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BACE1 Inhibitory Meroterpenoids from Aspergillus terreus

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单位: [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
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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.

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出版当年[2017]版:
大类 | 2 区 生物
小类 | 2 区 药物化学 2 区 药学 2 区 植物科学
最新[2025]版:
大类 | 2 区 生物学
小类 | 2 区 药物化学 2 区 药学 2 区 植物科学
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出版当年[2016]版:
Q1 CHEMISTRY, MEDICINAL Q1 PLANT SCIENCES Q2 PHARMACOLOGY & PHARMACY
最新[2023]版:
Q1 PLANT SCIENCES Q2 CHEMISTRY, MEDICINAL Q2 PHARMACOLOGY & PHARMACY

影响因子: 最新[2023版] 最新五年平均 出版当年[2016版] 出版当年五年平均 出版前一年[2015版] 出版后一年[2017版]

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第一作者单位: [1]Huazhong Univ Sci & Technol, Tongji Med Coll, Hubei Key Lab Nat Med Chem & Resource Evaluat, Wuhan 430030, Hubei, Peoples R China
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