Natural products as butyrylcholinesterase inhibitors - Screening of a small compound collection

A1 Journal article (refereed)


Internal Authors/Editors


Publication Details

List of Authors: Karlsson D, Fallarero A, Busygin I, Leino R, Vuorela P
Publisher: GEORG THIEME VERLAG KG
Publication year: 2012
Journal: Planta Medica
Journal acronym: PLANTA MED
Volume number: 78
Issue number: 11
Start page: 1102
End page: 1102
Number of pages: 1
ISSN: 0032-0943


Abstract

Investigation of the involvement of butyrylcholinesterase (BChE) in
diseases such as Alzheimer's disease (AD), type 2 diabetes mellitus
(T2DM) and multiple sclerosis (MS) makes it a valuable target for drug
discovery. Cholinesterase inhibitors of natural origin have shown
success in AD therapy and have encouraged further exploration of nature
as a source of cholinesterase inhibitors. Using the Ellman's reaction a
collection of 111 compounds containing commercially available compounds
e.g. flavonoids and coumarins, as well as a subset of cinchona alkaloid
derivatives synthesized by our group, were screened for
anti-cholinesterase activity. Two cinchona alkaloids were found to
inhibit the hydrolase activity of BChE in the micromolar range (IC50
≤10µM) and were further characterized. Considering their wide medical
use (mostly as antimalarials) the cinchona alkaloid scaffold may serve
as an advantage in drug development for various diseases.


Last updated on 2019-14-11 at 04:32