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

D Karlsson; Adyary Fallarero; I Busygin; Reko Leino; P Vuorela

doi:10.1055/s-0032-1320489

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

D Karlsson, Adyary Fallarero, I Busygin, Reko Leino, P Vuorela

Research output: Contribution to journal › Conference article › Scientific › peer-review

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.

Original language	Undefined/Unknown
Pages (from-to)	1102–1102
Number of pages	1
Journal	Planta Medica
Volume	78
Issue number	11
DOIs	https://doi.org/10.1055/s-0032-1320489
Publication status	Published - 2012
MoE publication type	A4 Article in a conference publication

Access to Document

10.1055/s-0032-1320489

https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0032-1320489

Cite this

@article{74327ee32ec34579b5875ec65e613b51,

title = "Natural products as butyrylcholinesterase inhibitors - Screening of a small compound collection",

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.",

author = "D Karlsson and Adyary Fallarero and I Busygin and Reko Leino and P Vuorela",

year = "2012",

doi = "10.1055/s-0032-1320489",

language = "Odefinierat/ok{\"a}nt",

volume = "78",

pages = "1102–1102",

journal = "Planta Medica",

issn = "0032-0943",

publisher = "Thieme Gruppe",

number = "11",

}

TY - JOUR

T1 - Natural products as butyrylcholinesterase inhibitors - Screening of a small compound collection

AU - Karlsson, D

AU - Fallarero, Adyary

AU - Busygin, I

AU - Leino, Reko

AU - Vuorela, P

PY - 2012

Y1 - 2012

N2 - 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.

AB - 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.

U2 - 10.1055/s-0032-1320489

DO - 10.1055/s-0032-1320489

M3 - Konferensartikel

SN - 0032-0943

VL - 78

SP - 1102

EP - 1102

JO - Planta Medica

JF - Planta Medica

IS - 11

ER -