In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier
Language English Country United States Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Acetylcholinesterase metabolism MeSH
- Amaryllidaceae Alkaloids pharmacology MeSH
- Alzheimer Disease drug therapy MeSH
- Biological Transport drug effects MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Blood-Brain Barrier drug effects MeSH
- Humans MeSH
- Molecular Structure MeSH
- In Vitro Techniques MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 8-demethylmaritidine MeSH Browser
- Acetylcholinesterase MeSH
- Amaryllidaceae Alkaloids MeSH
- Cholinesterase Inhibitors MeSH
- undulatine MeSH Browser
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.
References provided by Crossref.org
The Genus Nerine Herb. (Amaryllidaceae): Ethnobotany, Phytochemistry, and Biological Activity
Amaryllidaceae Alkaloids as Potential Glycogen Synthase Kinase-3β Inhibitors
