Anti-inflammatory effects of GPR55 agonists and antagonists in LPS-treated BV2 microglial cells
Abstract: Chronic inflammation is driven by proinflammatory cytokines such as interleukin 6 (IL-6), tumor necrosis factor-α (TNF-α), and chemokines, such as c-c motif chemokine ligand 2 (CCL2), CCL3, C-X-C motif chemokine ligand 2 (CXCL2), and CXCL10. Inflammatory processes of the central nervous system (CNS) play an important role in the pathogenesis of various neurological and psychiatric disorders like Alzheimer’s disease, Parkinson’s disease, and depression. Therefore, identifying novel anti-inflammatory drugs may be beneficial for treating disorders with a neuroinflammatory background. The G-protein-coupled receptor 55 (GPR55) gained interest due to its role in inflammatory processes and possible involvement in different disorders. This study aims to identify the anti-inflammatory effects of the coumarin-based compound KIT C, acting as an antagonist with inverse agonistic activity at GPR55, in lipopolysaccharide (LPS)-stimulated BV2 microglial cells in comparison to the commercial GPR55 agonist O-1602 and antagonist ML-193. All compounds significantly suppressed IL-6, TNF-α, CCL2, CCL3, CXCL2, and CXCL10 expression and release in LPS-treated BV2 microglial cells. The anti-inflammatory effects of the compounds are partially explained by modulation of the phosphorylation of p38 mitogen-activated protein kinase (MAPK), p42/44 MAPK (ERK 1/2), protein kinase C (PKC) pathways, and the transcription factor nuclear factor (NF)-κB, respectively. Due to its potent anti-inflammatory properties, KIT C is a promising compound for further research and potential use in inflammatory-related disorders
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Notes
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Pharmaceuticals. - 17, 6 (2024) , 674, ISSN: 1424-8247
- Event
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Veröffentlichung
- (where)
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Freiburg
- (who)
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Universität
- (when)
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2024
- Creator
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Sun, Lu
Apweiler, Matthias Benedikt
Normann, Claus
Grathwol, Christoph Werner
Hurrle, Thomas
Gräßle, Simone
Jung, Nicole
Bräse, Stefan
Fiebich, Bernd L.
- DOI
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10.3390/ph17060674
- URN
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urn:nbn:de:bsz:25-freidok-2493010
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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25.03.2025, 1:41 PM CET
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Sun, Lu
- Apweiler, Matthias Benedikt
- Normann, Claus
- Grathwol, Christoph Werner
- Hurrle, Thomas
- Gräßle, Simone
- Jung, Nicole
- Bräse, Stefan
- Fiebich, Bernd L.
- Universität
Time of origin
- 2024
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Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters
Influence of Dopaminergic Agonists/Antagonists on Fucose Metabolism in the Rat Brain
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Investigation of the binding site of agonists and antagonists at the human neuropeptide Y receptor family
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Combined anti-inflammatory effects of β2-adrenergic agonists and PDE4 inhibitors on astrocytes by upregulation of intracellular cAMP
Anti-neuroinflammatory effects of GPR55 antagonists in LPS-activated primary microglial cells
Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters
Influence of Dopaminergic Agonists/Antagonists on Fucose Metabolism in the Rat Brain
Peptides in oncology, 1.. LH-RH agonists and antagonists : with 11 tables
Where Do We Draw the Line? Interlopers, (Ant)agonists, and an Unbounded Journalistic Field
Opioid agonists, antagonists and mixed narcotic analgesics : theoret. background and considerations for pract. use
Activation of murine microglial cells by muramyl dipeptide alone and in combination with Toll-like receptor agonists
Investigation of the binding site of agonists and antagonists at the human neuropeptide Y receptor family
Asymmetric synthesis and histamine receptor activity of new H1-receptor agonists and conformationally restricted H3-receptor antagonists
Cardiovascular effects of dihydropyridine type calcium antagonists and agonists : [held at Boppard, Germany, October 3 - 6, 1984]
Activin A increases phagocytosis of Escherichia coli K1 by primary murine microglial cells activated by toll-like receptor agonists