The Graduate School of Natural and Applied Sciences, Dokuz Eylül University, Izmir, Turkey.
Izmir Biomedicine and Genome Center, Izmir, Turkey.
J Biol Inorg Chem. 2018 May;23(3):425-435. doi: 10.1007/s00775-018-1549-5. Epub 2018 Mar 22.
The new ruthenium (III) complex has been synthesized and characterized by elemental analysis, FT-IR, UV-Vis, EI-Mass, EPR spectroscopy, and magnetic susceptibility measurement. Cytotoxic effects of organoruthenium (II/III) complexes 1a, 1b, and 2a, and their ligands (TSC and TSC) in cultured human ovarian (A2780, SKOV-3, and OVCAR-3) and colon (DLD, CCD18Co, and Caco-2) cells have been investigated comparing reactivity of the Ru (II/III) complexes and their free TSC ligands. The complexes exhibit higher cytotoxicity in three cancer cell lines than in normal cells. The binding with CT-DNA and BSA of the all complexes were weak compared with their ligand in spite of the cellular uptake of these complexes into the cytoplasm and then nucleus while their cytotoxic effects were vice versa. All the results showed that Complex 1b has more efficient cytotoxicity on the colon cancer cells than ovarian cancer cells. However, Complex 2a is a better drug candidate especially for antitumor therapy of metastasized ovarian cancer.
新型钌（III）配合物已通过元素分析、FT-IR、UV-Vis、EI-Mass、EPR 光谱和磁化率测量进行了合成和表征。研究了有机钌（II/III）配合物 1a、1b 和 2a 及其配体（TSC 和 TSC）在培养的人卵巢（A2780、SKOV-3 和 OVCAR-3）和结肠（DLD、CCD18Co 和 Caco-2）细胞中的细胞毒性作用，比较了 Ru（II/III）配合物及其游离 TSC 配体的反应性。与正常细胞相比，这些配合物在三种癌细胞系中的细胞毒性更高。所有配合物与 CT-DNA 和 BSA 的结合能力均弱于其配体，尽管这些配合物进入细胞质，然后进入细胞核，但它们的细胞毒性作用却相反。所有结果表明，配合物 1b 对结肠癌细胞的细胞毒性比卵巢癌细胞更强。然而，配合物 2a 是一种更好的候选药物，特别是对转移性卵巢癌的抗肿瘤治疗。
