Schulzki Rami, Apweiler Matthias, Röttger Caroline, Grathwol Christoph W, Struchtrup Nora, Abou El Mirate Sophia, Normann Claus, Bräse Stefan, Fiebich Bernd L
Neuroimmunology and Neurochemistry Research Group, Department of Psychiatry and Psychotherapy, Medical Center-University of Freiburg, Faculty of Medicine, University of Freiburg, D-79104 Freiburg, Germany.
Institute of Organic Chemistry (IOC), Karlsruhe Institute of Technology (KIT), Kaiserstraße 12, D-76131 Karlsruhe, Germany.
Molecules. 2025 Jun 3;30(11):2452. doi: 10.3390/molecules30112452.
Coumarins are known for their multiple biological effects and have been established as anti-coagulative drugs for years. Furthermore, some coumarins can promote anti-inflammatory effects via the GPR55 receptor, and dual target coumarins have been synthesized. 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 effects, followed by the 3-pyridin-2-ylmethylcoumarin analog. The observed effects might be mediated by an inhibition of ERK phosphorylation.
香豆素因其多种生物学效应而闻名，多年来一直被用作抗凝血药物。此外，一些香豆素可通过GPR55受体发挥抗炎作用，并且已经合成了双靶点香豆素。如炎症假说所示，抗炎药物可能对神经精神疾病的治疗有益。在本研究中，我们比较了N原子位置改变的异构3-吡啶基甲基香豆素对脂多糖刺激的BV2小胶质细胞中细胞因子和趋化因子合成及表达的影响。3-吡啶-4-基甲基香豆素显示出最有效的抗炎作用，其次是3-吡啶-2-基甲基香豆素类似物。观察到的效应可能是由ERK磷酸化的抑制介导的。
