激活具有有益的健康影响。
Although herbs and spices have been used in traditional medicine for more than a century owing to their health benefits, the associated underlying mechanism is still not clear. Since the G protein-coupled receptor 35 (GPR35) has been linked to exert various antioxidant and anti-inflammatory effects, we screened 19 different herbs and spices for possible GPR35 agonist(s) to understand the GPR35-dependent functions on herbs and spices. Among the screened extracts, the ethyl acetate extract of thyme exhibited a remarkable GPR35 agonistic activity. Activity-guided separations allowed us to identify two polyphenolic phytochemicals, eriodictyol and thymonin, acting as GPR35 agonists. Both eriodictyol and thymonin showed a potent and specific agonist activity toward GPR35 with half maximal effective concentration values of 5.48 and 8.41 μM, respectively. These findings indicate that these phytochemicals may have beneficial health effects upon GPR35 activation.