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Cytotoxic and anticancer properties of new ruthenium polypyridyl complexes with different lipophilicities
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2018-01-09 , DOI: 10.1016/j.jinorgbio.2018.01.003
Anjong Florence Tikum , Yu Jeong Jeon , Ju Hyun Lee , Min Hee Park , In Yeong Bae , Sang Heon Kim , Hye Jin Lee , Jinheung Kim

Three ruthenium complexes containing a bidentate piq ligand, [(piq)Ru(bpy)2]2+ (1), [(piq)Ru(phen)2]2+ (2), and [(piq)Ru(DIP)2]2+ (3) (piq = phenylisoquinolinate, bpy = 2,2′-bipyridine, phen = 1,10-phenanthroline, DIP = 4,7-diphenyl-1,10-phenanthroline), were prepared. The DNA binding properties of complexes 13 to double-stranded DNA were studied. The binding of 13 to calf-thymus DNA (ct-DNA) yielded lower emission intensities than those observed with the corresponding Ru complexes alone. To explore potential interactions of complexes 13 with lipid-rich organs in live cells, the emission properties of the Ru probes were studied with liposomes. The emission intensities of complexes 13 were enhanced to similar extents upon interaction with liposomes. The cytotoxic activities of the complexes against MDA-MB-231 and HUVECs were evaluated in vitro. The effects of complexes 13 on the survival of MDA-MB-231 cells were examined and compared with that of cis-platin. Complexes 2 and 3 were more cytotoxic to cancer cells than cis-platin. Complexes 13 showed cellular uptakes of 1.1, 10.6, and 76.6%, respectively, indicating that the greatest amount of complex 3 entered the cancer cells. Inhibition of cell migration by complexes 13 was also evaluated by the wound healing assay.



中文翻译:

具有不同亲脂性的新型钌多吡啶基配合物的细胞毒性和抗癌特性

三种钌络合物,包含二齿piq配体,[(piq)Ru(bpy)2 ] 2+1),[(piq)Ru(phen)2 ] 2+2)和[(piq)Ru(DIP)2 ] 2+3)(piq =异喹啉苯基酯,bpy = 2,2′-联吡啶,phen = 1,10-菲咯啉,DIP = 4,7-二苯基-1,10-菲咯啉)。DNA结合复合物的性能1 - 3至双链DNA进行了研究。13的绑定小牛胸腺DNA(ct-DNA)的发射强度比单独使用相应的Ru配合物观察到的发射强度低。为了探索复合物的潜在相互作用1 - 3用在活细胞中富含脂质的机关,茹探测器的发射特性进行了研究与脂质体。配合物的发光强度1 - 3分别增强,以在与脂质体的相互作用类似的程度。在体外评估了复合物对MDA-MB-231和HUVEC的细胞毒活性。配合物的影响1 - 3进行了检查,并与相比对MDA-MB-231细胞的存活率-platin。配合物23铂对癌细胞的细胞毒性更大。配合物1 - 3显示细胞摄取的1.1,10.6,和76.6%,分别表示的复合物的量最大3输入的癌细胞。通过复合物的细胞迁移的抑制1 - 3也由伤口愈合测定法来评估。

更新日期:2018-01-09
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