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首页> 外文期刊>Journal of Inorganic Biochemistry: An Interdisciplinary Journal >Synthesis, crystal structure and biological activity of two Mn complexes with 4-acyl pyrazolone derivatives
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Synthesis, crystal structure and biological activity of two Mn complexes with 4-acyl pyrazolone derivatives

机译：两种Mn与4-酰基吡唑啉酮衍生物的配合物的合成，晶体结构和生物学活性

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In order to study the biological activities of transitional metal complexes based on 4-acyl pyrazolone derivatives, two Mn complexes [Mn(HLa)(L-a)]center dot(CH3CN)(1.5)center dot H2O (1) and [Mn-2(L-b)(2)(mu-EtO)(2)(EtOH)(2)] (2) (H2La = N-(1-phenyl-3-methyl-4-benzoyl-5-pyrazolone)-2-thiophenecarboxylic acid hydrazide, H2Lb = N-(1-phenyl-3-methyl-4-propenylidene-5-pyrazolone)-2-thiophenecarboxylic acid hydrazide) have been synthesized and characterized. Single crystal X-ray diffraction analysis indicated that 1 is a mononuclear complex and 2 exhibits a dinuclear centrosymmetric structure. Binding of the complexes with Herring Sperm DNA (HS-DNA) showed that complexes 1 and 2 could intercalate to DNA with quenching constant of 53 x 10(4) M-1 and 4.9 x 10(4) M-1, respectively. The interactions of the complexes with bovine serum albumin (BSA) indicated that complexes 1 and 2 could quench the intrinsic fluorescence of BSA in a static quenching process. Further, the inhibitory effects of the complexes on the cell population growth of the human esophageal cancer Eca-109 cells and the cervical cancer HeLa cells were determined by MIT assay, which indicated that both 1 and 2 significantly inhibited the growth of Eca-109 and HeLa cells, the inhibitory activity of complex 1 is stronger than that of 2. We further observed that complex 1 inhibited the growth of HeLa cells through inducing the apoptosis and arresting cell cycle at S phase. Our results suggested that both complexes 1 and 2 have DNA- and protein-binding capacity and antitumor activity. (C) 2015 Elsevier Inc. All rights reserved.
机译：为了研究基于4-酰基吡唑啉酮衍生物的过渡金属配合物的生物活性，使用两种Mn配合物[Mn（HLa）（La）]中心点（CH3CN）（1.5）中心点H2O（1）和[Mn-2 （Lb）（2）（mu-EtO）（2）（EtOH）（2）]（2）（H2La = N-（1-苯基-3-甲基-4-苯甲酰基-5-吡唑啉酮）-2-噻吩羧酸合成并表征了H 2 Lb ＝ N-（1-苯基-3-甲基-4-丙烯基-亚丙基-5-吡唑酮）-2-噻吩羧酸酰肼。 X射线单晶衍射分析表明1是单核络合物，2是双核中心对称结构。复合物与鲱鱼精子DNA（HS-DNA）的结合表明复合物1和2可以插入到DNA中，其淬灭常数分别为53 x 10（4）M-1和4.9 x 10（4）M-1。配合物与牛血清白蛋白（BSA）的相互作用表明，配合物1和2可以在静态猝灭过程中猝灭BSA的固有荧光。此外，通过MIT测定确定了该复合物对人食道癌Eca-109细胞和子宫颈癌HeLa细胞的细胞群生长的抑制作用，表明1和2均显着抑制了Eca-109和Eca-109的生长。对于HeLa细胞，复合物1的抑制活性强于2。我们进一步观察到，复合物1通过诱导S期凋亡和阻滞细胞周期来抑制HeLa细胞的生长。我们的结果表明，复合物1和2均具有DNA和蛋白质的结合能力以及抗肿瘤活性。 （C）2015 Elsevier Inc.保留所有权利。

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