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为系统研究平面芳香结构的共轭体系配体的加入对稀土-姜黄素配合物抑制肿瘤作用的影响,合成了四种稀土元素(RE=Eu,La,Ce,Nd)与姜黄素(L)、吡啶(L’)、2,2-联吡啶(L″)、1,10-菲啰啉(L)的配合物。二元配合物的化学组成为:REL3·2H2O;三元配合物的化学组成分别为:REL3L2’,REL3L″及REL3L。并利用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐(MTT)比色法,系统研究了稀土离子(III)、姜黄素、稀土-姜黄素二元配合物及稀土与姜黄素的吡啶、2,2-联吡啶、1,10-菲啰啉三元配合物对人肝癌细胞HepG2的抑制作用。体外抗肿瘤活性结果表明:稀土离子、配体姜黄素、稀土三元、二元配合物对癌细胞生长都表现出一定的抑制作用,多个配合物对肿瘤HepG2有明显的抑制作用,部分配合物显示了较强的抗癌活性。REL3L配合物的抑制作用在相同测试条件下常常强于其他配合物;Nd的三种三元配合物的抑制作用在其他三种稀土元素同类配合物中始终最强,说明Nd元素的此类配合物是有潜在实用价值的抗肿瘤药物;在测试的浓度范围内常出现REL3L2’配合物的抑制作用强于REL3L″配合物、REL3·2H2O强于某些三元配合物的现象。为初步探究配合物抗肿瘤作用的原因,用荧光法研究了Nd的三元配合物与DNA的作用,结果表明NdL3L″及NdL3L对DNA分子存在嵌插作用,NdL3L2’无嵌插作用。
In order to systematically study the effect of conjugate ligand with planar aromatic structure on the inhibition of tumor activity by the rare earth-curcumin complex, four rare earth elements (RE = Eu, La, Ce, Nd) and curcumin , Pyridine (L ’), 2,2-bipyridine (L “) and 1,10-phenanthroline (L) .The chemical composition of the binary complex is: REL3 · 2H2O; ternary complex The chemical composition is: REL3L2 ’, REL3L ”and REL3L. The effects of rare earth ions (III), curcumin, rare earth - Curcumin binary complexes and rare earth and curcumin pyridine, 2,2-bipyridine, 1,10-phenanthroline ternary complexes on human hepatocellular carcinoma cells HepG2 inhibition. In vitro antitumor activity results show that: rare earth ions, curcumin ligand, rare earth ternary, binary complexes on the growth of cancer cells showed some inhibition, a number of complexes on tumor HepG2 significant inhibition, part of the cooperation The substance shows a strong anticancer activity. The inhibitory effect of REL3L complexes is always stronger than that of other complexes under the same test conditions. The inhibition of the three ternary complexes of Nd is always the strongest among the other three kinds of rare earth complexes, indicating that Nd Complexes are potential antitumor drugs with potential practical value. In the tested concentration range, the inhibition of REL3L2 ’complexes is stronger than that of REL3L complexes and REL3.2H2O is stronger than some ternary complexes. The purpose of this study was to investigate the anti-tumor effects of the complexes. Fluorescence was used to study the interaction between Nd and the DNA. The results showed that NdL3L “and NdL3L” had intercalative effect on DNA and NdL3L2 had no intercalative effect.