Effect of viologen-phosphorus dendrimers on acetylcholinesterase and butyrylcholinesterase activities.

Abstract

The inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) is the first step in checking whether new compounds can be considered as drugs for treating neurodegenerative diseases. The effect of viologen-phosphorus dendrimers on AChE and BChE activities was studied. The results show that the effects on the cholinesterase activities depend on dendrimer type and size. Viologen dendrimers can interact with the enzymes in two ways: they can bind either to a peripheral site of the enzyme or to amino acids located near the active site, inhibiting catalysis by both cholinesterases. All tested non-toxic viologen-phosphorus dendrimers inhibited the activities of both cholinesterases, showing their potential as new drugs for treating neurodegenerative diseases.

• Authors: Karol Ciepluch, Monika Weber, Nadia Katir, Anne-Marie Caminade, Abdelkrim El Kadib, Barbara Klajnert, Jean Pierre Majoral, Maria Bryszewska
• Journal: International journal of biological macromolecules (Int J Biol Macromol) Vol. 54 Pg. 119-24 (Mar 2013) ISSN: 1879-0003 [Electronic] Netherlands
• PMID: 23237795 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2012 Elsevier B.V. All rights reserved.

Chemical References

• Dendrimers
• Viologens
• Phosphorus
• Acetylcholinesterase
• Butyrylcholinesterase

Topics

• Acetylcholinesterase (metabolism)
• Butyrylcholinesterase (metabolism)
• Circular Dichroism
• Dendrimers (chemistry, pharmacology)
• Erythrocyte Membrane (drug effects, enzymology)
• Fluorescence
• Humans
• Phosphorus (chemistry, pharmacology)
• Static Electricity
• Viologens (chemistry, pharmacology)