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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Conjugates of desferrioxamine and aromatic amines improve markers of iron-dependent neurotoxicity

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Author(s):
Carvalho, Rodrigo R. V. [1] ; Peres, Tanara V. [2] ; Liria, Cleber W. [3] ; Machini, M. Teresa [3] ; Aschner, Michael [2] ; Esposito, Breno P. [1]
Total Authors: 6
Affiliation:
[1] Univ Sao Paulo, Dept Fundamental Chem, Inst Chem, Sao Paulo, SP - Brazil
[2] Albert Einstein Coll Med, Dept Mol Pharmacol, Bronx, NY 10467 - USA
[3] Univ Sao Paulo, Inst Chem, Dept Biochem, Sao Paulo, SP - Brazil
Total Affiliations: 3
Document type: Journal article
Source: BIOMETALS; v. 34, n. 2 JAN 2021.
Web of Science Citations: 0
Abstract

Alzheimer's Disease (AD) is a complex neurodegenerative disorder associated in some instances with dyshomeostasis of redox-active metal ions, such as copper and iron. In this work, we investigated whether the conjugation of various aromatic amines would improve the pharmacological efficacy of the iron chelator desferrioxamine (DFO). Conjugates of DFO with aniline (DFOANI), benzosulfanylamide (DFOBAN), 2-naphthalenamine (DFONAF) and 6-quinolinamine (DFOQUN) were obtained and their properties examined. DFOQUN had good chelating activity, promoted a significant increase in the inhibition of beta-amyloid peptide aggregation when compared to DFO, and also inhibited acetylcholinesterase (AChE) activity both in vitro and in vivo (Caenorhabditis elegans). These data indicate that the covalent conjugation of a strong iron chelator to an AChE inhibitor offers a powerful approach for the amelioration of iron-induced neurotoxicity symptoms. (AU)

FAPESP's process: 15/14360-4 - Magnetic bionanocatalysts: preparation, characterization, properties and use in protein and peptide chemistry
Grantee:Maria Teresa Machini
Support Opportunities: Regular Research Grants
FAPESP's process: 18/19684-0 - Applications of new desferrioxamine derivatives with high cell permeability
Grantee:Breno Pannia Esposito
Support Opportunities: Regular Research Grants
FAPESP's process: 16/03709-9 - Modulation of the levels and reactivity of physiological iron by mean of new natural or bifunctional chelators: possible applications in human health
Grantee:Breno Pannia Esposito
Support Opportunities: Regular Research Grants