曲霉属中具有 BACE1 抑制作用的倍半萜类化合物。
BACE1 Inhibitory Meroterpenoids from Aspergillus terreus.
机构信息
Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, Tongji Medical College , Huazhong University of Science and Technology , Wuhan , Hubei Province 430030 , People's Republic of China.
Department of Pharmacy, The Central Hospital of Wuhan, Tongji Medical College , Huazhong University of Science and Technology , Wuhan , Hubei Province 430030 , People's Republic of China.
出版信息
J Nat Prod. 2018 Sep 28;81(9):1937-1945. doi: 10.1021/acs.jnatprod.7b01050. Epub 2018 Sep 12.
Sixteen 3,5-dimethylorsellinic acid-based (DMOA-based) meroterpenoids, including 10 new compounds, asperterpenes D-M (1-10), were obtained from Aspergillus terreus. The structures and absolute configurations of the new compounds were confirmed by extensive spectroscopy, single-crystal X-ray diffraction analysis, and experimental electronic circular dichroism (ECD) measurements. Compounds 2, 3, and 7 are the first 3,5-dimethylorsellinic acid-based meroterpenoids possessing a unique cis-fused A/B ring system. These new compounds were evaluated for their inhibitory activity against β-site amyloid precursor protein-cleaving enzyme 1 (BACE1). Compounds 2, 3, and 7, the first 3,5-dimethylorsellinic acid-based meroterpenoids possessing cis-fused A/B rings, exhibited significant inhibitory activities against BACE1 with IC values of 3.3, 5.9, and 31.7 μM, respectively.
十六个基于 3,5-二甲基奥尔酸（DMOA）的混合萜类化合物，包括 10 个新化合物，asperterpenes D-M（1-10），从土曲霉中获得。新化合物的结构和绝对构型通过广泛的光谱、单晶 X 射线衍射分析和实验电子圆二色性（ECD）测量来确定。化合物 2、3 和 7 是第一个具有独特顺式稠合 A/B 环系统的基于 3,5-二甲基奥尔酸的混合萜类化合物。这些新化合物被评估了对β-位点淀粉样前体蛋白切割酶 1（BACE1）的抑制活性。化合物 2、3 和 7，第一个具有顺式稠合 A/B 环的基于 3,5-二甲基奥尔酸的混合萜类化合物，对 BACE1 表现出显著的抑制活性，IC 值分别为 3.3、5.9 和 31.7 μM。
Zotero 插件