In vitro study on potential pharmacological activity of curcumin analogues and their copper complexes.
Chem Biol Drug Des
; 89(3): 411-419, 2017 03.
Article
en En
| MEDLINE
| ID: mdl-27569739
Curcumin and its derivatives have attracted great interest in the prevention and treatment of Alzheimer's disease, thanks both to the ability to hinder the formation of amyloid-beta (Aß) 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 Aß1-40 aggregation. These derivatives were obtained by introducing the t-butyl ester group through a methylenic spacer on the central carbon atom of the ß-diketo moiety of curcumin frame. The studied curcuminoids were demonstrated to inhibit Aß1-40 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.
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Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Cobre
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Curcumina
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Complejos de Coordinación
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Antioxidantes
Idioma:
En
Revista:
Chem Biol Drug Des
Año:
2017
Tipo del documento:
Article
País de afiliación:
Italia