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Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against mu-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble A beta peptide formation

Title
Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against mu-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble A beta peptide formation
Authors
Jeon, Kyung-HwaLee, EunyoungJun, Kyu-YeonEom, Ji-EunKwak, Soo YeonNa, YounghwaKwon, Youngjoo
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2016
Journal Title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN
0223-5234JCR Link1768-3254JCR Link
Citation
vol. 121, pp. 433 - 444
Keywords
Alzheimer's diseaseChalconemu-Calpain inhibitorCathepsin B inhibitorA beta formationTau hyperphosphorylation
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of chalcone derivatives were synthesized and evaluated for their mu-calpain and cathepsin B inhibitory activities. Among the tested chalcone derivatives, two compounds, 7 and 11, showed potent inhibitory activities against mu-calpain and cathepsin B and were selected for further evaluation. Compounds 7 and 11 showed enzyme inhibitory activities at the cellular level and displayed neuroprotective effects against oxidative stress-induced apoptosis in SH-SY5Y cells, a human neuroblastoma cell line. Moreover, compounds 7 and 11 reduced p25 formation, tau phosphorylation and insoluble A beta peptide formation. Enzyme kinetic experiments and docking studies revealed that compounds 7 and 11 competitively inhibited both mu-calpain and cathepsin B enzymes. (C) 2016 Elsevier Masson SAS. All rights reserved.
DOI
10.1016/j.ejmech.2016.06.008
Appears in Collections:
약학대학 > 약학과 > Journal papers
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