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Synthesis and anti-glioblastoma effects of artemisinin-isothiocyanate derivatives

机译：青蒿素 - 异硫氰酸酯衍生物的合成与抗胶质母细胞瘤作用

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摘要

A series of novel artemisinin (ART) derivatives containing an isothiocyanate (ITC) group were synthesized. All the compounds showed more potent anti-tumor effects than those of parent dihydroartemisinin (DHA) towards glioblastoma multiforme U87 in vitro. Among them, 5b had the strongest cytotoxic activity which exerted its effects in a concentration-dependent but not time-dependent manner (IC50 7.41 M for 24 h, 7.35 M for 72 h). Pyknosis was observed in 5b-treated U87 cells. Multiple intrinsic apoptotic pathways were induced by 5b including the upregulation of caspase 9, the release of cytochrome c, an increase of the proapoptotic protein Bax, a decrease of the anti-apoptotic protein Bcl 2, and the activation of execution pathways by the upregulation of caspase 3. In addition to apoptosis, an autophagic mechanism was also involved in 5b-induced cytotoxicity to human GBM U87 cells by upregulating the expression of LC3-II and downregulating p62. Furthermore, 5b also significantly attenuated the migration of U87 cells. Therefore, our results suggest that 5b may be a promising molecule for the further development of a novel drug for the treatment of glioblastoma.
机译：合成了含有异硫氰酸异氰酸酯（ITC）基团的一系列新的野生素（ART）衍生物。所有化合物均显示出比母体二氢甲醛蛋白（DHA）朝向胶质母细胞瘤多形态素U87体外的含量高效的抗肿瘤作用。其中，5B具有最强的细胞毒性活性，其在浓度依赖性但不是时间依赖的方式中施加其作用（IC50 7.41M，24小时，72小时72小时。在5B处理的U87细胞中观察到氏肾冬。通过5b诱导多种内在凋亡途径，包括胱天蛋白酶9的上调，细胞色素c的释放，促凋亡蛋白Bax的增加，抗凋亡蛋白Bcl 2的减少，并通过上调激活执行途径的激活Caspase 3.除了细胞凋亡之外，通过上调LC3-II的表达和下调P62，还通过对人GBM U87细胞进行自噬机理。[中测量P62，还参与5B诱导的细胞毒性。此外，5B还显着抑制了U87细胞的迁移。因此，我们的结果表明，5B可以是用于进一步发展用于治疗胶质母细胞瘤的新药的有希望的分子。

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  • 来源
    《RSC Advances》 |2018年第71期|共10页
  • 作者

    Nyein Chan Myae; Zhong Xiaolin; Lu Junfeng; Luo Huijuan; Wang Jiamin; Rapposelli Simona; Li Mingtao; Ying Ou-yang; Pi Rongbiao; He Xixin;

  • 作者单位

    Guangzhou Univ Chinese Med Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Guangzhou Univ Chinese Med Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Guangzhou Univ Chinese Med Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Guangzhou Univ Chinese Med Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Univ Pisa Dept Pharm Via Bonanno 6 I-56126 Pisa Italy;

    Sun Yat Sen Univ Zhongshan Sch Med Guangdong Prov Key Lab Brain Funct &

    Dis Guangzhou Guangdong Peoples R China;

    Sun Yat Sen Univ Sun Yat Sen Mem Hosp Dept Pediat Guangzhou 510120 Guangdong Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Guangzhou Univ Chinese Med Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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