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新型血卟啉 IX 与顺磁钯(III)配合物的合成、结构及体外细胞毒性研究。

Synthesis, structure and in vitro cytotoxic studies of novel paramagnetic palladium(III) complexes with hematoporphyrin IX.

机构信息

Department of Analytical Chemistry, Faculty of Chemistry and Pharmacy, University of Sofia, 1J. Bourchier Str., 1164 Sofia, Bulgaria.

出版信息

J Inorg Biochem. 2013 Jul;124:54-62. doi: 10.1016/j.jinorgbio.2013.03.012. Epub 2013 Apr 2.

Abstract

Two coordination compounds of Pd(III) with hematoporphyrin IX ((7,12-bis(1-hydroxyethyl)-3,8,13,17-tetramethyl-21H-23H-porphyn-2,18-dipropionic acid), Hp), dinuclear [Pd(III)2(Hp-3H)Cl3(H2O)5]·2PdCl2, 1 and mononuclear [Pd(III)(Hp-2H)Cl(H2O)]·H2O, 2 were obtained and structurally characterized in solid state and solution using spectroscopic, thermal and magnetic methods. In the dinuclear complex, 1 one of the Pd(III) ions is coordinated to the deprotanated COO(-) groups from the side chains of the porphyrin ligand and the second Pd(III) ion - to two adjacent pyrrole N-atoms on the top of the porphyrin ring and a Pd(III)-Hp-Pd(III) system was formed. The Pd(III) ion in the mononuclear complex, 2 is incorporated in the porphyrin core. The Pd(III) centers in both complexes have a distorted octahedral coordination filled with additional donor species such as Cl(-) and H2O. The studied compounds showed in vitro cell growth inhibitory effects at micromolar concentration against a panel of human tumor cell lines. A DNA fragmentation assay indicated that the growth inhibitory effects are at least partly mediated by induction of apoptosis.

摘要

两个钯(III)与血卟啉 IX((7,12-双(1-羟乙基)-3,8,13,17-四甲基-21H-23H-卟啉-2,18-二丙酸),Hp)的配位化合物,二核[Pd(III)2(Hp-3H)Cl3(H2O)5]·2PdCl2,1和单核[Pd(III)(Hp-2H)Cl(H2O)]·H2O,2在固态和溶液中使用光谱,热和磁方法进行了结构表征。在双核配合物1中,一个钯(III)离子与来自卟啉配体侧链的去质子化 COO(-)基团配位,第二个钯(III)离子与卟啉环顶部的两个相邻吡咯 N-原子配位,形成 Pd(III)-Hp-Pd(III)体系。单核配合物2中的钯(III)离子被纳入卟啉核心。两个配合物中的 Pd(III)中心具有扭曲的八面体配位,填充有额外的供体物质,如 Cl(-)和 H2O。研究的化合物在微摩尔浓度下对一系列人肿瘤细胞系显示出体外细胞生长抑制作用。DNA 片段化分析表明,生长抑制作用至少部分是通过诱导细胞凋亡介导的。

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