Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- acetylcholinesterasa metabolismus MeSH
- alkaloidy chemie izolace a purifikace terapeutické užití MeSH
- Alzheimerova nemoc farmakoterapie MeSH
- Berberis chemie MeSH
- butyrylcholinesterasa metabolismus MeSH
- cholinesterasové inhibitory terapeutické užití MeSH
- hematoencefalická bariéra účinky léků MeSH
- isochinoliny chemie izolace a purifikace terapeutické užití MeSH
- lidé MeSH
- magnetická rezonanční spektroskopie MeSH
- rostlinné exsudáty analýza MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- acetylcholinesterasa MeSH
- alkaloidy MeSH
- butyrylcholinesterasa MeSH
- cholinesterasové inhibitory MeSH
- isochinoliny MeSH
- rostlinné exsudáty MeSH
Three new alkaloids, bersavine (3), muraricine (4), and berbostrejdine (8), together with seven known isoquinoline alkaloids (1-2, 5-7, 9, and 10) were isolated from an alkaloidal extract of the root bark of Berberis vulgaris. The structures of the isolated compounds were determined by spectroscopic methods, including 1D and 2D NMR techniques, HRMS, and optical rotation, and by comparison of the obtained data with those in the literature. The NMR data of berbamine (5), aromoline (6), and obamegine (7) were completely assigned employing 2D NMR experiments. Alkaloids isolated in sufficient amounts were evaluated for their in vitro acetylcholinesterase, butyrylcholinesterase (BuChE), prolyl oligopeptidase, and glycogen synthase kinase-3β inhibitory activities. Selected compounds were studied for their ability to permeate through the blood-brain barrier. Significant human BuChE ( hBuChE) inhibitory activity was demonstrated by 6 (IC50 = 0.82 ± 0.10 μM). The in vitro data were further supported by computational analysis that showed the accommodation of 6 in the active site of hBuChE.
Centro de Investigaciones Biologicas CSIC Avenida Ramiro de Maeztu 9 28040 Madrid Spain
Department for Life Quality Studies University of Bologna Corso D'Augusto 237 47921 Rimini Italy
Department of Toxicoloxy and Military Pharmacy Trebesska 1575 500 05 Hradec Kralove Czech Republic
Citace poskytuje Crossref.org
Natural Alkaloids as Multi-Target Compounds towards Factors Implicated in Alzheimer's Disease
