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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
- 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
- Jeon, Kyung-Hwa; Lee, Eunyoung; Jun, Kyu-Yeon; Eom, Ji-Eun; Kwak, Soo Yeon; Na, Younghwa; Kwon, Youngjoo
- Ewha Authors
- SCOPUS Author ID
- Issue Date
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- 0223-5234; 1768-3254
- vol. 121, pp. 433 - 444
- Alzheimer's disease; Chalcone; mu-Calpain inhibitor; Cathepsin B inhibitor; A beta formation; Tau hyperphosphorylation
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- SCI; SCIE; SCOPUS
- 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.
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