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In vitro study on potential pharmacological activity of curcumin analogues and their copper complexes.
Ferrari, Erika; Benassi, Rois; Saladini, Monica; Orteca, Giulia; Gazova, Zuzana; Siposova, Katarina.
Afiliación
  • Ferrari E; Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
  • Benassi R; Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
  • Saladini M; Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
  • Orteca G; Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
  • Gazova Z; Department of Biophysics, Institute of Experimental Physics Slovak Academy of Sciences, Kosice, Slovakia.
  • Siposova K; Department of Biophysics, Institute of Experimental Physics Slovak Academy of Sciences, Kosice, Slovakia.
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 / Curcumina / Complejos de Coordinación / Antioxidantes Idioma: En Revista: Chem Biol Drug Des Año: 2017 Tipo del documento: Article País de afiliación: Italia

Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Cobre / Curcumina / Complejos de Coordinación / Antioxidantes Idioma: En Revista: Chem Biol Drug Des Año: 2017 Tipo del documento: Article País de afiliación: Italia