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首页> 外文期刊>Biochimie >2-Methyl-pyran-4-one-3-0-(3-D-glucopyranoside isolated from leaves of Punica granatum inhibits the TNFa-induced cell adhesion molecules expression by blocking nuclear transcription factor-KB (NF-kB)
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2-Methyl-pyran-4-one-3-0-(3-D-glucopyranoside isolated from leaves of Punica granatum inhibits the TNFa-induced cell adhesion molecules expression by blocking nuclear transcription factor-KB (NF-kB)

机译:从石榴中提取的2-甲基-吡喃-4-酮-3-0-(3-D-吡喃葡萄糖苷)通过阻断核转录因子-KB(NF-kB)抑制TNFa诱导的细胞粘附分子表达。

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摘要

Here, we report bioactivity-guided isolation, purification and characterization of a novel compound, 2-methyl-pyran-4-one-3-O-β-D-glucopyranoside (MPG) from the leaves of Punica granatum. The structure of MPG was established on the basis of its detailed spectral analyses. We demonstrated that MPG not only inhibited the expression of cell adhesion molecules but also significantly blocked its functional consequence, that is, the adhesion of neutrophils on human endothelial cells monolayer. To elucidate the molecular mechanism of action of MPG, we showed that MPG decreased the transcript levels of ICAM-1, VCAM-1 and E-selectin genes. Using electrophoretic mobility shift assay (EMSA) and western blot analyses, we demonstrated that MPG significantly blocked both the TNFa-induced translocation and activation of nuclear transcription factor-KB (NF-kB). Thus, MPG could be useful as a novel lead molecule for developing future anti-inflammatory agents.
机译:在这里,我们报道了从石榴叶中提取的新型化合物2-甲基-吡喃-4-酮-3-酮-O-β-D-吡喃葡萄糖苷(MPG)的生物活性指导的分离,纯化和表征。 MPG的结构是基于其详细的光谱分析建立的。我们证明,MPG不仅抑制细胞粘附分子的表达,而且还显着阻断其功能性结果,即嗜中性粒细胞粘附在人内皮细胞单层上。为了阐明MPG作用的分子机制,我们表明MPG降低了ICAM-1,VCAM-1和E-选择素基因的转录水平。使用电泳迁移率变动分析(EMSA)和Western印迹分析,我们证明MPG显着阻断TNFa诱导的移位和核转录因子KB(NF-kB)的激活。因此,MPG可用作开发未来抗炎药的新型先导分子。

著录项

  • 来源
    《Biochimie》 |2011年第5期|p.921-930|共10页
  • 作者单位

    Institute of Genomks &Integrative Biology (Unit of CS.I.R.), Mall Road, Delhi 110 007, India;

    Department of Medicinal Chemistry, Indian Institute of Chemical Biology (Unit of C.S.I.R), Jadavpur, Kolkata 700 032, India;

    Department of Medicinal Chemistry, Indian Institute of Chemical Biology (Unit of C.S.I.R), Jadavpur, Kolkata 700 032, India;

    Institute of Genomks &Integrative Biology (Unit of CS.I.R.), Mall Road, Delhi 110 007, India;

  • 收录信息 美国《科学引文索引》(SCI);美国《化学文摘》(CA);
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    punica granatum; 2-methyl-pyran-4-one-3-o-β-d-glucopyranoside; tnfα; icam-1; vcam-1; e-selectin; nf-kb;

    机译:刺槐;2-甲基-吡喃-4-酮-3-一-β-d-吡喃葡萄糖苷;tnfα;icam-1;vcam-1;e-选择素;nf-kb;

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