来自紫堇的异喹啉生物碱及其与阿尔茨海默病相关的生物活性。

Isoquinoline Alkaloids from Fumaria officinalis L. and Their Biological Activities Related to Alzheimer's Disease.

作者信息

Chlebek Jakub, Novák Zdeněk, Kassemová Dominika, Šafratová Marcela, Kostelník Jan, Malý Lukáš, Ločárek Miroslav, Opletal Lubomír, Hošt'álková Anna, Hrabinová Martina, Kuneš Jiří, Novotná Pavlína, Urbanová Marie, Nováková Lucie, Macáková Kateřina, Hulcová Daniela, Solich Petr, Pérez Martín Concepción, Jun Daniel, Cahlíková Lucie

机构信息

ADINACO Research Group, Department of Pharmaceutical Botany and Ecology, Faculty of Pharmacy, Charles University, Heyrovského 1203, CZ-500 05 Hradec Králové, (phone: +420-495-067311; fax: +420-495-067162).

Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, CZ-500 05 Hradec Králové

出版信息

Chem Biodivers. 2016 Jan;13(1):91-9. doi: 10.1002/cbdv.201500033.

DOI:10.1002/cbdv.201500033

PMID:26765356

Abstract

Two new isoquinoline alkaloids, named fumaranine (2) and fumarostrejdine (10), along with 18 known alkaloids were isolated from aerial parts of Fumaria officinalis. The structures of the isolated compounds were elucidated on the basis of spectroscopic analyses and by comparison with literature data. The absolute configuration of the new compound 2 was determined by comparing its circular dichroism spectra with those of known analogs. Compounds isolated in sufficient amounts were evaluated for their acetylcholinesterase, butyrylcholinesterase, prolyl oligopeptidase (POP), and glycogen synthase kinase-3β inhibitory activities. Parfumidine (8) and sinactine (15) exhibited potent POP inhibition activities (IC50 99±5 and 53±2 μM, resp.).

摘要

从紫堇的地上部分分离出两种新的异喹啉生物碱，分别命名为富马兰宁（2）和富马罗斯捷丁（10），以及18种已知生物碱。通过光谱分析并与文献数据比较，阐明了分离得到的化合物的结构。通过将新化合物2的圆二色光谱与已知类似物的圆二色光谱进行比较，确定了其绝对构型。对分离得到的足量化合物进行了乙酰胆碱酯酶、丁酰胆碱酯酶、脯氨酰寡肽酶（POP）和糖原合酶激酶-3β抑制活性的评估。帕夫米定（8）和辛那亭（15）表现出较强的POP抑制活性（IC50分别为99±5和53±2 μM）。