Spiroterreusnoids A-F, six undescribed spiro-dioxolane-containing adducts bearing 3,5-dimethylorsellinic acid-based meroterpenoid and 2,3-butanediol moieties were isolated from the endophytic fungus Aspergillus terreus Thom from Tripterygium wilfordii Hook. f. (Celastraceae). The structures of these adducts were established by spectroscopy, single-crystal X-ray diffraction, and experimental electronic circular dichroism (ECD) measurements. Spiroterreusnoids A-F represent the first examples of adducts composed of 3,5-dimethylorsellinic acidbased meroterpenoids. It is noteworthy that spiroterreusnoids A-F possessing a spiro-dioxolane moiety exhibited potential abilities in inhibiting BACE1 (IC50 values ranging from 5.86 to 27.16 mu M) and AchE (IC50 values ranging from 22.18 to 32.51 mu M), while the other analogues without this fragment displayed no such activities. Taken together, spiroterreusnoids A-F represent the first multitargeted natural adducts that could inhibit BACE1 and AchE, and might provide a new template for the development of new anti-Alzheimer's disease drugs.
基金：
National Natural Science Foundation of China [81502943, 31600266, 81573316, 21602068, 31670354, 31370372, 21702067]; Program for Changjiang Scholars [T2016088]; China Postdoctoral Science Foundation [2018M632879, 2017M610479, 2018T110777]; National Science Fund for Distinguished Young Scholars [81725021]; Innovative Research Groups of the National Natural Science Foundation of China [81721005]
第一作者单位：[1]Huazhong Univ Sci & Technol, Tongji Med Coll, Sch Pharm, Hubei Key Lab Nat Med Chem & Resource Evaluat, Wuhan 430030, Hubei, Peoples R China
通讯作者：
推荐引用方式(GB/T 7714)：
Qi Changxing,Zhou Qun,Gao Weixi,et al.Anti-BACE1 and anti-AchE activities of undescribed spiro-dioxolane-containing meroterpenoids from the endophytic fungus Aspergillus terreus Thom[J].PHYTOCHEMISTRY.2019,165:doi:10.1016/j.phytochem.2019.05.014.
APA：
Qi, Changxing,Zhou, Qun,Gao, Weixi,Liu, Mengting,Chen, Chunmei...&Zhang, Yonghui.(2019).Anti-BACE1 and anti-AchE activities of undescribed spiro-dioxolane-containing meroterpenoids from the endophytic fungus Aspergillus terreus Thom.PHYTOCHEMISTRY,165,
MLA：
Qi, Changxing,et al."Anti-BACE1 and anti-AchE activities of undescribed spiro-dioxolane-containing meroterpenoids from the endophytic fungus Aspergillus terreus Thom".PHYTOCHEMISTRY 165.(2019)
