School of Chemistry and Biosciences, University of Bradford, Bradford, BD7 1DP, UK.
ChemMedChem. 2021 Feb 17;16(4):624-629. doi: 10.1002/cmdc.202000672. Epub 2020 Nov 24.
Electron-deficient half-sandwich complexes are a class of under-studied organometallics with demonstrated potential as metallodrug candidates. This study investigates the effect of two 16-electron organoruthenium complexes ([(p-cym)Ru(benzene-1,2-dithiolato)] (1) and [(p-cym)Ru(maleonitriledithiolate)] (2)) on the cell viability of non-immortalised human lymphocytes from healthy individuals. The genotoxic effects of 1 and 2 in lymphocytes are also investigated by using the Comet and cytokinesis-block micronucleus assays. Gene expression studies were carried out on a panel of genes involved in apoptosis and the DNA damage-repair response. Results show that the two 16-electron complexes do not have significant effect on the cell viability of human lymphocytes from healthy individuals. However, an increase in DNA damage is induced by both compounds, presumably through oxidative stress production.
缺电子半三明治配合物是一类研究较少的有机金属配合物,具有作为金属药物候选物的潜力。本研究调查了两种 16 电子有机钌配合物([(p-cym)Ru(苯-1,2-二硫醇)](1)和[(p-cym)Ru(马来二腈二硫醇)](2))对健康个体来源的未永生化人淋巴细胞细胞活力的影响。还通过彗星和胞质分裂阻断微核试验研究了 1 和 2 在淋巴细胞中的遗传毒性作用。进行了基因表达研究,涉及参与细胞凋亡和 DNA 损伤修复反应的一组基因。结果表明,两种 16 电子配合物对健康个体来源的人淋巴细胞的细胞活力没有显著影响。然而,这两种化合物都诱导了 DNA 损伤的增加,可能是通过产生氧化应激。