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奥莫希宁 A-P,结构多样的具有 AChE 抑制作用的喹诺利啶生物碱,来自.

Ormosianines A-P, Structurally Diverse Quinolizidine Alkaloids with AChE Inhibitory Effects from .

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China.

University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China.

出版信息

J Nat Prod. 2023 Sep 22;86(9):2193-2205. doi: 10.1021/acs.jnatprod.3c00493. Epub 2023 Aug 17.

DOI:10.1021/acs.jnatprod.3c00493
PMID:37589667
Abstract

Sixteen new quinolizidine alkaloids (QAs), named ormosianines A-P (-), and 18 known congeners (-) were isolated from the stems and leaves of . The structures were elucidated based on spectroscopic analyses and electron circular dichroism (ECD) calculations. Structurally, ormosianines A () and B () are the first examples of cytisine and type alkaloids with the cleavage of the piperidine ring. Results of the acetylcholinesterase (AChE) inhibitory assay revealed that the pentacycline type QAs, including , , , and -, are good AChE inhibitors. Ormosianine A () exhibited more potent AChE inhibitory activity with an IC value of 1.55 μM. Molecular docking revealed that might bind to the protein 1DX4, forming two hydrogen bonds with residues SER-238 and HIS-480.

摘要

十六种新的喹诺利啶生物碱(QAs),命名为奥罗米辛 A-P(-),以及 18 种已知同系物(-)从 Ormosia henryi 的茎和叶中分离出来。基于光谱分析和电子圆二色性(ECD)计算确定了其结构。结构上,奥罗米辛 A()和 B()是第一个具有哌啶环裂解的 cytisine 和型生物碱的例子。乙酰胆碱酯酶(AChE)抑制试验的结果表明,包括、、、和-在内的五环型 QAs 是良好的 AChE 抑制剂。奥罗米辛 A()对乙酰胆碱酯酶(AChE)具有更强的抑制活性,IC 值为 1.55 μM。分子对接表明,可能与蛋白 1DX4 结合,与残基 SER-238 和 HIS-480 形成两个氢键。

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