Key Laboratory of Advanced Energy Materials Chemistry (MOE), Nankai University, Tianjin 300071, PR China; TKL of Metal and Molecule Based Material Chemistry, Nankai University, Tianjin 300071, PR China; College of Chemistry, Chemical Engineering and Materials Science, Shandong Normal University, Jinan 250014, PR China.
J Inorg Biochem. 2013 Oct;127:39-45. doi: 10.1016/j.jinorgbio.2013.06.002. Epub 2013 Jun 13.
As a continuing investigation of our previous studies about the influence of the different rare earth metal ions on the bioactivity, a family of heavy rare earth metal complexes, [RE(acac)3(dpq)] (RE=Tb (1), Dy (2), Ho (3), Er (4), Tm (5), Yb (6), Lu (7)) and [RE(acac)3(dppz)]·CH3OH (RE=Tb (8), Dy (9), Ho (10), Er (11), Tm (12), Yb (13), Lu (14) viz. acetylacetonate (acac), dipyrido[3,2-d:20,30-f]quinoxaline (dpq), dipyrido[3,2-a:20,30-c] phenazine (dppz)), has been synthesized and their biological activities were also investigated. On the irradiation with UV-A light of 365nm or ambient light, all complexes exhibit efficient DNA cleavage activity via the mechanistic pathway involving the formation of singlet oxygen and hydroxyl radical as the reactive species. In addition, the in vitro cytotoxicity of these complexes on HeLa cells has been examined by MTT assay, which indicate that these compounds have the potential to act as effective anticancer drugs. The results of the above biological experiments also reveal that the choice of different rare earth metal ions has little influence on the DNA binding, DNA cleavage and cytotoxicity.
作为我们之前关于不同稀土金属离子对生物活性影响的研究的延续，我们合成了一系列重稀土金属配合物，[RE(acac)3(dpq)]（RE=Tb（1）、Dy（2）、Ho（3）、Er（4）、Tm（5）、Yb（6）、Lu（7））和[RE(acac)3(dppz)]·CH3OH（RE=Tb（8）、Dy（9）、Ho（10）、Er（11）、Tm（12）、Yb（13）、Lu（14），即乙酰丙酮（acac）、二吡啶并[3,2-d:2',3'-f]喹喔啉（dpq）、二吡啶并[3,2-a:2',3'-c]吩嗪（dppz）），并研究了它们的生物活性。在 365nm 的紫外光或环境光照射下，所有配合物都通过涉及形成单线态氧和羟基自由基作为活性物质的机制途径表现出有效的 DNA 切割活性。此外，通过 MTT 测定法研究了这些配合物对 HeLa 细胞的体外细胞毒性，结果表明这些化合物具有作为有效抗癌药物的潜力。上述生物学实验的结果还表明，选择不同的稀土金属离子对 DNA 结合、DNA 切割和细胞毒性影响不大。
