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Luminescent anticancer Ru(II)-arenebipyridine and phenanthroline complexes: Synthesis, characterization, DFT studies, biological interactions and cellular imaging application.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2020-05-16 , DOI: 10.1016/j.jinorgbio.2020.111099
Anuja P K 1 , Priyankar Paira 1
Affiliation  

A series of ruthenium(II)-arene complexes of several bipyridine and phenanthroline derivatives have been synthesized by employing a green and efficient protocol involving water as a solvent under sonication. The structures of all the complexes were elucidated by the spectroscopic analysis. The geometry of the chlorido and PTA (1,3,5-Triaza-7-phosphaadamantane) complexes were further confirmed by DFT and single crystal XRD. The stability study in various solvents, specifically in the intracellular one was conducted. Most of the compounds exhibited significant potency and selectivity against MCF7 and HeLa cell lines with respect to normal HEK-293 cells compared to cisplatin and RAPTA-C (Ruthenium(II)-arene PTA complex). Complex [(η6-hexamethylbenzene)RuCl(κ2-N,N-4,4′-di-n-nonyl-2,2′-bpy)]Cl (3e) presented best anticancer profiles against all the human cancer cells. Interestingly, few complexes turned up to be highly fluorescent depicted by the quantum yield values. Remarkably, [(η6-p-cymene)RuCl(κ2-N,N-bpy)]Cl (3i) was identified as most significant anticancer theranostic agent interms of potency, selectivity and fluorescence quantum yield. This complex also represented itself as significant cellular imaging agent in live U-87 MG cells which was monitored by confocal microscope. Absorption and emission spectral studies of bypyridine and phenanthroline complex series revealed that the complexes interacted with calf thymus DNA through groove binding as well as intercalative mode. In addition to this, strong binding efficacy of these scaffolds wih BSA (Bovin Serum Albumin) also enhanced their transportation property inside the cells.



中文翻译:

发光抗癌Ru(II)-亚芳基联吡啶和菲咯啉配合物:合成,表征,DFT研究,生物相互作用和细胞成像应用。

通过采用绿色高效方法,在超声处理下以水为溶剂,合成了几种联吡啶和菲咯啉衍生物的一系列钌(II)-芳烃配合物。通过光谱分析阐明了所有配合物的结构。DFT和单晶XRD进一步证实了氯离子和PTA(1,3,5-Triaza-7-phosphaadamantane)配合物的几何形状。在各种溶剂中,特别是在细胞内的溶剂中进行了稳定性研究。与顺铂和RAPTA-C(钌(II)-芳烃PTA配合物)相比,大多数化合物相对于正常的HEK-293细胞显示出对MCF7和HeLa细胞系的显着效力和选择性。络合物[(η6-六甲基苯)RuCl(κ2-N,N-4,4'-二正壬基-2,2'-bpy)] Cl(3e)展示了针对所有人类癌细胞的最佳抗癌特性。有趣的是,很少有复合物被量子产率值描述为高度荧光的。显着地,[(η6 - p- Cymene)RuCl(κ2-N,N-bpy)] Cl(3i在效能,选择性和荧光量子产率方面,被认为是最重要的抗癌治疗药物。该复合物还代表自己是活U-87 MG细胞中重要的细胞显像剂,可通过共聚焦显微镜进行监测。吡啶和菲咯啉配合物系列的吸收和发射光谱研究表明,该配合物通过凹槽结合和嵌入模式与小牛胸腺DNA相互作用。除此之外,这些支架与BSA(Bovin血清白蛋白)的强结合力也增强了它们在细胞内的转运特性。

更新日期:2020-05-16
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