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Amaryllidaceae alkaloids with new framework types from Zephyranthes candida as potent acetylcholinesterase inhibitors
发布时间：2025-04-30
- 论文名称：
- Amaryllidaceae alkaloids with new framework types from Zephyranthes candida as potent acetylcholinesterase inhibitors
- 发表刊物：
- European Journal of Medicinal Chemistry
- 摘要：
- Abstract：
Three new Amaryllidaceae alkaloids, named zephycandidines IIII (1e3), were isolated from Zephyranthes candida. The structures of 13 were elucidated by spectroscopic analyses including HRESIMS, 1H NMR, 13C NMR, DEPT, HSQC, 1H1H COSY, HMBC, ROESY, and electronic circular dichroism (ECD), as well as ECD calculation. The absolute configuration of 1 was finally established by single crystal X-ray diffraction using Cu Ka radiation. Zephycandidines I (1) and III (3) with new framework types represent the first example of 7-phenyl-hexahydroindole and 5,2'-dimethyl-biphenyl-2-ylamine alkaloids, respectively, and their plausible biosynthetic pathway are proposed. Zephycandidine II (2) is the first C3a-phenyl-hexahydroindole type alkaloid isolated from the genus of Zephyranthes. These new alkaloids
1e3 were evaluated for their acetylcholinesterase (AChE) inhibitory activities, and 3 showed potent AChE inhibitory activity with an IC50 value of 8.82 mM, suggesting that the framework of 5,2'-dimethylbiphenyl-2-ylamine in 3 may be a potential group for the AChE inhibitory activity. The docking studies of 1-3 and galanthamine with AChE revealed that interactions with W286 and Y337 are necessary for the
AChE inhibitory activity.
- 合写作者：
- Guanqun Zhan, Junjun Liu, Guangmin Yao, et al.
- 卷号：
- 127
- 页面范围：
- 771
- 是否译文：
- 否
- 发表时间：
- 2016-10-27
