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Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus.

Abstract：

:Inhibition of acetylcholinesterase (AChE) and therefore prevention of acetylcholine degradation is one of the most accepted therapy opportunities for Alzheimer s disease (AD), today. Due to lack of selectivity of AChE inhibitor drugs on the market, AD-patients suffer from side effects like nausea or vomiting. In the present study the isolation of two alkaloids, infractopicrin (1) and 10-hydroxy-infractopicrin (2), from Cortinarius infractus Berk. (Cortinariaceae) is presented. Both compounds show AChE-inhibiting activity and possess a higher selectivity than galanthamine. Docking studies show that lacking pi-pi-interactions in butyrylcholinesterase (BChE) are responsible for selectivity. Studies on other AD pathology related targets show an inhibitory effect of both compounds on self-aggregation of Abeta-peptides but not on AChE induced Abeta-peptide aggregation. Low cytotoxicity as well as calculated pharmacokinetic data suggest that the natural products could be useful candidates for further drug development.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Geissler T,Brandt W,Porzel A,Schlenzig D,Kehlen A,Wessjohann L,Arnold N

doi

10.1016/j.bmc.2010.01.074

subject

Has Abstract

pub_date

2010-03-15 00:00:00

pages

2173-2177

issue

6

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00105-7

journal_volume

18

pub_type

杂志文章

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