Effect of viologen-phosphorus dendrimers on acetylcholinesterase and butyrylcholinesterase activities

Int J Biol Macromol. 2013 Mar:54:119-24. doi: 10.1016/j.ijbiomac.2012.12.002. Epub 2012 Dec 10.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

  • Dendrimers
  • Viologens
  • Phosphorus
  • Acetylcholinesterase
  • Butyrylcholinesterase