Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease

Karim Jiménez-Aligaga, Paloma Bermejo-Bescós, Sagrario Martín-Aragón, Aurelio G. Csákÿ

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.

Original languageEnglish
Pages (from-to)426-429
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number2
DOIs
StatePublished - 15 Jan 2013

Bibliographical note

Funding Information:
This work was supported by grant CTQ2010-6170 from the Ministerio de Economía y Competitividad from the government of Spain. We thank Fundación Folch for a pre-doctoral grant to K. J.-A.

Keywords

  • Boronic acids
  • Caspase
  • Glutathione
  • Lipid peroxidation
  • β-Amyloid fibrillogenesis

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