KIT | KIT-Bibliothek | Impressum | Datenschutz

Functional Selectivity of Coumarin Derivates Acting via GPR55 in Neuroinflammation

Apweiler, Matthias; Streyczek, Jana; Saliba, Soraya Wilke; Collado, Juan Antonio; Hurrle, Thomas; Gräßle, Simone; Muñoz, Eduardo; Normann, Claus; Hellwig, Sabine; Bräse, Stefan; Fiebich, Bernd L.

Abstract:

Anti-neuroinflammatory treatment has gained importance in the search for pharmacological treatments of different neurological and psychiatric diseases, such as depression, schizophrenia, Parkinson’s disease, and Alzheimer’s disease. Clinical studies demonstrate a reduction of the mentioned diseases’ symptoms after the administration of anti-inflammatory drugs. Novel coumarin derivates have been shown to elicit anti-neuroinflammatory effects via G-protein coupled receptor GPR55, with possibly reduced side-effects compared to the known anti-inflammatory drugs. In this study, we, therefore, evaluated the anti-inflammatory capacities of the two novel coumarin-based compounds, KIT C and KIT H, in human neuroblastoma cells and primary murine microglia. Both compounds reduced PGE$_{2}$-concentrations likely via the inhibition of COX-2 synthesis in SK-N-SH cells but only KIT C decreased PGE$_{2}$-levels in primary microglia. The examination of other pro- and anti-inflammatory parameters showed varying effects of both compounds. Therefore, the differences in the effects of KIT C and KIT H might be explained by functional selectivity as well as tissue- or cell-dependent expression and signal pathways coupled to GPR55. ... mehr


Verlagsausgabe §
DOI: 10.5445/IR/1000142402
Veröffentlicht am 27.01.2022
Originalveröffentlichung
DOI: 10.3390/ijms23020959
Scopus
Zitationen: 4
Web of Science
Zitationen: 4
Dimensions
Zitationen: 5
Cover der Publikation
Zugehörige Institution(en) am KIT Institut für Biologische und Chemische Systeme (IBCS)
Institut für Organische Chemie (IOC)
Publikationstyp Zeitschriftenaufsatz
Publikationsjahr 2022
Sprache Englisch
Identifikator ISSN: 1661-6596, 1422-0067
KITopen-ID: 1000142402
HGF-Programm 43.33.11 (POF IV, LK 01) Adaptive and Bioinstructive Materials Systems
Erschienen in International Journal of Molecular Sciences
Verlag MDPI
Band 23
Heft 2
Seiten 959
Schlagwörter neuroinflammation; GPR55; coumarin derivates; PGE2; functional selectivity; SK-N-SH; primary microglia
Nachgewiesen in Dimensions
Web of Science
Scopus
KIT – Die Forschungsuniversität in der Helmholtz-Gemeinschaft
KITopen Landing Page