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In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier
Authors: Cahlikova Lucie | Perez Daniel I. | Štěpánková Šárka | Chlebek Jakub | Safratova Marcela | Host'alkova Anna | Opletal Lubomir
Year: 2015
Type of publication: článek v odborném periodiku
Name of source: Journal of Natural Products
Publisher name: American Chemical Society
Place: Washington
Page from-to: 1189-1192
Titles:
Language Name Abstract Keywords
cze In vitro inhibiční účinnost 8-O-demethylmaritidinu a undulatinu vůči acetylcholinesteráze a jejich předpokládaný průchod přes hematoencefalickou bariéru Alzheimerova choroba je jedna z nejběžnějších příčin demence. Inhibice acetylcholinesterázy (AChE) je v současné době nejpoužívanějším způsobem léčby. Velké množství přírodních látek je schopno inhibovat AChE. V této práci byl studován mechanismus inhibice AChE dvěma alkaloidy rostli čeledi Amaryllidaceae (8-O-demethylmaritidin a undulatin) a jejich možný přechod přes hematoencefalickou bariéru. U obou látek byl určen smíšený typ inhibice a jen undulatin je schopen přecházet přes hematoencefalickou bariéru. inhibiční účinnost; 8-O-demethylmaritidin; undulatin; acetylcholinesteráza; hematoencefalická bariéra
eng In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier Alzheimer's disease is the most common cause of dementia. Currently, acetylcholinesterase (AChE) inhibition is the most widely used therapeutic treatment. A large number of naturally occurring compounds have been found to inhibit AChE. In this report the mechanism of AChE inhibition of two Amaryllidaceae alkaloids, 8-O-demethylmaritidine (1) and undulatine (2), and their possible penetration across the blood-brain barrier have been studied. Both compounds act via a mixed inhibition mechanism. Based on the parallel artificial permeation assay (PAMPA) for the prediction of blood brain barrier (BBB) penetration, only 2 should be able to cross the BBB by passive permeation. alzheimers-disease; prolyl oligopeptidase; alkaloids; butyrylcholinesterase; therapies; protein; drug; beta

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