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来自于……的生物活性氮杂卓 - 吲哚生物碱

Bioactive Azepine-Indole Alkaloids from .

作者信息

Klein-Júnior Luiz C, Cretton Sylvian, Vander Heyden Yvan, Gasper André L, Nejad-Ebrahimi Samad, Christen Philippe, Henriques Amélia T

机构信息

Laboratory of Pharmacognosy and Quality Control of Phytomedicines, Faculty of Pharmacy, Universidade Federal do Rio Grande do Sul-UFRGS, 90610-000 Porto Alegre/RS Brazil.

Department of Analytical Chemistry, Applied Chemometrics and Molecular Modelling, Center for Pharmaceutical Research (CePhaR), Vrije Universiteit Brussel-VUB, B-1090 Brussels, Belgium.

出版信息

J Nat Prod. 2020 Apr 24;83(4):852-863. doi: 10.1021/acs.jnatprod.9b00469. Epub 2020 Mar 9.

Abstract

Phytochemical investigation of the alkaloid extract of the aerial parts of led to the isolation and characterization of 10 azepine-indole alkaloids, i.e., cimitrypazepine (), fargesine (), nemorosines A (), and B (), nemorosinosides A-F (-), as well as two β-carboline derivatives, 10-hydroxyisodolichantoside () and 10-hydroxydolichantoside (), an isoxazole alkaloid, nemorosinoside G (), serotonin (), bufotenine (), and ()-gentianol (). Compounds - have not yet been described. These compounds were isolated by semipreparative HPLC, and their structures were determined by means of HRMS, NMR, and ECD measurements. In addition, the monoamine oxidase-A (MAO-A), MAO-B, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) inhibitory activities were evaluated. Alkaloids - inhibited the MAO-A activity with IC values of 1.4, 1.4, and 0.9 μM, respectively.

摘要

对[植物名称]地上部分生物碱提取物进行的植物化学研究,导致分离并鉴定出10种氮杂卓 - 吲哚生物碱,即西米曲氮杂卓()、法尔吉辛()、内莫罗辛A()和B()、内莫罗辛苷A - F( - ),以及两种β - 咔啉衍生物,10 - 羟基异多利香豆素苷()和10 - 羟基多利香豆素苷()、一种异恶唑生物碱、内莫罗辛苷G()、血清素()、蟾蜍特宁()和() - 龙胆醇()。化合物 - 尚未见报道。这些化合物通过半制备高效液相色谱法分离,其结构通过高分辨质谱、核磁共振和电子圆二色光谱测量确定。此外,还评估了单胺氧化酶 - A(MAO - A)、单胺氧化酶 - B、乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)的抑制活性。生物碱 - 分别以1.4、1.4和0.9 μM的IC值抑制MAO - A活性。

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