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In vitrostudy on potential pharmacological activity of curcumin analogues and their copper complexes

Authors :
Rois Benassi
Monica Saladini
Zuzana Gazova
Katarina Siposova
Erika Ferrari
Giulia Orteca
Source :
Chemical Biology & Drug Design. 89:411-419
Publication Year :
2016
Publisher :
Wiley, 2016.

Abstract

Curcumin and its derivatives have attracted great interest in the prevention and treatment of Alzheimer's disease (AD), thanks both to the ability to hinder the formation of amyloid-beta (Aβ) aggregates and the ability to bind Cu (II) ion. In this article, we explore the ability of curcumin derivatives of K2T series to affect amyloid Aβ1-40 aggregation. These derivatives were obtained by introducing the t-butyl ester group through a methylenic spacer on the central carbon atom of the β-diketo moiety of curcumin frame. The studied curcuminoids were demonstrated to inhibit Aβ1-40 fibrillization at substoichiometric concentrations with IC50 value near that of curcumin. In addition the antioxidant properties and DNA interaction of their Cu(II) complexes is evaluated. The structure of Cu(II)-K2T31 complex is also proposed on the basis of DFT calculation. This article is protected by copyright. All rights reserved.

Details

ISSN :
17470277
Volume :
89
Database :
OpenAIRE
Journal :
Chemical Biology & Drug Design
Accession number :
edsair.doi.dedup.....18844fe4ed61abbae85c090a5337aafc
Full Text :
https://doi.org/10.1111/cbdd.12847