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In vitrostudy on potential pharmacological activity of curcumin analogues and their copper complexes
- 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.
- Subjects :
- 0301 basic medicine
Curcumin
Antioxidant
Amyloid
Stereochemistry
medicine.medical_treatment
Drug Evaluation, Preclinical
chemistry.chemical_element
Curcumin analogues
Microscopy, Atomic Force
010402 general chemistry
01 natural sciences
Biochemistry
Antioxidants
Inhibitory Concentration 50
Structure-Activity Relationship
03 medical and health sciences
chemistry.chemical_compound
Alzheimer Disease
Coordination Complexes
Drug Discovery
medicine
Humans
In vitro study
Moiety
IC50
Alzheimer's disease
Aβ amyloid
Copper complexes
Protein aggregation inhibition
Molecular Medicine
Pharmacology
Amyloid beta-Peptides
Molecular Structure
Chemistry
Organic Chemistry
Biological activity
DNA
Free Radical Scavengers
Copper
Peptide Fragments
0104 chemical sciences
030104 developmental biology
Subjects
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