Evaluation of Anti-Neuroinflammatory Activity of Isatin Derivatives in Activated Microglia.
Alejandro CenalmorElena PascualSergio Gil-MansoRafael Correa-RochaJosé Ramón SuárezIsabel García-ÁlvarezPublished in: Molecules (Basel, Switzerland) (2023)
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 N 1 -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.
Keyphrases
- inflammatory response
- lps induced
- lipopolysaccharide induced
- induced apoptosis
- toll like receptor
- nitric oxide
- neuropathic pain
- cell cycle arrest
- endoplasmic reticulum stress
- cell death
- big data
- hydrogen peroxide
- traumatic brain injury
- cell therapy
- cognitive decline
- bone marrow
- subarachnoid hemorrhage
- spinal cord
- stem cells
- artificial intelligence
- immune response
- oxidative stress
- high resolution
- brain injury
- machine learning