Quercetin Derivatives from Siegesbeckia glabrescens Inhibit the Expression of COX-2 Through the Suppression of NF-kappa B Activation in Microglia
- Authors
- Lim, Hyo Jin; Li, Hua; Kim, Jae Yeon; Ryu, Jae-Ha
- Issue Date
- 31-Jan-2011
- Publisher
- KOREAN SOC APPLIED PHARMACOLOGY
- Keywords
- Siegesbeckia glabrescens; Quercetin; Cyclooxygenase; Nuclear factor kappa B; Microglia
- Citation
- BIOMOLECULES & THERAPEUTICS, v.19, no.1, pp 27 - 32
- Pages
- 6
- Journal Title
- BIOMOLECULES & THERAPEUTICS
- Volume
- 19
- Number
- 1
- Start Page
- 27
- End Page
- 32
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/12695
- DOI
- 10.4062/biomolther.2011.19.1.027
- ISSN
- 1976-9148
2005-4483
- Abstract
- The activation of microglia induces the overproduction of inflammatory mediators that are responsible for the neurodegenerative disorders including Alzheimer's disease and Parkinson's disease. The large amounts of prostaglandin E-2 (PGE(2)) produced by inducible cyclooxygenase (COX-2) is one of the main inflammatory mediators that can contribute to neurodegeneration. The inhibition of COX-2 thus may provide therapeutic strategy for the treatment of neurodegenerative diseases. From the activity-guided purification of EtOAc soluble fraction of Siegesbeckia glabrescens, four compounds were isolated as inhibitors of PGE(2) production in LPS-activated microglia. Their structures were determined as 3, 4'-dimethylquercetin (1), 3, 7-dimethylquercetin (2), 3-methylquercetin (3) and 3, 7, 4'-trimethylquercetin (4) by the mass and NMR spectral data analysis. The compounds 1-4 showed dose-dependent inhibition of PGE(2) production in LPS-activated microglia with their IC50 values of 7.1, 4.9, 4.4, 12.4 mu M respectively. They reduced the expression of protein and mRNA of COX-2 through the inhibition of I-kappa B alpha degradation and NF-kappa B activity that were correlated with the inactivation of p38 and ERK. Therefore the active compounds from Siegesbeckia glabrescens may have therapeutic effects on neuro-inflammatory diseases through the inhibition of overproduction of PGE(2) and suppression of COX-2 overexpression.
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