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首页> 外文期刊>RSC Advances >Phenanthroindolizidine alkaloids from Tylophora atrofolliculata with hypoxia-inducible factor-1 (HIF-1) inhibitory activity
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Phenanthroindolizidine alkaloids from Tylophora atrofolliculata with hypoxia-inducible factor-1 (HIF-1) inhibitory activity

机译：来自Tylophora Atrofollata的菲妥芬醇生物碱，具有缺氧诱导因子-1（HIF-1）抑制活性

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摘要

Eleven new alkaloids (1-11), together with eleven known phenanthroindolizidine alkaloids (12-22) were isolated from the whole plants of Tylophora atrofolliculata (Asclepiadaceae). Their structures were characterized by means of NMR spectroscopies including HSQC, HMBC, H-1-H-1 COSY and NOESY experiments, assisted by high-resolution MS and CD spectral analyses. HIF-1-mediated reporter gene assay in T47D cells was used to evaluate the inhibitory effects of isolated alkaloids on HIF-1 activation. Most alkaloids exhibited extremely potent inhibitory effects with IC50 values in the low nanomolar range. The potency of 14 and 17 are comparable to manassantin B, one of the most potent HIF-1 inhibitors identified so far. Structure-activity relationship (SAR) analyses showed the necessities for high activity, i.e. non-planarity at indolizidine moiety, substitution types and patterns on the phenanthrene and indolizidine moieties. This is the first report on HIF-1 inhibitory activity of phenanthroindolizidine alkaloids, providing a new insight into their underlying anti-cancer mechanism.
机译：11新的生物碱（1-11）与11份已知的菲甲酰胺生物碱（12-22）与Tylophora Atrofollat​​a（Asclepiadaceae）的整株植物分离出来。它们的结构通过NMR光谱表征，包括HSQC，HMBC，H-1-H-1舒适和NOESY实验，通过高分辨率MS和CD光谱分析辅助。 HIF-1介导的T47D细胞的报告基因测定用于评估分离生物碱对HIF-1活化的抑制作用。大多数生物碱在低纳米摩尔范围内表现出极其有效的抑制作用。 14和17的效力与Manandantin B相当，到目前为止鉴定的最有效的HIF-1抑制剂之一。结构 - 活性关系（SAR）分析显示了高活性的必要性，即靛蓝部分的非平面性，亚己丁烯和吲哚啉部分的替代品和图案。这是关于菲苯甲酸甲烷类生物碱的HIF-1抑制活性的第一份报告，对其潜在的抗癌机制提供了新的洞察力。

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  • 来源
    《RSC Advances》 |2016年第83期|共10页
  • 作者

    Chen Cheng-Yu; Zhu Guo-Yuan; Wang Jing-Rong; Jiang Zhi-Hong;

  • 作者单位

    Macau Univ Sci &

    Technol Macau Inst Appl Res Med &

    Hlth State Key Lab Qual Res Chinese Med Taipa Macau Peoples R China;

    Macau Univ Sci &

    Technol Macau Inst Appl Res Med &

    Hlth State Key Lab Qual Res Chinese Med Taipa Macau Peoples R China;

    Macau Univ Sci &

    Technol Macau Inst Appl Res Med &

    Hlth State Key Lab Qual Res Chinese Med Taipa Macau Peoples R China;

    Macau Univ Sci &

    Technol Macau Inst Appl Res Med &

    Hlth State Key Lab Qual Res Chinese Med Taipa Macau Peoples R China;

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