The First Affiliated Hospital of Shenzhen University, Shenzhen Second People's Hospital, Shenzhen 518035, Guangdong Province, People's Republic of China.
Wu Zhengzhi Academician Workstation, Ningbo College of Health Sciences, Ningbo 315800, Zhejiang Province, People's Republic of China.
Org Biomol Chem. 2023 Aug 30;21(34):6949-6955. doi: 10.1039/d3ob01007d.
Euphorlactone A (1), a rare rearranged -atisane norditerpenoid with an undescribed 3--2,4-olide--atisane scaffold, and euphorlactone B (2), a new -atisane diterpenoid with an unprecedented seven-membered lactone ring C, were isolated from the roots of . Their planar structures with absolute configurations were extensively elucidated by analysis of 1D and 2D NMR data, electronic circular dichroism (ECD) calculations, Rh(OCOCF)-induced ECD curves, and single-crystal X-ray diffraction. Euphorlactone A (ELA) showed a remarkable AChE (acetylcholinesterase) inhibitory activity (IC = 2.13 ± 0.06 μM and = 0.058 μM), which was five times stronger than that of the positive control (rivastigmine, IC = 12.46 ± 0.82 μM), and further enzyme inhibition kinetic analysis and molecular docking studies were performed to investigate the AChE inhibitory mechanism.
euphorlactone A (1)，一种罕见的重排 -atisane 倍半萜，具有未描述的 3--2,4-内酯--atisane 支架，和 euphorlactone B (2)，一种具有前所未有的七元内酯环 C 的新 -atisane 二萜，从 的根部分离得到。通过分析 1D 和 2D NMR 数据、电子圆二色性 (ECD) 计算、Rh(OCOCF)-诱导的 ECD 曲线和单晶 X 射线衍射，详细阐明了它们的平面结构和绝对构型。Euphorlactone A (ELA) 表现出显著的 AChE（乙酰胆碱酯酶）抑制活性（IC = 2.13 ± 0.06 μM 和 = 0.058 μM），比阳性对照（rivastigmine，IC = 12.46 ± 0.82 μM）强五倍，进一步进行了酶抑制动力学分析和分子对接研究，以研究 AChE 抑制机制。
