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Sci.Rep:湖北工业大学汤亚杰研究组发表发表鬼臼类抗肿瘤药物研究成果

摘要 : 2015年10月7日,Nature出版集团旗下子刊《Scientific Reports》在线刊登了湖北工业大学一项关于鬼臼类抗肿瘤药物的研究进展。

 2015年10月7日,Nature出版集团旗下子刊《Scientific Reports》在线刊登了湖北工业大学一项关于鬼臼类抗肿瘤药物的研究进展,该研究由汤亚杰课题组青年教师赵巍、研究生李建龙和周晨等共同完成,其中李建龙为论文第一作者,汤亚杰研究员为论文通讯作者。

该论文系统报道了碳硫键修饰和碳氮键修饰对鬼臼毒素抗肿瘤活性影响及其抗肿瘤机理机制。与临床上使用的鬼臼类抗肿瘤药物“依托泊苷”相比,4β-S-杂环-鬼臼类衍生物对人肺癌A549的抗肿瘤活性提高了76-286倍;对人胃癌BGC-823抗肿瘤活性提高了5-65倍;对人子宫癌HeLa抗肿瘤活性提高了50-348倍。而对人正常肝脏细胞HL-7702的细胞毒性降低了2-5倍,且具有较强的微管蛋白或拓扑异构酶II靶向能力,诱导细胞早期凋亡。这表明4β-S-杂环-鬼臼类衍生物有望开发为新型广谱抗肿瘤药。

原文链接:

Comparison of carbon-sulfur and carbon-amine bond in therapeutic drug: 4β-S-aromatic heterocyclic podophyllum derivatives display antitumor activity

原文摘要:

Herein is a first effort to systematically study the significance of carbon-sulfur (C-S) and carbon-amine (C-NH) bonds on the antitumor proliferation activity of podophyllum derivatives and their precise mechanism of apoptosis. Compared with the derivative modified by a C-NH bond, the derivative modified by a C-S bond exhibited superior antitumor activity, the inhibition activity of target proteins tubulin or Topo II, cell cycle arrest, and apoptosis induction. Antitumor mechanistic studies showed that the death receptor and the mitochondrial apoptotic pathways were simultaneously activated by the C-S bond modified aromatic heterocyclic podophyllum derivatives with a higher cellular uptake percentage of 60–90% and induction of a higher level of reactive oxygen species (ROS). only the mitochondrial apoptotic pathway was activated by the C-NH bond modified aromatic heterocyclic podophyllum derivatives, with a lower cellular uptake percentage of 40–50%. This study provided insight into effects of the C-S and C-NH bond modification on the improvement of the antitumor activity of Podophyllum derivatives.

来源: Scientific Reports 浏览次数:0

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