Some ferrocenyl chalcones as useful candidates for cancer treatment
Some ferrocenyl chalcones as useful candidates for cancer treatment
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DOI：
10.1007/s11626-015-9919-6
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发表时间：
2015-10-01
影响因子：
2.1
通讯作者：
Gabriela, Mojzisova
中科院分区：
文献类型：
--
作者：
Janka, Vaskova;Zatko, Daniel;Gabriela, Mojzisova
虽然癌症管理方面的知识很丰富，但目前这一领域的死亡率并没有下降。因此，重要的是执行一项旨在预防这些严重疾病的长期战略。与二茂铁相关的有机金属化合物具有比苯基类似物更强的生物活性，因此有望成为设计新药的候选药物。在我们的工作中，我们重点研究了五个二茂铁基衍生物对选定的肿瘤细胞株的细胞毒性和抗增殖作用。我们发现，其中一些物质显著降低Jurkat细胞的存活率，并在较小程度上降低HeLa、MCF7、A549和MDA细胞的存活率。用这些药物长期处理HeLa细胞培养物可显著阻断肿瘤细胞集落的形成。我们发现，当最终浓度为10(-4)和10(-5)摩尔L(-1)时，化合物的作用机制之一可能是影响线粒体的氧化还原状态。在所测试的化合物中，吲哚二茂铁衍生物(C)是最有效的，特别是通过谷胱甘肽耗尽。根据实验结果，可以得出结论：含铁化合物具有潜在的抗肿瘤活性。
Although knowledge of cancer management is extensive, mortality is not currently declining in this area. It is therefore important to implement a long-term strategy that would aim to prevent these serious diseases. Ferrocene-related organometallic compounds are promising candidates for design of new drugs since they can exhibit much greater biological activity than their phenyl analogs. In our work, we focused on investigating the cytotoxic and antiproliferative effects of five ferrocenyl derivatives toward selected tumor cell lines. We found that some of these substances significantly reduced Jurkat cell survival and, to a lesser extent, that of the HeLa, MCF7, A549, and MDA cells. Long-term treatment of HeLa cell cultures with these agents resulted in a significant blockade of formation of tumor cell colonies. We found that one of the mechanisms of action of the compounds is likely to display an effect on the redox state of the mitochondria at a final concentration of 10(-4) and 10(-5) mol l(-1). Of the compounds tested, the indanonyl ferrocene derivative (C) was the most effective, especially via glutathione depletion. Based on the obtained results, it can be concluded that synthetic substances containing iron have potential antitumor activity.