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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
L. Cahlíková, DI. Pérez, Š. Štěpánková, J. Chlebek, M. Šafratová, A. Hošt'álková, L. Opletal,
Jazyk angličtina Země Spojené státy americké
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- acetylcholinesterasa metabolismus MeSH
- alkaloidy amarylkovitých farmakologie MeSH
- Alzheimerova nemoc farmakoterapie MeSH
- biologický transport účinky léků MeSH
- cholinesterasové inhibitory farmakologie MeSH
- hematoencefalická bariéra účinky léků MeSH
- lidé MeSH
- molekulární struktura MeSH
- techniky in vitro MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
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.
Citace poskytuje Crossref.org
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