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The protective effect of the TSPO ligands 2,4-Di-Cl-MGV-1, CB86, and CB204 against LPS-induced M1 pro-inflammatory activation of microglia
- Source :
- Brain, Behavior, & Immunity-Health, Vol 5, Iss, Pp 100083-(2020), Brain, Behavior, & Immunity-Health
- Publication Year :
- 2020
- Publisher :
- Elsevier BV, 2020.
-
Abstract
- We have shown previously, that the 18 kDa translocator protein (TSPO) synthetic ligands quinazoline derivatives (2-Cl-MGV-1 and MGV-1) can inhibit activation of in BV-2 microglial cells. In the present study we assessed the impact of novel TSPO ligands on lipopolysaccharide (LPS)-induced microglial activation as expressed by release of pro-inflammatory molecules, including cytokines [interleukin-6 (IL-6), IL-1β, interferon- γ (IFN-γ)] nitric oxide (NO), CD8, and cyclo-oxygenase-2 (COX-2). The TSPO ligands 2,4-Di-Cl-MGV-1, CB86, and CB204 counteracted with the LPS-induced microglial activation. Exposure to LPS along with the TSPO ligand 2,4-Di-Cl-MGV-1 (25 μM) reduced significantly the release of NO by 24-, IL-6 by 14-, IL-β by 14-, IFN- γ by 6-, and TNF-α by 29-folds, respectively. In contrast to the anti-neuroinflammatory effect of the TSPO ligands, the effect of diclofenac sodium (DS; 25 μM) did not reach statistical significance. No alterations in IL-10 and IL-13 were detected (M2 anti-inflammatory pathway) during the inhibition of M1 pro-inflammatory pathway.
- Subjects :
- Lipopolysaccharide
Translocator protein (TSPO)
Pro-inflammatory cytokines
Neurosciences. Biological psychiatry. Neuropsychiatry
Pharmacology
BV-2 cell line
Nitric oxide
Proinflammatory cytokine
chemistry.chemical_compound
Neuroinflammation
Interferon
Full Length Article
LPS (Lipopolysaccharide)
2,4-Di-Cl-MGV-1
Translocator protein
medicine
Microglial activation
General Environmental Science
biology
Microglia
Diclofenac Sodium
medicine.anatomical_structure
chemistry
M1 and M2 pathway
biology.protein
General Earth and Planetary Sciences
RC321-571
medicine.drug
Subjects
Details
- ISSN :
- 26663546
- Volume :
- 5
- Database :
- OpenAIRE
- Journal :
- Brain, Behavior, & Immunity - Health
- Accession number :
- edsair.doi.dedup.....36707c92867775956d571551ac6c2b69
- Full Text :
- https://doi.org/10.1016/j.bbih.2020.100083