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首页> 外文期刊>Acta Pharmacologica Sinica >Cytotoxicity, apoptosis induction, and mitotic arrest by a novel podophyllotoxin glucoside, 4DPG, in tumor cells
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Cytotoxicity, apoptosis induction, and mitotic arrest by a novel podophyllotoxin glucoside, 4DPG, in tumor cells

机译：新型鬼臼毒素葡萄糖苷4DPG在肿瘤细胞中的细胞毒性，凋亡诱导和有丝分裂阻滞

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Aim: To define the in vitro cytotoxic activities of 4-demethyl-picropodophyllotoxin 7′-O-β-D-glucopyranoside (4DPG), a new podophyllotoxin glucoside. Methods: Antiproliferation activity was measured in several tumor cell lines by using the microculture tetrazolium MTT assays. Cell cycle distribution was analyzed using flow cytometry and mitosis index assays. Furthermore, transmission electron microscopy, TUNEL, DNA agarose electrophoresis, and activated caspase-3 were used to analyze the induction of apoptotic cell death. Moreover, intracellular changes in the cytoskeleton were detected using immunocytochemistry. Results: 4DPG effectively inhibited the proliferation of cancer cells (HeLa, CNE, SH-SY5Y, and K562 cell lines). For the K562 cell line, the antiproliferation effect of 4DPG was much more potent than that of etoposide (IC_(50) value: 7.79 x 10~(-9) mol/L for 4DPG vs 2.23 x 10~(-5) mol/L for etoposide). Further, 4DPG blocked the cell cycle in the mitotic phase. The induction of apoptosis and elevated levels of activated caspase-3 were confirmed in cells treated with 4DPG. The microtubule skeleton of HeLa cells was disrupted immediately after treatment with 4DPG. Conclusion: The cytotoxi-city of 4DPG is due to its inhibition of the microtubule assembly of cancer cells at a low concentration, thus inducing apoptosis. These properties qualify 4DPG to be a potential antitumor drug.
机译：目的：确定新的鬼臼毒素葡糖苷4-去甲基-鬼臼毒素7'-O-β-D-吡喃葡萄糖苷（4DPG）的体外细胞毒活性。方法：采用微培养四唑MTT法测定了几种肿瘤细胞系的抗增殖活性。使用流式细胞仪和有丝分裂指数测定法分析细胞周期分布。此外，透射电镜，TUNEL，DNA琼脂糖电泳和激活的caspase-3用于分析凋亡细胞的诱导。此外，使用免疫细胞化学检测了细胞骨架中的细胞内变化。结果：4DPG有效抑制癌细胞（HeLa，CNE，SH-SY5Y和K562细胞系）的增殖。对于K562细胞系，4DPG的抗增殖作用比依托泊苷强得多（IC_（50）值：4DPG的抗衰老作用为7.79 x 10〜（-9）mol / L，2.24 x10〜（-5）mol / L L为依托泊苷）。此外，4DPG阻断了有丝分裂期的细胞周期。在用4DPG处理的细胞中证实了细胞凋亡的诱导和活化的caspase-3水平的升高。用4DPG处理后，HeLa细胞的微管骨架立即被破坏。结论：4DPG的细胞毒性是由于它以低浓度抑制癌细胞的微管装配，从而诱导了细胞凋亡。这些特性使4DPG成为潜在的抗肿瘤药物。

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