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Bioactive lignan derivatives from the stems of Firmiana simplex

机译:枯草的茎中具有生物活性的木脂素衍生物

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摘要

The CHCl3 soluble fraction of the 80% MeOH extract of the stems of Firmiana simplex strongly inhibited nitric oxide production in lipopolysaccharide-activated BV-2 cells. A bioactivity-guided column chromatographic separation yielded two new lignans, firmianols A and B (1-2) together with seventeen known lignans (3-19). The structural elucidation of the new compounds was determined by spectroscopic methods, including 1D, 2D NMR and HR-FAB-MS. All isolated lignans were evaluated for their antineuroinflammatory effects on nitric oxide (NO) production in lipopolysaccharides (LPS)-activated murine microglia BV2 cells. Among the isolated, compounds 14 and 15 showed potent inhibitory activity against NO production (IC50 1.05 and 0.929 mu M, respectively) without cell toxicity in murine microglia BV-2 cells. Compounds 11-13 and 17 also exhibited strong inhibitory effects on NO production, with IC50 values ranging from 7.07 to 15.28 mu M. (C) 2016 Elsevier Ltd. All rights reserved.
机译:Firmiana simplex茎的80%MeOH提取物的CHCl3可溶性级分强烈抑制脂多糖激活的BV-2细胞中一氧化氮的产生。生物活性引导柱色谱分离产生了两个新的木脂素,硬脂酸A和B(1-2)以及十七种已知的木脂素(3-19)。通过光谱方法确定了新化合物的结构,包括1D,2D NMR和HR-FAB-MS。评估所有分离的木脂素对脂多糖(LPS)激活的鼠小神经胶质BV2细胞中一氧化氮(NO)产生的抗神经炎作用。在分离出的化合物中,化合物14和15在鼠小神经胶质BV-2细胞中显示出对NO产生的有效抑制活性(分别为IC50 1.05和0.929μM),而没有细胞毒性。化合物11-13和17对NO的产生也表现出强烈的抑制作用,IC50值范围为7.07至15.28μM。(C)2016 Elsevier Ltd.保留所有权利。

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