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Comparative study of the antitumoral activity of phosphine-thiosemicarbazone gold(I) complexes obtained by different methodologies.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2019-11-22 , DOI: 10.1016/j.jinorgbio.2019.110931
Luis M González-Barcia 1 , Sandra Fernández-Fariña 1 , Laura Rodríguez-Silva 2 , Manuel R Bermejo 1 , Ana M González-Noya 1 , Rosa Pedrido 1
Affiliation  

A series of phosphino-thiosemicarbazone gold(I) dinuclear complexes obtained by two different synthetic procedures have been prepared. All the compounds have been spectroscopically characterized including single crystal X ray diffraction analysis in some of cases. [Au2(HL1)Cl2] (1), [Au2(HL2)2]Cl2 (2) and [Au2(HL3)2]Cl2 (3) have been prepared by chemical synthesis using a gold(III) salt as precursor; while [Au2(L1)2] (4), [Au2(L2)2]∙2CH3CN (5) and [Au2(L3)2] (6) have been isolated from an electrochemical synthesis (HLn = 2-[2-(diphenylphosphanyl)-benzylidene]-N-R-thiosemicarbazone; HL1: R = methyl, HL2: R = methoxyphenyl, HL3: R = nitrophenyl). The in vitro cytotoxic activity of these gold(I) complexes was tested against some human tumor cell lines: HeLa 229 (cervical epithelial carcinoma), MCF-7 (ovarian adenocarcinoma), NCI-H460 (non-small-cell lung cancer) and MRC5 (normal human lung fibroblast), and the IC50 values compared with those of cisplatin. The neutral methyl-substituted complexes 1 and 4 and methoxyphenyl 5 displayed significant cytotoxic activities in all investigated cancer cell lines, being 1 and 4 the most effective. The ability of complexes 1 and 4 to induce cell death by apoptosis in Hela 229 was also investigated by fluorescence microscopy using the apoptotic DNA fragmentation as marker. These results indicated that the inhibition of cell proliferation is mainly due to an apoptotic process. In order to obtain more information about the mechanism of action of these metallocompounds, the interactions of complexes 1 and 4 with the thioredoxin reductase (TrxR) enzyme were analyzed. Both complexes exhibited a strong inhibition of the thioredoxin reductase activity.

中文翻译:

通过不同方法获得的膦-硫代半碳zone金(I)配合物的抗肿瘤活性的比较研究。

已经制备了通过两种不同的合成方法获得的一系列膦基-硫代半碳酮金(I)双核配合物。在某些情况下,所有化合物都经过了光谱表征,包括单晶X射线衍射分析。[Au2(HL1)Cl2](1),[Au2(HL2)2] Cl2(2)和[Au2(HL3)2] Cl2(3)是使用金(III)盐为前体通过化学合成制得的。而[Au2(L1)2](4),[Au2(L2)2]∙2CH3CN(5)和[Au2(L3)2](6)已从电化学合成中分离出来(HLn = 2- [2- (二苯基膦基)-亚苄基] -NR-硫半脲; HL1:R =甲基,HL2:R =甲氧基苯基,HL3:R =硝基苯基)。测试了这些gold(I)配合物对某些人类肿瘤细胞系的体外细胞毒性活性:HeLa 229(宫颈上皮癌),MCF-7(卵巢腺癌),NCI-H460(非小细胞肺癌)和MRC5(正常人肺成纤维细胞),并与顺铂比较IC50值。在所有研究的癌细胞系中,中性甲基取代的配合物1和4和甲氧基苯基5表现出显着的细胞毒性活性,其中1和4最有效。还通过使用凋亡DNA片段化作为标记的荧光显微镜研究了复合物1和4通过Hela 229中的凋亡诱导细胞死亡的能力。这些结果表明细胞增殖的抑制主要是由于凋亡过程。为了获得有关这些金属化合物作用机理的更多信息,分析了配合物1和4与硫氧还蛋白还原酶(TrxR)的相互作用。
更新日期:2019-11-22
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