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首页> 美国卫生研究院文献>Oncotarget >New bipyridine gold(III) dithiocarbamate-containing complexes exerted a potent anticancer activity against cisplatin-resistant cancer cells independent of p53 status
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New bipyridine gold(III) dithiocarbamate-containing complexes exerted a potent anticancer activity against cisplatin-resistant cancer cells independent of p53 status

机译：新的含联吡啶金（III）二硫代氨基甲酸盐的复合物对顺铂耐药的癌细胞具有有效的抗癌活性而与p53的状态无关

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We synthesized, characterized and tested in a panel of cancer cell lines, nine new bipyridine gold(III) dithiocarbamate-containing complexes. In vitro studies demonstrated that compounds 1, 2, 4, 5, 7 and 8 were the most cytotoxic in prostate, breast, ovarian cancer cell lines and in Hodgkin lymphoma cells with IC50 values lower than the reference drug cisplatin. The most active compound 1 was more active than cisplatin in ovarian (A2780cis and 2780CP-16) and breast cancer cisplatin-resistant cells. Compound 1 determined an alteration of the cellular redox homeostasis leading to increased ROS levels, a decrease in the mitochondrial membrane potential, cytochrome-c release from the mitochondria and activation of caspases 9 and 3. The ROS scavenger NAC suppressed ROS generation and rescued cells from damage. Compound 1 resulted more active in tumor cells than in normal human Mesenchymal stromal cells. Gold compounds were active independent of p53 status: exerted cytotoxic effects on a panel of non-small cell lung cancer cell lines with different p53 status and in the ovarian A2780 model where the p53 was knocked out. In conclusion, these promising results strongly indicate the need for further preclinical evaluation to test the clinical potential of these new gold(III) complexes.
机译：我们在一组癌细胞系中合成，表征和测试了九种新的含联吡啶金（III）二硫代氨基甲酸酯的配合物。体外研究表明，化合物1、2、4、5、7和8在前列腺癌，乳腺癌，卵巢癌细胞系和霍奇金淋巴瘤细胞中的细胞毒性最高，其IC50值低于参考药物顺铂。在卵巢癌（A2780cis和2780CP-16）和乳腺癌对顺铂耐药的细胞中，活性最高的化合物1比顺铂更具活性。化合物1决定了细胞氧化还原稳态的改变，从而导致ROS水平升高，线粒体膜电位降低，线粒体细胞色素c释放以及胱天蛋白酶9和3的激活。损伤。与正常人间充质基质细胞相比，化合物1在肿瘤细胞中的活性更高。金化合物的活性与p53状态无关：在具有不同p53状态的一组非小细胞肺癌细胞系中以及在敲除p53的卵巢A2780模型中发挥了细胞毒性作用。总之，这些有希望的结果强烈表明需要进一步的临床前评估，以测试这些新的gold（III）复合物的临床潜力。

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