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7 alpha,8 alpha-Epoxynagilactones and their glucosides from the twigs of Podocarpus nagi: Isolation, structures, and cytotoxic activities

机译:来自Podocarpus Nagi的树枝的7α,8个α-环氧化素及其葡糖苷:分离,结构和细胞毒性活动

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摘要

A phytochemical investigation of twigs of Podocarpus nagi resulted in the identification of eight new type B nagilactones (1-8), all bearing a 7 alpha,8 alpha-epoxy-9(11)-enolide substructure, along with two known analogs (9-10). Their structures were determined on the basis of spectroscopic analysis, including HRESIMS, IR and NMR experiments, and X-ray crystallographic analysis. In vitro cytotoxic assay exhibited that compounds 1, 2, 9 and 10 could induce antiproliferation against three different types of human cancer cells while compounds 3 and 5 were inactive. Notably, the IC50 value of compound 1 is 0.208 mu M for A431 human epidermoid carcinoma cells, reaching the same level as the positive control combretastatin A-4 (0.104 mu M). Furthermore, compound 1 performed a strong inhibition of cancer cells by triggering apoptosis and arresting the cell cycle at G(1) phase. These results unfold potential anticancer therapeutic applications of type B nagilactones.
机译:Podocarpus Nagi枝的植物化学研究导致鉴定八种新型B型鼻内(1-8),均轴承为7α,8个α-环氧-9(11) - 丙醇酯亚结构以及两种已知的类似物(9 -10)。 它们的结构是基于光谱分析确定的,包括Hresims,IR和NMR实验和X射线晶体分析。 体外细胞毒性测定表明,化合物1,2,9和10可以诱导抗溶解,而抗溶解在三种不同类型的人癌细胞,而化合物3和5是无活性的。 值得注意的是,对于A431人表皮癌细胞,化合物1的IC 50值为0.208μm,达到与阳性对照组合A-4(0.104μm)相同的水平。 此外,化合物1通过触发细胞凋亡并在G(1)相时捕获细胞周期进行强烈抑制癌细胞。 这些结果展开了B型纳吉酮型抗癌治疗应用。

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  • 来源
    《Fitoterapia》 |2018年第2018期|共10页
  • 作者单位

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

    Chinese Acad Sci Shanghai Inst Mat Med State Key Lab Drug Res Shanghai 201203 Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 林区药材;
  • 关键词

    Podocarpus nagi; Type B nagilactone; Cytotoxic activity; Apoptosis;

    机译:podocarpus nagi;b型纳格替纳蛋白;细胞毒性活性;细胞凋亡;

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