Department of Chemistry, Indian Institute of Technology Guwahati, Guwahati 781039, Assam, India.
Biomaterial and Tissue Engineering Laboratory, Department of Biosciences & Bioengineering, Indian Institute of Technology Guwahati, Guwahati 781039, Assam, India.
Inorg Chem. 2021 May 17;60(10):7422-7432. doi: 10.1021/acs.inorgchem.1c00698. Epub 2021 Apr 28.
The synthesis and characterization of chiral pincer-ruthenium complexes of the type (NNN)RuCl (PPh) (R = 3-methylbutyl and 3,3-dimethylbutyl) is reported here. The cytotoxicity studies of these complexes were studied and compared with the corresponding activity of achiral complexes. The cytotoxic effect of pincer-ruthenium complexes on human dermal fibroblasts and human tongue carcinoma cells assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay displayed an inhibition of normal and cancer cell growth in a dose-dependent manner. Intracellular reactive oxygen species (ROS) level measurement, lactate dehydrogenase assay, DNA fragmentation, and necrosis studies revealed that treatment with pincer-ruthenium complexes induced a redox imbalance in SAS cells by upregulating ROS generation and caused necrotic cell death by disrupting the cellular membrane integrity.
本文报道了手性钳式钌配合物（NNN）RuCl（PPh）（R = 3-甲基丁基和 3,3-二甲基丁基）的合成与表征。研究了这些配合物的细胞毒性，并与相应的非手性配合物的活性进行了比较。采用 3-（4,5-二甲基噻唑-2-基）-2,5-二苯基四氮唑溴化物（MTT）法评估钳式钌配合物对人真皮成纤维细胞和人舌癌细胞的细胞毒性作用，显示出对正常和癌细胞生长的剂量依赖性抑制。细胞内活性氧（ROS）水平测量、乳酸脱氢酶测定、DNA 片段化和坏死研究表明，钳式钌配合物通过上调 ROS 的产生而导致 SAS 细胞中氧化还原失衡，并通过破坏细胞膜完整性导致坏死性细胞死亡。
