Muralisankar Mathiyan, Dheepika Ramachandran, Haribabu Jebiti, Balachandran Chandrasekar, Aoki Shin, Bhuvanesh Nattamai S P, Nagarajan Samuthira
Department of Chemistry, Central University of Tamil Nadu, Thiruvarur 610005, India.
Department of Chemistry, National Institute of Technology, Tiruchirappalli 620015, India.
ACS Omega. 2019 Jul 5;4(7):11712-11723. doi: 10.1021/acsomega.9b01022. eCollection 2019 Jul 31.
Organoruthenium complexes are potent alternatives for platinum-based complexes because of their superior anticancer activity. In this investigation, a series of new Ru(II)-arene complexes with triarylamine-thiosemicarbazone hybrid ligands with higher anticancer activity than cisplatin are reported. The molecular structure of the ligands and complexes was confirmed spectroscopically and supported by single-crystal X-ray crystallography. These complexes adopted a three-leg piano stool geometry. All the Ru(II)-arene complexes were systematically investigated for their in vitro cytotoxicity against human cervical (HeLa S3), lung (A549) cancer, and human normal lung (IMR-90) cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Interestingly, a pyrrolidine-attached Ru(II)-benzene complex exhibited superior activity against cancer cells with low IC values, and colony formation study showed complete inhibition at 5 and 10 μM concentration. Furthermore, morphological changes assessed by acridine orange and propidium iodide staining revealed that the cell death occurred by apoptosis. In addition, the interaction between synthesized Ru(II)-arene complexes and DNA/protein was explored by absorption and emission spectroscopy methods. These synthesized new organoruthenium complexes can be used for developing new metal-based anticancer drugs.
由于具有优异的抗癌活性,有机钌配合物是铂基配合物的有力替代品。在本研究中,报道了一系列具有三芳基胺-硫代半卡巴腙杂化配体的新型Ru(II)-芳烃配合物,其抗癌活性高于顺铂。通过光谱对配体和配合物的分子结构进行了确认,并得到了单晶X射线晶体学的支持。这些配合物采用了三腿钢琴凳几何结构。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐法,对所有Ru(II)-芳烃配合物针对人宫颈(HeLa S3)、肺(A549)癌细胞以及人正常肺(IMR-90)细胞系的体外细胞毒性进行了系统研究。有趣的是,一种连接吡咯烷的Ru(II)-苯配合物对癌细胞表现出优异的活性,IC值较低,集落形成研究表明在5和10 μM浓度下完全抑制。此外,通过吖啶橙和碘化丙啶染色评估的形态学变化表明细胞死亡是由凋亡引起的。另外,通过吸收和发射光谱法探索了合成的Ru(II)-芳烃配合物与DNA/蛋白质之间的相互作用。这些合成的新型有机钌配合物可用于开发新型金属基抗癌药物。
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