摘要
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。
This thesis aims to learn the effect of plane size of molecular on the growth of cancer cells of HepG2. The binary and ternary complexes of rare earth （III） nitrate were synthesized with the first lig- and curcumin and the second ligand pyridine, 2, 2- bipyridyl, 1, 10-phenanthroline in alcohol solution （pH =6.5 -7.0, RE =Eu, La, Ce, Nd, L = curcu- min, L＇ - pyridine, L″ = 2, 2-bipyridyl, L″ = 1,10- phenanthroline）. The composition of the complexes included REL3.2H20 and REL3L2＇, RELy＇ and REL3L″. By a method of methyl thiazolyl tetrazolium （MTT）, 16 kinds of complexes, RE（III） and curcumin on the inhibition of proliferation of HepG2 cells were identified. The result of anti -tumor activity in vitro indicated that the ternary and binary complexes, RE （III） and curcumin have a certain degree of inhibi- tion on the growth of HepG2 cells. All REL3L″com- plexes show a strong anti-tumor activity under the test conditions, and the NdL3L″ and NdL3L′′′ anti-tumor activity of NdL3L2＇, is stronger than that of other cornplexes. Especially NdL3L′′′ complex has more than 50% inhibition rate on the growth of HepG2 cells in rage of 1 × 10 ^-2 - 1 ×10^ -3 mol.L^-1, which means Nd complexes can be a potential anti-tumor drug. A sur- prise phenomenon was discovered that unde concentrations, the complexes of REL3L＇2 has inhibition rate than that of REL3L＂ complexes, hibition rate of REL^3＋2H2O is higher than r some higher the in- that of some ternary complexes. The anti-tumor activity of the complexes on HepG2 cells does not increase with the aromatic plane increases in molecular. The results of interaction of DNA with Nd-complexes showed that these complexes have different interaction type with DNA
出处
《中国稀土学报》
CAS
CSCD
北大核心
2014年第1期50-60,共11页
Journal of the Chinese Society of Rare Earths
基金
国家自然科学基金(21062017)
甘肃省教育厅(1101-05)
甘肃省高分子材料重点实验室资助项目
