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

Abstract：

:A series of chalcone derivatives were synthesized and evaluated for their μ-calpain and cathepsin B inhibitory activities. Among the tested chalcone derivatives, two compounds, 7 and 11, showed potent inhibitory activities against μ-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 Aβ peptide formation. Enzyme kinetic experiments and docking studies revealed that compounds 7 and 11 competitively inhibited both μ-calpain and cathepsin B enzymes.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Jeon KH,Lee E,Jun KY,Eom JE,Kwak SY,Na Y,Kwon Y

doi

10.1016/j.ejmech.2016.06.008

subject

Has Abstract

pub_date

2016-10-04 00:00:00

pages

433-444

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30485-8

journal_volume

121

pub_type

杂志文章

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