Isomeric 3-Pyridinylmethylcoumarins Differ in Erk1/2-Inhibition and Modulation of BV2 Microglia-Mediated Neuroinflammation.

IF 4.2 2区 化学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Rami Schulzki, Matthias Apweiler, Caroline Röttger, Christoph W Grathwol, Nora Struchtrup, Sophia Abou El Mirate, Claus Normann, Stefan Bräse, Bernd L Fiebich
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引用次数: 0

Abstract

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.

异构体3-吡啶甲基香豆素在BV2小胶质细胞介导的神经炎症中erk1 /2抑制和调节的差异
香豆素因其多种生物效应而闻名,多年来一直被认为是抗凝血药物。此外,一些香豆素可以通过GPR55受体促进抗炎作用,双靶香豆素已被合成。正如炎症假说所表明的那样,抗炎药物可能对治疗神经精神疾病有益。在本研究中,我们比较了n原子位置改变的异构体3-吡啶甲基香豆素对lps刺激的BV2小胶质细胞中细胞因子和趋化因子合成和表达的影响。3-吡啶-4-基甲基香豆素表现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通过抑制ERK磷酸化介导的。
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来源期刊
Molecules
Molecules 化学-有机化学
CiteScore
7.40
自引率
8.70%
发文量
7524
审稿时长
1.4 months
期刊介绍: Molecules (ISSN 1420-3049, CODEN: MOLEFW) is an open access journal of synthetic organic chemistry and natural product chemistry. All articles are peer-reviewed and published continously upon acceptance. Molecules is published by MDPI, Basel, Switzerland. Our aim is to encourage chemists to publish as much as possible their experimental detail, particularly synthetic procedures and characterization information. There is no restriction on the length of the experimental section. In addition, availability of compound samples is published and considered as important information. Authors are encouraged to register or deposit their chemical samples through the non-profit international organization Molecular Diversity Preservation International (MDPI). Molecules has been launched in 1996 to preserve and exploit molecular diversity of both, chemical information and chemical substances.
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