加州细辛中类黄酮对苦味受体 hTAS2R31 拮抗活性的体外评价。
In vitro evaluation of flavonoids from Eriodictyon californicum for antagonist activity against the bitterness receptor hTAS2R31.
机构信息
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 500 West 12th Avenue, Columbus, Ohio 43210, United States.
出版信息
J Agric Food Chem. 2011 Dec 28;59(24):13117-21. doi: 10.1021/jf204359q. Epub 2011 Nov 17.
Abstract
The leaves of the native North American plant, Eriodictyon californicum, were once used to mask the bitter taste of pharmaceuticals, an application currently of importance. Ten flavonoids (1-10) were isolated from the leaves of E. californicum, of which the structure and absolute configuration of 6-methoxyhesperetin (8) were assigned for the first time. In addition, the absolute configurations at C-2 were established for 4'-isobutyrylhomoeriodictyol (3) and 6-methoxyhomoeriodictyol (7). Using a cell-based assay, it was determined that the 7-methoxylated flavanones, sakuranetin (2) and 6-methoxysakuranetin (9), and the flavone, jaceosidin (10), are antagonists of hTAS2R31.
摘要
原产于北美的 Eriodictyon californicum 植物的叶子曾被用于掩盖药物的苦味，这一用途目前非常重要。从 E. californicum 的叶子中分离出了 10 种类黄酮（1-10），其中 6-甲氧基橙皮素（8）的结构和绝对构型首次被确定。此外，还确定了 4'-异丁酰基 homoeriodictyol（3）和 6-甲氧基 homoeriodictyol（7）中 C-2 的绝对构型。通过基于细胞的测定，确定了 7-甲氧基黄烷酮，樱黄素（2）和 6-甲氧基樱黄素（9）以及黄酮，乔松苷（10）是 hTAS2R31 的拮抗剂。
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