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丙二胺桥联邻菲罗啉镧配合物的合成及抗癌活性

作者:时间:2014-09-12点击数:

全文下载:2012010033 

李风华

(青岛科技大学 化学与分子工程学院, 山东 青岛266042)

 摘要: 以1,10-菲罗啉-2-甲醛为原料合成了1,3-丙二胺和1,2-丙二胺桥联2-甲基邻菲罗啉配体及其镧(Ⅲ)配合物,研究了配合物对人的HL60白血病、PC-3MIE8前列腺癌、BGC-823胃癌、MDA-MB-435乳腺癌、Bel-7402肝癌、Hela宫颈癌等6个瘤株的体外抗肿瘤活性及其与DNA的作用方式。结果表明,该化合物对实验的6种瘤株均具有明显的生长抑制作用,其作用机理可能是配合物以部分插入方式, 同时伴随共价作用与静电作用,与DNA发生作用,进而影响基因调控与表达,从而抑制肿瘤细胞的生长,最终导致癌细胞的死亡。

 关键词: 2-甲基邻菲罗啉; 镧(Ⅲ)配合物; 抗癌活性; DNA

中图分类号: O 614.33+1文献标志码: A

 Synthesis and Antitumor Activity of Lanthanum(Ⅲ) Complexes Containing 2-Methyl-1,10-phenanthroline Units Bridged by Propylenediamine

 LI Feng-hua

 (CollegeofChemistryand Molecular Engineering,QingdaoUniversityof Science and Technology,Qingdao266042,China)

 Abstract: Two lanthanum(III) complexes containing 2-methyl-1,10-phenanthroline units bridged by 1,3-propylenediamine and 1,2-propylenediamine were synthesized and characterized. The complexes have been assayed for in vitro antitumor activity against HL-60 (human leukocytoma) cells, PC-3MIE8 (human prostate carcinoma) cells, BGC-823 (human stomach carcinoma) cells, MDA-MB-435 (human galactophore carcinoma) cells, Bel-7402 (human liver carcinoma) cells, Hela (human cervix carcinoma) cells. The results show that the complexes exhibit good growth inhibition against different cell lines in general. DNA-binding studies indicate that the complexes possibly interact with ctDNA by partial intercalativeness, covalent binding and electrostatic effection.

 Key words: 2-methyl-phenanthroline; La(Ⅲ) complex; antitumor activity; DNA

收稿日期:2011-04-25

作者简介: 李风华(1972—),女,副教授.

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