Department of Food Science and Nutrition, Pukyong National University, Busan, South Korea.
J Pharm Pharmacol. 2013 Jun;65(6):895-906. doi: 10.1111/jphp.12049. Epub 2013 Mar 18.
Microglial activation has been implicated in neurological disorders for its inflammatory and neurotrophic effects. We investigated the anti-inflammatory effect of the hexane fraction from Myagropsis myagroides (Mertens ex Turner) Fensholt ethanolic extract and its underlying molecular mechanism in lipopolysaccharide-stimulated microglia.
Various solvent fractions prepared from the ethanolic extract of M. myagroides were analysed for total phenolic content, 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activity and inhibitory effect on nitric oxide (NO) production in activated BV-2 microglia. We measured prostaglandin E2 (PGE2 ) and pro-inflammatory cytokine levels by enzyme-linked immunosorbent assay. Expression of inflammatory enzymes was analysed by Western blot. Nuclear translocation and activation of nuclear factor-kappaB (NF-κB) were determined by immunofluorescence and reporter gene assay, respectively.
Among the fractions, the hexane fraction (MMH), rich in fatty acid, showed the highest inhibitory activity on NO generation. Pretreatment with MMH decreased mRNA and protein levels of inducible NO synthase and cyclooxygenase-2, resulting in a decrease in NO and PGE2 in LPS-stimulated BV-2 cells. Furthermore, MMH inhibited the production of inducible pro-inflammatory cytokines at their transcriptional level via inactivation of NF-κB. MMH inhibited the activation of extracellular signal-regulated kinase and c-Jun N-terminal kinase.
These results indicate that MMH has a strong anti-inflammatory activity in LPS-stimulated microglia, suggesting that MMH can be used as a therapeutic agent against neuroinflammatory diseases.
小胶质细胞的激活与炎症和神经营养作用有关，被认为与神经紊乱有关。我们研究了从 Myagropsis myagroides (Mertens ex Turner) Fensholt 乙醇提取物的己烷部分的抗炎作用及其在脂多糖刺激的小胶质细胞中的潜在分子机制。
分析了 M. myagroides 乙醇提取物的各种溶剂部分的总酚含量、2,2-二苯基-1-苦基肼自由基清除活性以及对激活的 BV-2 小胶质细胞中一氧化氮（NO）产生的抑制作用。我们通过酶联免疫吸附试验测量前列腺素 E2 (PGE2) 和促炎细胞因子水平。通过 Western blot 分析炎症酶的表达。通过免疫荧光和报告基因测定分别测定核因子-κB (NF-κB) 的核易位和激活。
在这些部分中，富含脂肪酸的己烷部分 (MMH) 显示出对 NO 生成的最高抑制活性。用 MMH 预处理可降低 LPS 刺激的 BV-2 细胞中诱导型一氧化氮合酶和环氧化酶-2 的 mRNA 和蛋白水平，导致 NO 和 PGE2 减少。此外，MMH 通过 NF-κB 的失活抑制诱导型促炎细胞因子在转录水平的产生。MMH 抑制细胞外信号调节激酶和 c-Jun N 端激酶的激活。
这些结果表明，MMH 在 LPS 刺激的小胶质细胞中具有很强的抗炎活性，表明 MMH 可作为治疗神经炎症性疾病的药物。
