BACE1 Inhibitory Meroterpenoids from Aspergillus terreus.,Journal of Natural Products

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BACE1 Inhibitory Meroterpenoids from Aspergillus terreus.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2018-09-12 , DOI: 10.1021/acs.jnatprod.7b01050
Changxing Qi ₁ , Mengting Liu ₁ , Qun Zhou ₁ , Weixi Gao ₁ , Chunmei Chen ₁ , Yongji Lai ₂ , Zhengxi Hu ₁ , Yongbo Xue ₁ , Jinwen Zhang ₃ , Dongyan Li ₃ , Xiao-Nian Li ₄ , Qing Zhang ₁ , Jianping Wang ₁ , Hucheng Zhu ₁ , Yonghui Zhang ₁

Affiliation

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 IC50 values of 3.3, 5.9, and 31.7 μM, respectively.

中文翻译：

来自土曲霉的BACE1抑制性类萜。

从土曲霉中获得了16种3,5-二甲基熊果酸类（DMOA基）的类萜，包括10种新化合物，即白萜DM（1-10）。新化合物的结构和绝对构型已通过广泛的光谱学，单晶X射线衍射分析和实验性电子圆二色性（ECD）测量得到了证实。化合物2、3和7是第一个基于3,5-二甲基亚硒酸的类萜，具有独特的顺式A / B环系统。评估了这些新化合物对β位淀粉样蛋白前体蛋白裂解酶1（BACE1）的抑制活性。化合物2、3和7中第一个具有顺式A / B环的3,5-二甲基亚硒酸类甲萜类化合物对BACE1表现出显着的抑制活性，IC50值分别为3.3、5.9和31.7μM，

更新日期：2018-09-12

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