| Title : In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier - Cahlikova_2015_J.Nat.Prod_78_1189 |
| Author(s) : Cahlikova L , Perez DI , Stepankova S , Chlebek J , Safratova M , Host'alkova A , Opletal L |
| Ref : Journal of Natural Products , 78 :1189 , 2015 |
|
Abstract :
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. |
| PubMedSearch : Cahlikova_2015_J.Nat.Prod_78_1189 |
| PubMedID: 26030662 |
Cahlikova L, Perez DI, Stepankova S, Chlebek J, Safratova M, Host'alkova A, Opletal L (2015)
In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier
Journal of Natural Products
78 :1189
Cahlikova L, Perez DI, Stepankova S, Chlebek J, Safratova M, Host'alkova A, Opletal L (2015)
Journal of Natural Products
78 :1189