Jacinto Flávia E, de Oliveira Letícia Pires, Batista Alzir A, Oliveira Katia M, Correa Rodrigo S
Department of Chemistry, Institute of Biological and Exact Sciences, Campus Morro do Cruzeiro, Federal University of Ouro Preto (UFOP), Ouro Preto, MG 35400-000, Brazil.
Department of Chemistry, Federal University of São Carlos (UFSCar), CP 676, São Carlos, SP 13561-901, Brazil.
R Soc Open Sci. 2024 Jul 31;11(7):240353. doi: 10.1098/rsos.240353. eCollection 2024 Jul.
Ruthenium(II) complexes (-) with the general formula [Ru(O-O)(PPh)(bipy)]PF bearing two triphenylphosphine (PPh), bipyridine (bipy) and a series of natural and synthetic β-diketones (O,O) ligands were synthesized and characterized using various analytical techniques. The interaction between the complexes and DNA (CT-DNA) was investigated and demonstrated a weak interaction. The cytotoxicity of the complexes was investigated against breast cancer cells (MDA-MB-231 and MCF-7), lung cancer cells (A549), cisplatin-resistant ovarian cancer cells (A2780), as well as non-tumour lung (MRC-5) and non-tumour breast (MCF-10A) cell lines. All complexes exhibited cytotoxic activity against all the cell lines studied, with half maximal inhibitory concentration (IC) values ranging from 0.39 to 13 µM. Notably, the three complexes demonstrated selectivity against the A2780 cell line, with IC ranging from 0.39 to 0.82 µM. Among them, Ru2 exhibited the highest cytotoxicity, with an IC value of 0.39 µM. Consequently, this new class of complexes shows good selectivity towards cisplatin-resistant ovarian cancer cells and it is promising for further investigation as anti-cancer agents.
合成了通式为[Ru(O - O)(PPh)(bipy)]PF 的钌（II）配合物（-），其带有两个三苯基膦（PPh）、联吡啶（bipy）以及一系列天然和合成的β - 二酮（O，O）配体，并使用各种分析技术对其进行了表征。研究了这些配合物与DNA（CT - DNA）之间的相互作用，结果表明它们之间存在弱相互作用。考察了这些配合物对乳腺癌细胞（MDA - MB - 231和MCF - 7）、肺癌细胞（A549）、顺铂耐药卵巢癌细胞（A2780）以及非肿瘤性肺细胞（MRC - 5）和非肿瘤性乳腺细胞（MCF - 10A）系的细胞毒性。所有配合物对所研究的所有细胞系均表现出细胞毒性活性，半数最大抑制浓度（IC）值范围为0.39至13μM。值得注意的是，这三种配合物对A2780细胞系表现出选择性，IC值范围为0.39至0.82μM。其中，Ru2表现出最高的细胞毒性，IC值为0.39μM。因此，这类新型配合物对顺铂耐药卵巢癌细胞显示出良好的选择性，有望作为抗癌药物进行进一步研究。
