title: In vitro study on potential pharmacological activity of curcumin analogues and their copper complexes.
abstract: 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 (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 Aβ1-40aggregation. 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 Aβ1-40fibrillization at substoichiometric concentrations with IC50value 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.
authors: Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
authors: Erika
authors: E
authors: Ferrari
authors: Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
authors: Rois
authors: R
authors: Benassi
authors: Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
authors: Monica
authors: M
authors: Saladini
authors: Department of Chemical and Geological Sciences, University of Modena and Reggio Emilia, Modena, Italy.
authors: Giulia
authors: G
authors: Orteca
authors: Department of Biophysics, Institute of Experimental Physics Slovak Academy of Sciences, Kosice, Slovakia.
authors: Zuzana
authors: Z
authors: Gazova
authors: Department of Biophysics, Institute of Experimental Physics Slovak Academy of Sciences, Kosice, Slovakia.
authors: Katarina
authors: K
authors: Siposova
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy; D016229:Amyloid beta-Peptides / Q000378:metabolism; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology*; D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology*; D003300:Copper / Q000737:chemistry* / Q000494:pharmacology; D003474:Curcumin / Q000031:analogs & derivatives* / Q000737:chemistry; D004247:DNA / Q000737:chemistry / Q000378:metabolism; D004353:Drug Evaluation, Preclinical / Q000379:methods; D016166:Free Radical Scavengers / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D018625:Microscopy, Atomic Force; D015394:Molecular Structure; D010446:Peptide Fragments / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D016229:Amyloid beta-Peptides; D000975:Antioxidants; D056831:Coordination Complexes; D016166:Free Radical Scavengers; D010446:Peptide Fragments; C078592:amyloid beta-protein (1-40); D003300:Copper; D004247:DNA; D003474:Curcumin
keywords: Alzheimer's disease; Aβ amyloid; copper complexes; curcumin analogues; protein aggregation inhibition