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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Half-sandwich RuCl2(eta(6)-p-cymene) core complexes containing sulfur donor aroylthiourea ligands: DNA and protein binding, DNA cleavage and cytotoxic studies
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Half-sandwich RuCl2(eta(6)-p-cymene) core complexes containing sulfur donor aroylthiourea ligands: DNA and protein binding, DNA cleavage and cytotoxic studies

机译：含硫供体芳酰基硫脲配体的半三明治RuCl2（eta（6）-p-cymene）核心复合物：DNA和蛋白质结合，DNA裂解和细胞毒性研究

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摘要

A series of Ru(II)(eta(6)-p-cymene) complexes (1-4) bearing the general formula [RuCl2(eta(6)-p-cymene) L] (L = monodentate aroylthiourea ligand) has been synthesized and characterized by analytical and various spectroscopic techniques. The neutral monodentate coordination of aroylthiourea with Ru via an S atom was confirmed by single crystal X-ray diffraction study. The complexes were tested for their ability to interact with DNA and protein. The complexes bound with calf thymus DNA (CT DNA) with the intrinsic binding constant value in the order of 10(4) M-1. The intercalative mode of binding was confirmed by the ethidium bromide (EB) displacement study. The interaction of the complexes with CT DNA was further supported by viscosity measurements and circular dichroic (CD) spectra. The Ru(II) complexes cleaved the supercoiled DNA without the need of any external agent. The spectroscopic evidence showed good binding efficacy of the complexes with BSA (Bovine Serum Albumin). The alterations in the secondary structure of BSA by the Ru(II) complexes were confirmed by synchronous fluorescence spectra. Cytotoxicity examination by MTT assay was carried out in two cancer cell lines (MCF7 and A549) and one non-cancerous cell line (L929). Complex 4 showed significant activity [IC50 = 52.3 (MCF7) and 54.6 (A549) mu M] which was comparable with that of similar known complexes. The morphological changes assessed by Hoechst staining revealed that the cell death occurred by apoptosis.
机译：一系列带有通式[RuCl2（eta（6）-p-cymene）L]（L =单齿芳基硫脲配体）的Ru（II）（eta（6）-p-cymene）配合物（1-4）通过分析和各种光谱技术合成和表征。通过单晶X射线衍射研究证实了芳硫基脲与Ru经由S原子的中性单齿配位。测试复合物与DNA和蛋白质相互作用的能力。与小牛胸腺DNA（CT DNA）结合的复合物，其固有结合常数值为10（4）M-1。溴化乙锭（EB）置换研究证实了结合的结合模式。粘度测量和圆二向色（CD）光谱进一步支持了复合物与CT DNA的相互作用。 Ru（II）络合物无需任何外部试剂即可切割超螺旋DNA。光谱证据表明该复合物与BSA（牛血清白蛋白）具有良好的结合功效。同步荧光光谱证实了Ru（II）配合物对BSA二级结构的改变。在两种癌细胞系（MCF7和A549）和一种非癌细胞系（L929）中通过MTT分析进行细胞毒性检查。配合物4显示出显着的活性[IC 50 ＝ 52.3（MCF7）和54.6（A549）μM]，与相似的已知配合物相当。 Hoechst染色评估的形态学变化表明细胞死亡是由凋亡引起的。

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