Isomeric 3-Pyridinylmethylcoumarins Differ in Erk1/2-Inhibition and Modulation of BV2 Microglia-Mediated Neuroinflammation
Schulzki, Rami; Apweiler, Matthias; Röttger, Caroline 1; Grathwol, Christoph W. 2; Struchtrup, Nora 1; Abou El Mirate, Sophia 1; Normann, Claus; Bräse, Stefan
1,2; Fiebich, Bernd L.
1 Institut für Organische Chemie (IOC), Karlsruher Institut für Technologie (KIT)
2 Institut für Biologische und Chemische Systeme (IBCS), Karlsruher Institut für Technologie (KIT)
1,2; Fiebich, Bernd L.1 Institut für Organische Chemie (IOC), Karlsruher Institut für Technologie (KIT)
2 Institut für Biologische und Chemische Systeme (IBCS), Karlsruher Institut für Technologie (KIT)
Abstract:
Coumarins are known for their multiple biological effects and have been estab-
lished as anti-coagulative drugs for years. Furthermore, some coumarins can promote
anti-inflammatory effects via the GPR55 receptor, and dual target coumarins have been syn-
thesized. Anti-inflammatory drugs might be beneficial in the treatment of neuropsychiatric
disorders, as the inflammatory hypothesis suggests. For the current study, we compared
isomeric 3-pyridinylmethylcoumarins with altered N-atom position regarding their effects
on cytokine and chemokine synthesis and expression in LPS-stimulated BV2 microglial
cells. The 3-pyridin-4-yl-methylcoumarin showed the most potent anti-inflammatory ef-
fects, followed by the 3-pyridin-2-ylmethylcoumarin analog. The observed effects might be
mediated by an inhibition of ERK phosphorylation.
lished as anti-coagulative drugs for years. Furthermore, some coumarins can promote
anti-inflammatory effects via the GPR55 receptor, and dual target coumarins have been syn-
thesized. Anti-inflammatory drugs might be beneficial in the treatment of neuropsychiatric
disorders, as the inflammatory hypothesis suggests. For the current study, we compared
isomeric 3-pyridinylmethylcoumarins with altered N-atom position regarding their effects
on cytokine and chemokine synthesis and expression in LPS-stimulated BV2 microglial
cells. The 3-pyridin-4-yl-methylcoumarin showed the most potent anti-inflammatory ef-
fects, followed by the 3-pyridin-2-ylmethylcoumarin analog. The observed effects might be
mediated by an inhibition of ERK phosphorylation.
| Zugehörige Institution(en) am KIT | Institut für Biologische und Chemische Systeme (IBCS) Institut für Organische Chemie (IOC) |
| Publikationstyp | Zeitschriftenaufsatz |
| Publikationsjahr | 2025 |
| Sprache | Englisch |
| Identifikator | ISSN: 1420-3049, 1431-5157 KITopen-ID: 1000184081 |
| HGF-Programm | 43.33.11 (POF IV, LK 01) Adaptive and Bioinstructive Materials Systems |
| Erschienen in | Molecules |
| Verlag | MDPI |
| Band | 30 |
| Heft | 11 |
| Seiten | Art.-Nr.: 2452 |
| Vorab online veröffentlicht am | 03.06.2025 |
| Nachgewiesen in | Web of Science OpenAlex Dimensions Scopus |
| Globale Ziele für nachhaltige Entwicklung |