Merging memantine and ferulic acid to probe connections between NMDA receptors, oxidative stress and amyloid-β peptide in Alzheimer's disease.

Alzheimer Disease / drug therapy Amyloid beta-Peptides / antagonists & inhibitors Cell Survival / drug effects Coumaric Acids / chemical synthesis Dose-Response Relationship, Drug Humans Memantine / chemical synthesis Molecular Structure Neuroprotective Agents / chemical synthesis Oxidative Stress / drug effects Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors Structure-Activity Relationship Tumor Cells, Cultured
Amyloid-β peptide Ferulic acid Memantine NMDA receptors Oxidative stress

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
15 Oct 2019
Historique:
received: 10 06 2019
revised: 02 07 2019
accepted: 03 07 2019
pubmed: 14 7 2019
medline: 5 11 2019
entrez: 14 7 2019
Statut: ppublish

Résumé

N-methyl-d-aspartate receptors (NMDAR) are critically involved in the pathogenesis of Alzheimer's disease (AD). Acting as an open-channel blocker, the anti-AD drug memantine preferentially targets NMDAR overactivation, which has been proposed to trigger neurotoxic events mediated by amyloid β peptide (Aβ) and oxidative stress. In this study, we applied a multifunctional approach by conjugating memantine to ferulic acid, which is known to protect the brain from Aβ neurotoxicity and neuronal death caused by ROS. The most interesting compound (7) behaved, like memantine, as a voltage-dependent antagonist of NMDAR (IC

Identifiants

DOI: 10.1016/j.ejmech.2019.07.011 PMID: 31301562
pubmed: 31301562
pii: S0223-5234(19)30632-4
doi: 10.1016/j.ejmech.2019.07.011
pii:
doi:

Substances chimiques

Amyloid beta-Peptides 0
Coumaric Acids 0
Neuroprotective Agents 0
Receptors, N-Methyl-D-Aspartate 0
ferulic acid AVM951ZWST
Memantine W8O17SJF3T

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

111-120

Informations de copyright

Copyright © 2019 Elsevier Masson SAS. All rights reserved.

Auteurs

Michela Rosini (M)

Department of Pharmacy and Biotechnology, Alma Mater Studiorum - University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy. Electronic address: michela.rosini@unibo.it.

Elena Simoni (E)

Department of Pharmacy and Biotechnology, Alma Mater Studiorum - University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy.

Roberta Caporaso (R)

Department of Pharmacy and Biotechnology, Alma Mater Studiorum - University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy.

Filippo Basagni (F)

Department of Pharmacy and Biotechnology, Alma Mater Studiorum - University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy.

Michele Catanzaro (M)

Department of Drug Sciences (Pharmacology Section), University of Pavia, V.le Taramelli 14, 27100, Pavia, Italy.

Izuddin F Abu (IF)

School of Life Sciences, University of Nottingham, University Park, Nottingham, NG7 2RD, UK; Universiti Kuala Lumpur, Institute of Medical Science Technology, A1-1, Jalan TKS1, Taman Kajang Sentral, 43000, Kajang, Selangor, Malaysia.

Francesca Fagiani (F)

Department of Drug Sciences (Pharmacology Section), University of Pavia, V.le Taramelli 14, 27100, Pavia, Italy; Scuola Universitaria Superiore IUSS Pavia, P.zza Vittoria, 15, 27100, Pavia, Italy.

Federica Fusco (F)

Department of Neuroscience, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, 20156, Milan, Italy.

Sara Masuzzo (S)

Department of Neuroscience, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, 20156, Milan, Italy.

Diego Albani (D)

Department of Neuroscience, Istituto di Ricerche Farmacologiche Mario Negri IRCCS, Via Mario Negri 2, 20156, Milan, Italy.

Cristina Lanni (C)

Department of Drug Sciences (Pharmacology Section), University of Pavia, V.le Taramelli 14, 27100, Pavia, Italy.

Ian R Mellor (IR)

School of Life Sciences, University of Nottingham, University Park, Nottingham, NG7 2RD, UK.

Anna Minarini (A)

Department of Pharmacy and Biotechnology, Alma Mater Studiorum - University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy. Electronic address: anna.minarini@unibo.it.

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Classifications MeSH

questionsmedicales.fr › Troubles mentaux › Troubles neurocognitifs › Démence › Maladie d'Alzheimer › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Peptides bêta-amyloïdes › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Survie cellulaire › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Composés chimiques organiques › Acides carboxyliques › Acides carbocycliques › Cinnamates › Acides coumariques › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures cycliques › Amantadine › Mémantine › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Agents du système nerveux central › Neuroprotecteurs › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Phénomènes physiologiques › Stress physiologique › Stress oxydatif › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteurs au glutamate › Récepteurs ionotropes du glutamate › Récepteurs du N-méthyl-D-aspartate › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Merging memantine and ferulic acid to probe...
questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Merging memantine and ferulic acid to probe...