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New antiproliferative germacranolides from Carpesium divaricatum

机译:来自Carpesium Divaricatum的新型抗增殖衍生物

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摘要

Six new highly oxygenated (2-7) and one known (1) germacranolides were isolated from the whole plant of Carpesium divaricatum. The planar structures and relative configurations of the new compounds were determined by detailed spectroscopic analysis. The absolute configurations of 1 and 3 were established by circular dichroism (CD) and X-ray crystallographic analyses, and the stereochemistry of the new compounds 2 and 4-6 were determined by similar CD data to 1 and 3, respectively. All isolates were evaluated for their antiproliferative activities against three human tumor cell lines, and compounds 3 and 6 show antiproliferative activities against HeLa and Hep G2 cells with IC50 values of 4.13-8.37 M. Intensive mechanism study showed that 3 caused cell-cycle arrest at the S/G2 phase and induced apoptosis in Hep G2 cells through a mitochondria-related pathway.
机译:六种新的高度含氧(2-7)和一种已知的(1)个锗丙醇与肉瘤的整个植物中分离出来。 通过详细的光谱分析确定新化合物的平面结构和相对配置。 通过圆形二色性(CD)和X射线晶体分析建立了1和3的绝对配置,并分别通过类似的CD数据测定了新化合物2和4-6的立体化学。 评估所有分离物针对三种人肿瘤细胞系的抗增殖活动,化合物3和6显示抗增殖活动对抗HELA和HEP G2细胞,IC50值为4.13-8.37米。密集型机制研究表明,3引起了细胞周期逮捕 通过线粒体相关途径,S / G2相和HEPG2细胞诱导细胞凋亡。

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  • 来源
    《RSC Advances》 |2019年第20期|共10页
  • 作者单位

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Mat Med Beijing 100150 Peoples R China;

    Chinese Acad Med Sci Peking Union Med Coll Inst Med Plant Dev Beijing 100193 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

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