Evaluation of Anti-Neuroinflammatory Activity of Isatin Derivatives in Activated Microglia

Neuroinflammation plays a crucial role in the progression of Alzheimer’s disease and other neurodegenerative disorders. Overactivated microglia cause neurotoxicity and prolong the inflammatory response in many neuropathologies. In this study, we have synthesised a series of isatin derivatives to eva...

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Detalles Bibliográficos
Autores: Cenalmor, Alejandro, Pascual, Elena, Gil-Manso, Sergio, Correa-Rocha, Rafael, Ramón Suárez, José, García-Álvarez, Isabel
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2023
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/378699
Acceso en línea:http://hdl.handle.net/10261/378699
Access Level:acceso abierto
Palabra clave:Neuroinflammation
Microglia
Isatin
Nitric oxide
Interleukin 6
TNF-α
Descripción
Sumario:Neuroinflammation plays a crucial role in the progression of Alzheimer’s disease and other neurodegenerative disorders. Overactivated microglia cause neurotoxicity and prolong the inflammatory response in many neuropathologies. In this study, we have synthesised a series of isatin derivatives to evaluate their anti-neuroinflammatory potential using lipopolysaccharide activated microglia as a cell model. We explored four different substitutions of the isatin moiety by testing their anti-neuroinflammatory activity on BV2 microglia cells. Based on the low cytotoxicity and the activity in reducing the release of nitric oxide, pro-inflammatory interleukin 6 and tumour necrosis factor α by microglial cells, the N1-alkylated compound 10 and the chlorinated 20 showed the best results at 25 μM. Taken together, the data suggest that 10 and 20 are promising lead compounds for developing new neuroprotective agents.