Evodiamine derivatives improve cognitive abilities in APP
evodiamine derivatives
mouse model
neuroprotective
spatial memory
Journal
Animal models and experimental medicine
ISSN: 2576-2095
Titre abrégé: Animal Model Exp Med
Pays: United States
ID NLM: 101726292
Informations de publication
Date de publication:
Jun 2020
Jun 2020
Historique:
received:
30
03
2020
revised:
27
05
2020
accepted:
29
05
2020
entrez:
3
7
2020
pubmed:
3
7
2020
medline:
3
7
2020
Statut:
epublish
Résumé
Alzheimer's disease (AD) is a complex neurodegenerative disease. Due to the complexity of its molecular pathogenesis and the interaction of the numerous factors involved, the etiology and pathogenesis of AD have not been fully elucidated. Therefore, effective treatment for AD remains to be developed. Evodiamine, a quinolone alkaloid, has been found to improve learning and memory ability to in the APP Evodiamine and its derivatives were effectively synthesized by EDCI-mediated condensation at room temperature. These target compounds contained 1 thio- and 21 oxo-evodiamine derivatives with different substituted groups. The cytotoxicity of evodiamine and its derivatives and the neuroprotective effects of the evodiamine derivatives against H In this study, a series of oxo- and thio-evodiamine derivatives was synthesized. Several derivatives showed lower cytotoxicity and stronger neuroprotective effects than evodiamine and elicited enhanced cognitive improvement, especially in the test of spatial memory in APP Our study provides insights for developing novel evodiamine derivatives for chemical intervention and treatment of AD.
Sections du résumé
BACKGROUND
BACKGROUND
Alzheimer's disease (AD) is a complex neurodegenerative disease. Due to the complexity of its molecular pathogenesis and the interaction of the numerous factors involved, the etiology and pathogenesis of AD have not been fully elucidated. Therefore, effective treatment for AD remains to be developed. Evodiamine, a quinolone alkaloid, has been found to improve learning and memory ability to in the APP
METHODS
METHODS
Evodiamine and its derivatives were effectively synthesized by EDCI-mediated condensation at room temperature. These target compounds contained 1 thio- and 21 oxo-evodiamine derivatives with different substituted groups. The cytotoxicity of evodiamine and its derivatives and the neuroprotective effects of the evodiamine derivatives against H
RESULTS
RESULTS
In this study, a series of oxo- and thio-evodiamine derivatives was synthesized. Several derivatives showed lower cytotoxicity and stronger neuroprotective effects than evodiamine and elicited enhanced cognitive improvement, especially in the test of spatial memory in APP
CONCLUSION
CONCLUSIONS
Our study provides insights for developing novel evodiamine derivatives for chemical intervention and treatment of AD.
Identifiants
pubmed: 32613178
doi: 10.1002/ame2.12126
pii: AME212126
pmc: PMC7323704
doi:
Types de publication
Journal Article
Langues
eng
Pagination
193-199Informations de copyright
© 2020 The Authors. Animal Models and Experimental Medicine published by John Wiley & Sons Australia, Ltd on behalf of The Chinese Association for Laboratory Animal Sciences.
Déclaration de conflit d'intérêts
None.
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