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Activation by Oxidation: Ferrocene-Functionalized Ru(II)-Arene Complexes with Anticancer, Antibacterial, and Antioxidant Properties
Inorganic Chemistry ( IF 4.3 ) Pub Date : 2018-11-29 00:00:00 , DOI: 10.1021/acs.inorgchem.8b02542 Changhua Mu 1 , Kathleen E. Prosser 1 , Shane Harrypersad 1 , Gregory A. MacNeil 1 , Rikesh Panchmatia 1 , John R. Thompson 1 , Soumalya Sinha 1 , Jeffrey J. Warren 1 , Charles J. Walsby 1
Inorganic Chemistry ( IF 4.3 ) Pub Date : 2018-11-29 00:00:00 , DOI: 10.1021/acs.inorgchem.8b02542 Changhua Mu 1 , Kathleen E. Prosser 1 , Shane Harrypersad 1 , Gregory A. MacNeil 1 , Rikesh Panchmatia 1 , John R. Thompson 1 , Soumalya Sinha 1 , Jeffrey J. Warren 1 , Charles J. Walsby 1
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Organometallic Ru(II)-cymene complexes linked to ferrocene (Fc) via nitrogen heterocycles have been synthesized and studied as cytotoxic agents. These compounds are analogues of Ru(II)-arene piano-stool anticancer complexes such as RAPTA-C. The Ru center was coordinated by pyridine, imidazole, and piperidine with 0-, 1-, or 2-carbon bridges to Fc to give six bimetallic, dinuclear compounds, and the properties of these complexes were compared with their non-Fc-functionalized parent compounds. Crystal structures for five of the compounds, their Ru-cymene parent compounds, and an unusual trinuclear compound were determined. Cyclic voltammetry was used to determine the formal MIII/II potentials of each metal center of the Ru-cymene-Fc complexes, with distinct one-electron waves observed in each case. The Fc-functionalized complexes were found to exhibit good cytotoxicity against HT29 human colon adenocarcinoma cells, whereas the parent compounds were inactive. Similarly, antibacterial activity from the Ru-cymene-Fc compounds was observed against Bacillus subtilis, but not from the unfunctionalized complexes. In both cases, the IC50 values correlated quantitatively with the Fc+/0 reduction potentials. This is consistent with more facile oxidation to give ferrocenium, and subsequent generation of toxic reactive oxygen species, leading to greater cytotoxicity. The antioxidant properties of the complexes were quantified by a 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. EC50 values indicate that linking of the Ru and Fc centers promotes antioxidant activity.
中文翻译：
通过氧化活化：具有抗癌，抗菌和抗氧化性能的二茂铁官能化Ru（II）-Arene配合物
合成并研究了通过氮杂环与二茂铁（Fc）连接的有机金属Ru（II）-月桂烯复合物，并作为细胞毒性剂进行了研究。这些化合物是Ru（II）-芳烃钢琴凳式抗癌复合物（如RAPTA-C）的类似物。Ru中心通过吡啶，咪唑和哌啶与Fc的0、1，或2碳桥键配位得到六种双金属双核化合物，并将这些配合物的性质与其未Fc官能化的母体进行了比较化合物。确定了其中五个化合物，其Ru-cymene母体化合物和一种不寻常的三核化合物的晶体结构。循环伏安法用于测定正式的M III / IIRu-cymene-Fc配合物的每个金属中心的电势，在每种情况下均观察到不同的单电子波。发现Fc-官能化的复合物对HT29人结肠腺癌细胞显示出良好的细胞毒性，而母体化合物是无活性的。同样，Ru-cymene-Fc化合物对枯草芽孢杆菌具有抗菌活性，而未官能化的复合物则没有。在这两种情况下，IC 50值都与Fc + / 0定量相关还原潜力。这与更容易的氧化以得到二茂铁鎓，以及随后产生有毒的活性氧物种，从而导致更大的细胞毒性相一致。通过2，2-二苯基-1-吡啶并肼基（DPPH）自由基清除测定法定量复合物的抗氧化性能。EC 50值表明Ru和Fc中心的连接会促进抗氧化活性。
更新日期：2018-11-29
中文翻译：
通过氧化活化：具有抗癌，抗菌和抗氧化性能的二茂铁官能化Ru（II）-Arene配合物
合成并研究了通过氮杂环与二茂铁（Fc）连接的有机金属Ru（II）-月桂烯复合物，并作为细胞毒性剂进行了研究。这些化合物是Ru（II）-芳烃钢琴凳式抗癌复合物（如RAPTA-C）的类似物。Ru中心通过吡啶，咪唑和哌啶与Fc的0、1，或2碳桥键配位得到六种双金属双核化合物，并将这些配合物的性质与其未Fc官能化的母体进行了比较化合物。确定了其中五个化合物，其Ru-cymene母体化合物和一种不寻常的三核化合物的晶体结构。循环伏安法用于测定正式的M III / IIRu-cymene-Fc配合物的每个金属中心的电势，在每种情况下均观察到不同的单电子波。发现Fc-官能化的复合物对HT29人结肠腺癌细胞显示出良好的细胞毒性，而母体化合物是无活性的。同样，Ru-cymene-Fc化合物对枯草芽孢杆菌具有抗菌活性，而未官能化的复合物则没有。在这两种情况下，IC 50值都与Fc + / 0定量相关还原潜力。这与更容易的氧化以得到二茂铁鎓，以及随后产生有毒的活性氧物种，从而导致更大的细胞毒性相一致。通过2，2-二苯基-1-吡啶并肼基（DPPH）自由基清除测定法定量复合物的抗氧化性能。EC 50值表明Ru和Fc中心的连接会促进抗氧化活性。
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