Obovatol attenuates microglia‐mediated neuroinflammation by modulating redox regulation

British Journal of Pharmacology
2010.0

Abstract

<jats:p><jats:bold>Background and purpose: </jats:bold> Obovatol isolated from the medicinal herb <jats:italic>Magnolia obovata</jats:italic> exhibits a variety of biological activities. Here, the effect of obovatol and its mechanism of action on microglial activation, neuroinflammation and neurodegeneration were investigated.<jats:p><jats:bold>Experimental approach: </jats:bold> In microglial BV‐2 cells stimulated with lipopolysaccharide (LPS), we measured nitric oxide (NO) and cytokine production, and activation of intracellular signalling pathways by reverse transcription‐polymerase chain reaction and Western blots. Cell death was assayed in co‐cultures of activated microglia (with bacterial LPS) and neurons and in LPS‐induced neuroinflammation in mice <jats:italic>in vivo.</jats:italic><jats:p><jats:bold>Key results: </jats:bold> Obovatol inhibited microglial NO production with an IC<jats:sub>50</jats:sub> value of 10 µM. Obovatol also inhibited microglial expression of proinflammatory cytokines and inducible nitric‐oxide synthase, which was accompanied by the inhibition of multiple signalling pathways such as nuclear factor kappa B, signal transducers and activators of transcription 1, and mitogen‐activated protein kinases. In addition, obovatol protected cultured neurons from microglial toxicity and inhibited neuroinflammation in mice <jats:italic>in vivo.</jats:italic> One molecular target of obovatol in microglia was peroxiredoxin 2 (Prx2), identified by affinity chromatography and mass spectrometry. Obovatol enhanced the reactive oxygen species (ROS)‐scavenging activity of Prx2 <jats:italic>in vitro</jats:italic>, thereby suppressing proinflammatory signalling pathways of microglia where ROS plays an important role.<jats:p><jats:bold>Conclusions and implications: </jats:bold> Obovatol is not only a useful chemical tool that can be used to investigate microglial signalling, but also a promising drug candidate against neuroinflammatory diseases. Furthermore, our results indicate that Prx2 is a novel drug target that can be exploited for the therapeutic modulation of neuroinflammatory signalling.

Knowledge Graph

Similar Paper

Obovatol attenuates microglia‐mediated neuroinflammation by modulating redox regulation
British Journal of Pharmacology 2010.0
Arylbenzofuran isolated from Dalbergia odorifera suppresses lipopolysaccharide-induced mouse BV2 microglial cell activation, which protects mouse hippocampal HT22 cells death from neuroinflammation-mediated toxicity
European Journal of Pharmacology 2014.0
Anti-inflammatory effects of higenamine (Hig) on LPS-activated mouse microglia (BV2) through NF-κB and Nrf2/HO-1 signaling pathways
International Immunopharmacology 2020.0
α-Cyperone inhibits LPS-induced inflammation in BV-2 cells through activation of Akt/Nrf2/HO-1 and suppression of the NF-κB pathway
Food &amp; Function 2018.0
Obovatol inhibits colorectal cancer growth by inhibiting tumor cell proliferation and inducing apoptosis
Bioorganic &amp; Medicinal Chemistry 2008.0
Anti-Inflammatory Role of the Isoflavone Diadzein in Lipopolysaccharide-Stimulated Microglia: Implications for Parkinson’s Disease
Neurotoxicity Research 2013.0
Neuroprotective role of tripchlorolide on inflammatory neurotoxicity induced by lipopolysaccharide-activated microglia
Biochemical Pharmacology 2008.0
Z-ligustilide attenuates lipopolysaccharide-induced proinflammatory response via inhibiting NF-κB pathway in primary rat microglia
Acta Pharmacologica Sinica 2010.0
Oxymatrine Attenuates Dopaminergic Neuronal Damage and Microglia-Mediated Neuroinflammation Through Cathepsin D-Dependent HMGB1/TLR4/NF-κB Pathway in Parkinson’s Disease
Frontiers in Pharmacology 2020.0
Inhibitory effect of 9-hydroxy-6,7-dimethoxydalbergiquinol from Dalbergia odorifera on the NF-κB-related neuroinflammatory response in lipopolysaccharide-stimulated mouse BV2 microglial cells is mediated by heme oxygenase-1
International Immunopharmacology 2013.0