达旦醇 A-C，真菌来源的 BACE1 抑制剂。
Daedalols A-C, fungal-derived BACE1 inhibitors.
机构信息
Department of Chemistry, University of Hawai'i at Manoa, Honolulu, HI 96822, United States.
出版信息
Bioorg Med Chem. 2011 Nov 15;19(22):6581-6. doi: 10.1016/j.bmc.2011.09.029. Epub 2011 Sep 22.
Abstract
Bioassay-guided fractionation of an extract prepared from the fruiting bodies of a Daedalea sp. has led to the isolation of daedalols A-C (1-3). The structures of these new triterpenes were elucidated based on extensive NMR spectroscopic and mass spectrometric measurements. Assignment of the relative configuration of 3 required the preparation of a suitable derivative via a Payne rearrangement. The aspartic protease BACE1, an Alzheimer's drug target, was inhibited by 3 with an IC(50) value of 14.2 μM.
摘要
从一种戴氏蘑菇（Daedalea sp.）的子实体中提取的物质经生物测定指导分离，得到了 daedalols A-C（1-3）。这些新三萜的结构是基于广泛的 NMR 光谱和质谱测量来阐明的。3 的相对构型的分配需要通过 Payne 重排制备合适的衍生物。天冬氨酸蛋白酶 BACE1 是阿尔茨海默病药物的靶点，3 对其的抑制作用的 IC50 值为 14.2 μM。
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