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Eur J Med Chem ; 150: 140-155, 2018 Apr 25.
Article in English | MEDLINE | ID: mdl-29525434

ABSTRACT

Alzheimer's disease (AD) is a progressive neurodegenerative disorder affecting tens of million people. Currently marketed drugs have limited therapeutic efficacy and only slowing down the neurodegenerative process. Interestingly, it has been suggested that biometal cations in the amyloid beta (Aß) aggregate deposits contribute to neurotoxicity and degenerative changes in AD. Thus, chelation therapy could represent novel mode of therapeutic intervention. Here we describe the features of chelators with therapeutically relevant mechanism of action. We have found that the tested compounds effectively reduce the toxicity of exogenous Aß and suppress its endogenous production as well as decrease oxidative stress. Cholyl hydrazones were found to be the most active compounds. In summary, our data show that cation complexation, together with improving transport efficacy may represent basis for eventual treatment strategy in AD.


Subject(s)
Alzheimer Disease/drug therapy , Chelating Agents/pharmacology , Chelation Therapy , Cholinesterase Inhibitors/pharmacology , Metals/pharmacology , Alzheimer Disease/metabolism , Amyloid beta-Peptides/antagonists & inhibitors , Amyloid beta-Peptides/metabolism , Cations/chemistry , Cations/pharmacology , Cell Proliferation/drug effects , Cell Survival/drug effects , Chelating Agents/chemical synthesis , Chelating Agents/chemistry , Cholinesterase Inhibitors/chemical synthesis , Cholinesterase Inhibitors/chemistry , Dose-Response Relationship, Drug , Humans , Metals/chemistry , Molecular Structure , Protein Aggregates/drug effects , Structure-Activity Relationship , Tumor Cells, Cultured
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