PDF(Pubmed)
Abstract：
The crystal structures of two newly synthesized nitrilotriacetate oxidovanadium(IV) salts, namely [QH][VO(nta)(H2O)](H2O)2 (I) and [(acr)H][VO(nta)(H2O)](H2O)2 (II), were determined. Additionally, the cytotoxic effects of four N-heterocyclic nitrilotriacetate oxidovanadium(IV) salts-1,10-phenanthrolinium, [(phen)H][VO(nta)(H2O)](H2O)0.5 (III), 2,2\'-bipyridinium [(bpy)H][VO(nta)(H2O)](H2O) (IV), and two newly synthesized compounds (I) and (II)-were evaluated against prostate cancer (PC3) and breast cancer (MCF-7) cells. All the compounds exhibited strong cytotoxic effects on cancer cells and normal cells (HaCaT human keratinocytes). The structure-activity relationship analysis revealed that the number and arrangement of conjugated aromatic rings in the counterion had an impact on the antitumor effect. The compound (III), the 1,10-phenanthrolinium analogue, exhibited the greatest activity, whereas the acridinium salt (II), with a different arrangement of three conjugated aromatic rings, showed the lowest toxicity. The increased concentrations of the compounds resulted in alterations to the cell cycle distribution with different effects in MCF-7 and PC3 cells. In MCF-7 cells, compounds I and II were observed to block the G2/M phase, while compounds III and IV were found to arrest the cell cycle in the G0/G1 phase. In PC3 cells, all compounds increased the rates of cells in the G0/G1 phase.
摘要：
两种新合成的次氮基三乙酸酯氧化钒（IV）盐的晶体结构，即[QH][VO(nta)(H2O)](H2O)2(I)和[(acr)H][VO(nta)(H2O)](H2O)2(II)，决心。此外,四种N-杂环次氮基三乙酸氧化钒（IV）盐-1,10-菲咯啉的细胞毒性作用，[(phen)H][VO(nta)(H2O)](H2O)0.5(III)，2,2'-联吡啶[（bpy）H][VO（nta）（H2O）]（H2O）（IV），对两种新合成的化合物(I)和(II)进行了抗前列腺癌(PC3)和乳腺癌(MCF-7)细胞的评价。所有化合物对癌细胞和正常细胞(HaCaT人角质形成细胞)表现出强的细胞毒性作用。构效关系分析表明，反离子中共轭芳环的数量和排列对抗肿瘤作用有影响。化合物(III)，1,10-菲咯啉类似物，展示了最伟大的活动，而吖啶盐(II)，三个共轭芳香环的排列方式不同，毒性最低。化合物浓度的增加导致细胞周期分布的改变，在MCF-7和PC3细胞中具有不同的作用。在MCF-7细胞中,观察到化合物I和II阻断G2/M期，同时发现化合物III和IV将细胞周期阻滞在G0/G1期。在PC3单元格中，所有化合物都增加了G0/G1期细胞的比率。
