P K Anuja, Kar Binoy, Roy Nilmadhab, Paira Priyankar
Department of Chemistry, School of Advanced Sciences, Vellore Institute of Technology Vellore-632014 Tamilnadu India
RSC Adv. 2022 Jun 29;12(29):18911-18922. doi: 10.1039/d2ra02677e. eCollection 2022 Jun 22.
Herein, we have introduced a series of half-sandwich Ru(ii)arene(N^N bpy/phen)-based RAPTA complexes for brain cancer therapy. Among all the synthesized complexes, [(η--cymene)Ru(κ-,-4,7dimethyl phenanthroline)(PTA)]·2PF (4c) and [(η--cymene)Ru(κ-,-4,7diphenyl phenanthroline)(PTA)]·2PF (4d) showed outstanding potency against the T98G, LN229 and U87MG cancer cells. The antiproliferative activity of these complexes was reinforced by neurosphere, DNA intercalation, agarose gel electrophoresis, cell cycle analysis and time-dependent ROS detection assays. The real-time reverse transcription (RT)-polymerase chain reaction (PCR) study showed that complex 4c inhibited the TNF-α-induced NF-κB phosphorylation in glioma cells. Moreover, the biodistribution of complex 4c in different organs and the morphological patterns of widely used zebrafish embryos due to toxic effects have been evaluated.
在此，我们介绍了一系列基于半夹心钌（II）芳烃（N^N联吡啶/菲罗啉）的RAPTA配合物用于脑癌治疗。在所有合成的配合物中，[(η-对异丙基苯)钌(κ-，-4,7-二甲基菲罗啉)(PTA)]·2PF（4c）和[(η-对异丙基苯)钌(κ-，-4,7-二苯基菲罗啉)(PTA)]·2PF（4d）对T98G、LN229和U87MG癌细胞表现出出色的活性。通过神经球、DNA嵌入、琼脂糖凝胶电泳、细胞周期分析和时间依赖性活性氧检测试验增强了这些配合物的抗增殖活性。实时逆转录（RT）-聚合酶链反应（PCR）研究表明，配合物4c抑制了胶质瘤细胞中TNF-α诱导的NF-κB磷酸化。此外，还评估了配合物4c在不同器官中的生物分布以及由于毒性作用导致的广泛使用的斑马鱼胚胎的形态模式。
