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Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy

Romero, Alejandro ; Marco-Contelles, José ; Ramos, Eva

Neural regeneration research, 2020-01, Vol.15 (1), p.30-35 [Periódico revisado por pares]

India: Wolters Kluwer India Pvt. Ltd

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Título:
Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy
Autor: Romero, Alejandro ; Marco-Contelles, José ; Ramos, Eva
Assuntos: AChE; BuChE; gene expression; heat shock proteins; inflammation; in silico toxicology; MAO A/B; neuroprotection; oxidative stress; Wnt signaling ; Alzheimer's disease ; Amines ; Anti-Alzheimer's disease agents ; Antioxidants ; Antioxidants (Nutrients) ; Apoptosis ; Binding sites ; Blood-brain barrier ; Cyclin-dependent kinases ; Design ; Diagnosis ; Disease ; Donepezil ; Drug therapy ; Enzymes ; Kinases ; Ligands ; Memantine ; Metabolism ; Metabolites ; Monoamine oxidase ; Oxidases ; Physiological aspects ; Review ; Testing
É parte de: Neural regeneration research, 2020-01, Vol.15 (1), p.30-35
Notas: Author contributions: Data collection, manuscript writing and critical revision: AR, ER; critical revision: JMC. All authors approved the final version of the manuscript.
Descrição: There is no effective treatment to face Alzheimer's disease complexity. Multitarget molecules are a good approach against the multiple physiopathological events associated with its development and progression. In this context, N-((5-(3-(1-benzylpiperidin-4-yl) propoxy)-1- methyl-1H-indol-2-yl)methyl)-N-methylprop-2-yn-1-amine (ASS234) has been tested achieving promising results. ASS234 has demonstrated to cross the blood-brain barrier in vivo, and a good in silico safety profile being less toxic than donepezil. Besides, ASS234 reversibly inhibits human acetyl- and butyryl-cholinesterase, and irreversibly inhibits human monoamine oxidase A and B. Moreover, this multitarget molecule has antioxidant and neuroprotective properties, and inhibits Αβ1-42 and Αβ1-40 self-aggregation. Inquiring about the mechanism of action, several signaling pathways related to Alzheimer's disease had been explored showing that ASS234 induces the wingless-type MMTV integration site (Wnt) family and several members of the heat shock proteins family and moreover counteracts neuroinflammatory and oxidative stress-related genes promoting the induction of several key antioxidant genes. Finally, in vivo experiments with ASS234 in C57BL/6J mice displayed its ability to reduce amyloid plaque burden and gliosis in the cortex and hippocampus, ameliorating scopolamine-induced learning deficits. Here we gather the information regarding ASS234 evaluated so far, showing its ability to face different targets, necessary to counteract a neurodegenerative disease as complex as the Alzheimer's disease.
Editor: India: Wolters Kluwer India Pvt. Ltd
Idioma: Inglês;Chinês

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Highlights of ASS234: a novel and promising therapeutic agent for Alzheimer's disease therapy

Romero, Alejandro ; Marco-Contelles, José ; Ramos, Eva

India: Wolters Kluwer India Pvt. Ltd

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