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Synthesis of cucurbitacin IIa derivatives with apoptosis-inducing capabilities in human cancer cells

机译：用癌细胞中凋亡诱导能力的含油曲调IIA衍生物的合成

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摘要

Twenty-one cucurbitacin IIa derivatives were synthesized and screened for cytotoxic activity. Their structures were established using H-1 NMR, C-13 NMR, and LC-MS spectroscopic data. The absolute configuration of the derivatives was determined by single crystal diffraction. In sulforhodamine B (SRB) assays, nearly all compounds displayed low cytotoxicity toward normal human cells (HEK293). However, some derivatives displayed high cytotoxicity, in the low mu M range, toward several human tumor cell lines (SKOV3, HT29, HEPG2, MCF-7, and LOVO). Low IC50 values were obtained, especially for acetyl-protected product 2, 2,4,6-trichlorophenylhydrazine derivative 4a, and 2-hydrazinopyridine derivative 4d. In particular, compounds 2 and 4d showed low IC50 values of 1.2 +/- 0.01 and 2.2 +/- 0.19 mu M against SKOV3 cells. These compounds were submitted to extensive biological testing, which showed that compounds 2 and 4a did not inhibit tumor cells by influencing the cell cycle. Furthermore, compound 4a triggered the apoptotic pathway in cancer cells, showing high apoptosis ratios. This study mainly changed the structure of cucurbitacin tetracyclic triterpenoids and provided a novel tetracyclic skeleton derived from natural products that provided further references for the future modification of cucurbitacin tetracyclic triterpenoids.
机译：合成并筛选二十一根葫芦酸IIA衍生物以进行细胞毒性活性。它们的结构是使用H-1 NMR，C-13 NMR和LC-MS光谱数据建立的。通过单晶衍射确定衍生物的绝对配置。在亚磺胺胺B（SRB）测定中，几乎所有化合物都显示出正常人体细胞（HEK293）的低细胞毒性。然而，一些衍生物在低mu m范围内显示出高细胞毒性，朝向几种人肿瘤细胞系（Skov3，HT29，Hepg2，MCF-7和Lovo）。得到低IC 50值，特别是对于乙酰基保护产物2,2,4,6-三氯苯基肼衍生物4a和2-肼吡啶衍生物4d。特别地，化合物2和4D针对SkoV3细胞显示出1.2 +/- 0.01和2.2 +/-0.19μm的低IC 50值。将这些化合物提交至广泛的生物检测，这表明化合物2和4a通过影响细胞周期而不抑制肿瘤细胞。此外，化合物4a引发癌细胞中的凋亡途径，显示出高凋亡比。该研究主要改变了葫芦素四环素骨瓣的结构，并提供了一种新的四环骨架，其衍生自天然产物，提供了进一步提及葫芦素四环素萜类化合物的未来改性。

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  • 来源
    《RSC Advances》 |2020年第7期|共10页
  • 作者

    Yu Kun; Yang Xinmei; Li Ying; Cui Xue; Liu Bo; Yao Qingqiang;

  • 作者单位

    Univ Jinan Shandong Acad Med Sci Sch Med &

    Life Sci Jinan 250200 Shandong Peoples R China;

    Shandong First Med Univ Affiliated Hosp 1 Dept Pharm Jinan 250014 Peoples R China;

    Shandong First Med Univ Shandong Acad Med Sci Inst Mat Med Jinan 250062 Shandong Peoples R China;

    Univ Jinan Shandong Acad Med Sci Sch Med &

    Life Sci Jinan 250200 Shandong Peoples R China;

    Shandong First Med Univ Shandong Acad Med Sci Inst Mat Med Jinan 250062 Shandong Peoples R China;

    Shandong First Med Univ Shandong Acad Med Sci Inst Mat Med Jinan 250062 Shandong Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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