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新型 Pd(II)-salen 配合物通过调节特定的调控基因,显示出对人肝癌的高体外抗增殖作用。

Novel Pd(II)-salen complexes showing high in vitro anti-proliferative effects against human hepatoma cancer by modulating specific regulatory genes.

机构信息

Department of Chemistry, King Saud University, P. O. Box 2455, Riyadh 11451, KSA.

出版信息

Dalton Trans. 2012 Sep 21;41(35):10854-64. doi: 10.1039/c2dt31143g. Epub 2012 Aug 3.

DOI:10.1039/c2dt31143g
PMID:22858862
Abstract

We have reported the synthesis of a novel salen ligand and its mononuclear Pd-salen complexes derived from 2-{[2-hydroxy-3-{[(E)-(2-hydroxyphenyl)methylidene]amino}propyl)imino]methyl}phenol. The newly synthesized and isolated Pd(II) complexes have been identified and fully characterized by various physico-chemical studies viz., elemental analyses, IR, UV-Vis, (1)H, (13)C NMR spectroscopy, electron spray ionization mass spectrometry (ESI-MS) and TGA/DTA studies. The molecular structure of the salen ligand has been ascertained by single-crystal XRD and it is coordinated to Pd(II) ion through two nitrogen and two oxygen atoms. The UV-Vis data clearly suggest a square-planar environment around both the Pd(II) ions. The DNA binding studies of the synthesized compounds has been investigated by electron spectroscopy and fluorescence measurements. The results suggest that Pd(II) complexes bind to DNA strongly as compared to the free ligand. The free salen ligand and its Pd(II) complexes have also been tested against human hepatoma cancer cell line (Huh7) and results manifested exceptional anti-proliferative effects of the Pd(II) complexes. The anti-proliferative activity of Pd(II) complexes has been modulated by specific regulatory genes.

摘要

我们已经报道了一种新型席夫碱配体及其单核钯-席夫碱配合物的合成,该配体来源于 2-{[2-羟基-3-{[(E)-(2-羟基苯基)亚甲基]氨基}丙基)亚氨基}甲基}苯酚。新合成并分离的 Pd(II)配合物已通过各种物理化学研究进行了鉴定和充分表征,例如元素分析、IR、UV-Vis、(1)H、(13)C NMR 光谱、电子喷雾电离质谱(ESI-MS)和热重分析/差热分析(TGA/DTA)研究。席夫碱配体的分子结构已通过单晶 XRD 确定,其通过两个氮原子和两个氧原子与 Pd(II)离子配位。UV-Vis 数据清楚地表明两个 Pd(II)离子周围都具有平面正方形环境。合成化合物的 DNA 结合研究已通过电子光谱和荧光测量进行了研究。结果表明,与游离配体相比,Pd(II)配合物与 DNA 的结合更强。游离的席夫碱配体及其 Pd(II)配合物也已经针对人肝癌癌细胞系(Huh7)进行了测试,结果表明 Pd(II)配合物具有出色的抗增殖作用。Pd(II)配合物的抗增殖活性已通过特定的调节基因进行了调节。

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