稀土-全反式维甲酸-缬氨酸三元配合物的合成、表征及抗肿瘤活性检测

doi:10.11944/j.issn.1000-0518.2015.01.140152

摘要/Abstract

摘要：

在无水乙醇介质中,合成了4种新型稀土三元固体配合物。通过红外光谱、紫外光谱、元素分析和TG-DTA等技术手段测试,确定了配合物的化学组成为:REL₂L'·nH₂O (RE:Nd³⁺,Eu³⁺,La³⁺,Sc³⁺;L=全反式维甲酸;L'=L-缬氨酸)。利用MTT测试法,检测了配合物对体外培养的人肝癌细胞HepG2、人肺癌细胞A549和人宫颈癌细胞Hela生长的影响。结果表明,4种稀土配合物与稀土硝酸盐、配体全反式维甲酸和L-缬氨酸对3种癌细胞株的生长均有一定的抑制作用,但在一定的浓度范围内,三元固体配合物的抑制效果明显优于稀土硝酸盐和2种配体;稀土配合物对3种癌细胞株生长的抑制作用基本上随浓度的升高而增强,存在一定的时间依赖性和浓度依赖性。为了进一步阐明抗肿瘤作用的原因,利用光谱方法和黏度法的手段,对配合物与DNA之间的相互作用方式做了考察,推测配合物抗肿瘤活性的起效与这种嵌入DNA双螺旋结构的作用方式有关。

关键词: 稀土配合物, 合成与表征, 抗肿瘤活性, 小牛胸腺DNA

Abstract:

In the medium of anhydrous ethanol, the complexes of REL₂L'·nH₂O(RE:Nd³⁺, Eu³⁺, La³⁺, Sc³⁺; L:all-trans retinoic acid; L':L-valine acid) were synthesized at 60 ℃. The compositions of these complexes were tested by means of infrared spectra(IR), ultraviolet spectra(UV), elemental analysis and TG-DTA methods. Meanwhile, the antitumor activity against HepG2, A549 and Hela in vitro growth cells was investigated by MTT test method. The results show that these four synthesized rare earth complexes inhibit the growth of HepG2, A549 and Hela cells in different degrees. The inhibition rates of these complexes are significantly higher than that of rare earth nitrate and ligands. The interaction of REL₂L' complex with DNA was studied by fluorescence spectroscopy and viscosity measurement. The results show that the type of interaction is mainly intercalation, which results in the antitumor activity of these complexes. This investigation provides certain ideas and experimental basis for the design of efficient rare earth antitumor drugs with low toxicity.

Key words: rare earth complexes, synthesis and characterization, antitumor activity, ct-DNA

中图分类号:

O614.3

李文娟, 马俊怀, 宋玉民. 稀土-全反式维甲酸-缬氨酸三元配合物的合成、表征及抗肿瘤活性检测[J]. 应用化学, 2015, 32(1): 34-42.

LI Wenjuan,MA Junhuai,SONG Yumin . Synthesis, Characterization and Antitumor Activity of Rare Earth Metal Complexes with All-trans Retinoic Acid and L-Valine Acid[J]. Chinese Journal of Applied Chemistry, 2015, 32(1): 34-42.

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