BACE1 Inhibitory Meroterpenoids from Aspergillus terreus

被引：31

作者：

Qi, Changxing ^{[1
]}

Liu, Mengting ^{[1
]}

Zhou, Qun ^{[1
]}

Gao, Weixi ^{[1
]}

Chen, Chunmei ^{[1
]}

Lai, Yongji ^{[2
]}

Hu, Zhengxi ^{[1
]}

Xue, Yongbo ^{[1
]}

Zhang, Jinwen ^{[3
]}

Li, Dongyan ^{[3
]}

Li, Xiao-Nian ^{[4
]}

Zhang, Qing ^{[1
]}

Wang, Jianping ^{[1
]}

Zhu, Hucheng ^{[1
]}

Zhang, Yonghui ^{[1
]}

机构：

[1] Huazhong Univ Sci & Technol, Tongji Med Coll, Hubei Key Lab Nat Med Chem & Resource Evaluat, Wuhan 430030, Hubei, Peoples R China

[2] Huazhong Univ Sci & Technol, Tongji Med Coll, Cent Hosp Wuhan, Dept Pharm, Wuhan 430030, Hubei, Peoples R China

[3] Huazhong Univ Sci & Technol, Tongji Hosp, Tongji Med Coll, Dept Pharm, Wuhan 430030, Hubei, Peoples R China

[4] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Yunnan, Peoples R China

来源：

JOURNAL OF NATURAL PRODUCTS | 2018年 / 81卷 / 09期

基金：

中国国家自然科学基金; 中国博士后科学基金;

关键词：

ALZHEIMERS-DISEASE; AMYLOID-BETA; BIOSYNTHESIS;

D O I：

10.1021/acs.jnatprod.7b01050

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

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 beta-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 mu M, respectively.

引用

页码：1937 / 1945

页数：9

共 21 条

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