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通过将抗癌中药莲叶桐碱与金属离子结合开发潜在新型无机抗肿瘤药物及DNA结合研究

Potential new inorganic antitumour agents from combining the anticancer traditional Chinese medicine (TCM) liriodenine with metal ions, and DNA binding studies.

作者信息

Chen Zhen-Feng, Liu Yan-Cheng, Liu Li-Min, Wang Heng-Shan, Qin San-Hai, Wang Bo-Long, Bian He-Dong, Yang Bin, Fun Hoong-Kun, Liu Hua-Gang, Liang Hong, Orvig Chris

机构信息

The Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education), School of Chemistry & Chemical Engineering of Guangxi Normal University, Guilin 541004, P. R. China.

出版信息

Dalton Trans. 2009 Jan 14(2):262-72. doi: 10.1039/b813363h. Epub 2008 Nov 19.

Abstract

Liriodenine (), an active component of the anticancer traditional Chinese medicine (TCM), was isolated from Zanthoxylum nitidum. Its reactions with Pt(II) and Ru(II) afforded three metal complexes: cis-[PtCl2(L)] (), cis-[PtCl2(L)(DMSO)] (), and cis-[RuCl2(L)(DMSO)2].1.5H2O (), the crystal structures of , and were determined by single-crystal X-ray diffraction methods. These complexes were fully characterized by elemental analysis, IR spectrophotometry, 1H and 13C NMR spectroscopies, and ES mass spectrometry. The in vitro cytotoxicity of and complexes against 11 human tumour cell lines was assayed. The metal-based compounds exhibit enhanced cytotoxicity vs. free , suggesting that these compounds display synergy in the combination of metal ions and liriodenine. The binding properties of and its complexes to ct-DNA were investigated through UV-vis, fluorescence, CD spectra, viscosity and agarose gels electrophoretic measurements.

摘要

白屈菜红碱()是抗癌中药的一种活性成分,从两面针中分离得到。它与铂(II)和钌(II)反应得到三种金属配合物:顺式-[PtCl2(L)]()、顺式-[PtCl2(L)(DMSO)]()和顺式-[RuCl2(L)(DMSO)2]·1.5H2O(),通过单晶X射线衍射方法测定了、和的晶体结构。这些配合物通过元素分析、红外分光光度法、1H和13C核磁共振光谱以及电喷雾质谱进行了全面表征。测定了和配合物对11种人类肿瘤细胞系的体外细胞毒性。与游离相比,金属基化合物表现出增强的细胞毒性,表明这些化合物在金属离子和白屈菜红碱的组合中显示出协同作用。通过紫外可见光谱、荧光光谱、圆二色光谱、粘度和琼脂糖凝胶电泳测量研究了及其配合物与ct-DNA的结合特性。

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