Euphorlactone A (1), a rare rearranged ent-atisane norditerpenoid with an undescribed 3-nor-2,4-olideent-atisane scaffold, and euphorlactone B (2), a new ent-atisane diterpenoid with an unprecedented seven-membered lactone ring C, were isolated from the roots of Euphorbia fischeriana. Their planar structures with absolute configurations were extensively elucidated by analysis of 1D and 2D NMR data, electronic circular dichroism (ECD) calculations, Rh-2(OCOCF3)(4)(-)induced ECD curves, and single-crystal X-ray diffraction. Euphorlactone A (ELA) showed a remarkable AChE (acetylcholinesterase) inhibitory activity (IC50 = 2.13 +/- 0.06 mu M and K-i = 0.058 mu M), which was five times stronger than that of the positive control (rivastigmine, IC50 = 12.46 +/- 0.82 mu M), and further in vitro enzyme inhibition kinetic analysis and molecular docking studies were performed to investigate the AChE inhibitory mechanism.
基金：
Major New Drug Innovation Project of the Ministry of Science and Technology of China [2017ZX09301001]; National Natural Science Foundation of China [81574038, 82273811]; National Program for Support of Top-notch Young Professionals [0106514050]; National Key Ramp;D Program of China [2021YFA0910500]; Innovative Research Groups of the National Natural Science Foundation of China [81721005]; National Natural Science Foundation for Distinguished Young Scholars [81725021]; Academic Frontier Youth Team of HUST [2017QYTD19]
第一作者机构：[1]Shenzhen Univ, Affiliated Hosp 1, Shenzhen Peoples Hosp 2, Shenzhen 518035, Guangdong, Peoples R China[2]Ningbo Coll Hlth Sci, Wu Zhengzhi Academician Workstat, Ningbo 315800, Zhejiang, Peoples R China[3]Huazhong Univ Sci & Technol, Tongji Med Coll, Sch Pharm, Hubei Key Lab Nat Med Chem & Resource Evaluat, Wuhan 430030, Hubei, Peoples R China
共同第一作者：
通讯作者：
通讯机构：[1]Shenzhen Univ, Affiliated Hosp 1, Shenzhen Peoples Hosp 2, Shenzhen 518035, Guangdong, Peoples R China[2]Ningbo Coll Hlth Sci, Wu Zhengzhi Academician Workstat, Ningbo 315800, Zhejiang, Peoples R China
推荐引用方式(GB/T 7714)：
Wei Jiangchun,Li Zhiyue,Shan Min,et al.Discovery of two ent-atisane diterpenoid lactones with AChE inhibitory activity from the roots of Euphorbia fischeriana[J].ORGANIC & BIOMOLECULAR CHEMISTRY.2023,doi:10.1039/d3ob01007d.
APA：
Wei, Jiangchun,Li, Zhiyue,Shan, Min,Wu, Fengzhi,Li, Limin...&Wu, Zhengzhi.(2023).Discovery of two ent-atisane diterpenoid lactones with AChE inhibitory activity from the roots of Euphorbia fischeriana.ORGANIC & BIOMOLECULAR CHEMISTRY,,
MLA：
Wei, Jiangchun,et al."Discovery of two ent-atisane diterpenoid lactones with AChE inhibitory activity from the roots of Euphorbia fischeriana".ORGANIC & BIOMOLECULAR CHEMISTRY .(2023)
