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Four related mixed-ligand nickel(II) complexes: effect of steric encumbrance on the structure, DNA/BSA binding, DNA cleavage and cytotoxicity

机译:四种相关的混合配体镍(II)配合物:空间沉积对结构的影响,DNA / BSA结合,DNA裂解和细胞毒性

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摘要

Four closely related mononuclear nickel(II) complexes [Ni(L)(diimine) Cl](ClO4) (1-4), where L is a tridentate polypyridyl ligand of 4-methyl-N, N-bis(pyridin-2-ylmethyl) aniline and diimine is 2,2'-bipyridine (bpy, 1), 1,10-phenanthroline (phen, 2), dipyrido[3,2-d: 20,30-f] quinoxaline (dpq, 3) or dipyrido[3,2-a: 20,30-c]-phenazine (dppz, 4), have been synthesized and characterized using various physico-chemical techniques. All Ni centers adopt a distorted octahedral geometry with N5Cl donor sets. From 1 to 4, the dihedral angles between the benzene ring of L and the plane of the diimine gradually decline (52.5-6.8 degrees), leading to increasing steric encumbrance. The interactions of the complexes with CT-DNA and BSA have been explored using absorption and emission spectral methods. These complexes display binding propensity to CT-DNA in the order: 4 (dppz) > 3 (dpq) > 2 (phen) > 1 (bpy), and the quenching mechanisms of BSA by all the complexes are static procedures. In the absence of any external agents, only 1 (bpy) and 4 (dppz) exhibit apparent DNA cleavage activity, while with the addition of GSH or on the irradiation with UV-A light of 365 nm, the DNA cleavage abilities of the complexes are obviously enhanced, which vary as 1 > 2 > 3 > 4 (GSH) and 4 > 3 > 2 > 1 (UV-A). In addition, the in vitro cytotoxicity of the complexes on tumor cells lines (MCF-7, HepG-2 and SGC-7901) have been examined by MTT and the morphological assessment obtained using Hoechst 33342 staining reveals that 4 induces apoptosis against HepG-2.
机译:四个密切相关的单核镍(II)配合物[Ni(L)(二亚胺)Cl](ClO 4)(1-4),其中L是4-甲基-N,N-双(Pyridin-2-)的三氰基吡啶配体Ylmethyl)苯胺和二亚胺是2,2'-硼吡啶(BPY,1),1,10-菲咯啉(Phen,2),双氧碱[3,2-D:20,30-F]喹喔啉(DPQ,3)或双吡啶[3,2-A:20,30-C] - 苯嗪(DPPZ,4)已经合成,并使用各种物理化学技术进行了特征。所有NI中心采用扭曲的八面体几何与N5CL捐赠者套装。从1到4,L的苯环之间的二面角和二亚胺的平面逐渐下降(52.5-6.8度),导致超空间沉积。使用吸收和发射光谱方法探索了复合物与CT-DNA和BSA的相互作用。这些复合物按顺序显示到CT-DNA的结合倾斜:4(DPPZ)> 3(DPQ)> 2(PHPE)> 1(BPY),并且所有复合物的BSA的猝灭机制是静态程序。在没有任何外部药剂的情况下,只有1(BPY)和4(DPPZ)表现出明显的DNA切割活性,而在365nm的紫外线的辐射中添加GSH或辐照,则复合物的DNA切割能力明显增强,其改变为1> 2> 3> 4(GSH)和4> 3> 2> 1(UV-A)。此外,通过MTT检查肿瘤细胞系(MCF-7,HEPG-2和SGC-7901)的复合物的体外细胞毒性,并且使用Hoechst 33342染色获得的形态学评估显示,4诱导Hepg-2的细胞凋亡。

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  • 来源
    《RSC Advances》 |2015年第39期|共12页
  • 作者单位

    Nankai Univ Coll Chem Collaborat Innovat Ctr Chem Sci &

    Engn Tianjin Tianjin 300071 Peoples R China;

    Tianjin Med Univ Coll Pharm Tianjin 300070 Peoples R China;

    Shanxi Agr Univ Coll Arts &

    Sci Taigu 030801 Shanxi Peoples R China;

    Nankai Univ Coll Chem Collaborat Innovat Ctr Chem Sci &

    Engn Tianjin Tianjin 300071 Peoples R China;

    Nankai Univ Coll Chem Collaborat Innovat Ctr Chem Sci &

    Engn Tianjin Tianjin 300071 Peoples R China;

    Nankai Univ Coll Chem Collaborat Innovat Ctr Chem Sci &

    Engn Tianjin Tianjin 300071 Peoples R China;

    Nankai Univ Coll Chem Collaborat Innovat Ctr Chem Sci &

    Engn Tianjin Tianjin 300071 Peoples R China;

    Tianjin Med Univ Coll Pharm Tianjin 300070 Peoples R China;

    Shanxi Agr Univ Coll Arts &

    Sci Taigu 030801 Shanxi Peoples R China;

    Nankai Univ Coll Chem Collaborat Innovat Ctr Chem Sci &

    Engn Tianjin Tianjin 300071 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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