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新型镧系元素(铈、镧和钕)复合化合物的抗肿瘤活性

Antineoplastic activity of new lanthanide (cerium, lanthanum and neodymium) complex compounds.

作者信息

Kostova Irena, Kostova Raina, Momekov Georgi, Trendafilova Natasha, Karaivanova Margarita

机构信息

Department of Chemistry, Faculty of Pharmacy, Medical University, 2 Dunav St., Sofia 1000, Bulgaria.

出版信息

J Trace Elem Med Biol. 2005;18(3):219-26. doi: 10.1016/j.jtemb.2005.01.002.

DOI:10.1016/j.jtemb.2005.01.002
PMID:15966570
Abstract

Cerium (III), lanthanum (III) and neodymium (III) complexes with 3,3'-benzylidenebis[4-hydroxycoumarin] were synthesized in view of their application as cytotoxic agents. The complexes were characterized by different physicochemical methods: elemental analysis, mass spectrometry, 1H NMR, 13C NMR and IR spectroscopy. The spectra of the complexes were interpreted on the basis of comparison with the spectrum of the free ligand. The vibrational analysis showed that in the complexes the ligand coordinated to the metal ion through both deprotonated hydroxyl groups; however, participation of the carbonyl groups in the coordination to the metal ion was also suggested. The evaluation of the cytotoxic activity of the novel lanthanide complexes on HL-60 myeloid cells revealed that they are potent cytotoxic agents. The cerium complex was found to exhibit superior activity in comparison to the lanthanum and neodymium coordination compounds, the latter being the least active. Our data give us reason to conclude that the newly synthesized lanthanide complexes should be submitted to further more detailed pharmacological and toxicological evaluation.

摘要

鉴于铈(III)、镧(III)和钕(III)与3,3'-亚苄基双[4-羟基香豆素]的配合物可作为细胞毒性剂使用,因此合成了这些配合物。通过不同的物理化学方法对这些配合物进行了表征:元素分析、质谱分析、1H NMR、13C NMR和红外光谱分析。在与游离配体的光谱进行比较的基础上,对配合物的光谱进行了解释。振动分析表明,在配合物中,配体通过两个去质子化的羟基与金属离子配位;然而,也有人提出羰基参与了与金属离子的配位。对新型镧系元素配合物对HL-60髓细胞的细胞毒性活性评估表明,它们是有效的细胞毒性剂。发现铈配合物与镧和钕配位化合物相比具有更高的活性,而后者活性最低。我们的数据使我们有理由得出结论,新合成的镧系元素配合物应进行进一步更详细的药理和毒理学评估。

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J Mol Model. 2008 May;14(5):353-66. doi: 10.1007/s00894-008-0277-0. Epub 2008 Feb 20.