Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, 2-552-1 Noshio, Kiyose-shi, Tokyo 204-8588, Japan.
Department of Bioinformatics, Meiji Pharmaceutical University, 2-552-1 Noshio, Kiyose-shi, Tokyo 204-8588, Japan.
Bioorg Med Chem Lett. 2020 Jan 15;30(2):126808. doi: 10.1016/j.bmcl.2019.126808. Epub 2019 Nov 21.
Alzheimer's disease is a serious neurologic disorder that cannot be cured completely. In this study, we targeted compounds that inhibit amyloid-beta (Aβ) aggregation, based on the amyloid cascade hypothesis. Ten compounds (1-10) were isolated from CHCl extracts of the mushroom Albatrellus yasudae using Aβ-aggregation inhibitory activity-guided separation. The structures of these compounds were elucidated from 1D and 2D NMR and MS spectral data. Compounds 1-3 were novel, whereas 4-10 were identified as the known compounds grifolin, grifolic acid, neogrifolin, confluentin, 2-hydroxyneogrifolin, daurichromenic acid, and a cerebroside derivative. Compounds 1-10 were tested for Aβ-aggregation inhibitory activity. Compounds 1, 3, 5, 6, 8, and 9 have potential as Aβ-aggregation inhibitory activity.
阿尔茨海默病是一种严重的神经紊乱疾病，目前无法完全治愈。在这项研究中，我们根据淀粉样蛋白级联假说，针对抑制淀粉样蛋白-β（Aβ）聚集的化合物进行了研究。从蘑菇 Albatrellus yasudae 的 CHCl 提取物中，使用 Aβ 聚集抑制活性导向分离，分离得到了 10 种化合物（1-10）。这些化合物的结构通过 1D 和 2D NMR 和 MS 光谱数据得以阐明。化合物 1-3 是新化合物，而化合物 4-10 则被鉴定为已知化合物 grifolin、grifolic acid、neogrifolin、confluentin、2-hydroxyneogrifolin、daurichromenic acid 和神经酰胺衍生物。对化合物 1-10 进行了 Aβ 聚集抑制活性测试。化合物 1、3、5、6、8 和 9 具有抑制 Aβ 聚集的潜力。
