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目的研究2种喹啉有机锗倍半氧化物与小牛胸腺DNA(CT-DNA)和2种人工合成的寡聚核苷酸(22聚AT碱基对d(AT)_(22)和22聚GC碱基对d(GC)_(22)的相互作用,以便揭示化合物的抗癌作用机制。方法综合应用紫外-可见分光光度法(UV-Vis)、热变性(melting temperature studies)、荧光光谱变化(fluorescence titration experiments)、黏度测定(viscosity measurements)等方法,研究了2种喹啉有机锗倍半氧化物与3种DNA的相互作用。结果有机锗化合物与CT-DNA结合后,它们的UV-Vis光谱均发生了不同程度的减色效应和红移现象,相对荧光强度显著增强;化合物能使DNA的热变温度(Tm)提高、黏度增强;通过荧光滴定数据计算得到相应的结合常数(10~4-10~5L/mol)。结论喹啉有机锗倍半氧化物能够与DNA以插入方式结合,喹啉基团与有机锗的协同作用增强了抗癌活性,DNA可能是其作用靶点。这些结果对进一步合成高效低毒的有机锗抗癌药物、揭示它们的抗癌作用机制具有重要的参考价值。
Objective To investigate the effect of two kinds of quinoline organogermanium sesquioxide on the surface of human breast cancer cells induced by calf thymus DNA (CT-DNA) and two synthetic oligonucleotides (22 poly AT base pairs d (AT) _ (22) and 22 (GC) _ (22) in order to reveal the anticancer mechanism of the compounds.Methods The UV-Vis, melting temperature studies, fluorescence Fluorescence titration experiments and viscosity measurements were used to investigate the interaction between two kinds of quinoline organogermanium sesquioxide and three kinds of DNA.Results After the organogermanium compounds were combined with CT-DNA, their UV-Vis spectra all have different hypochromic effect and redshift phenomenon, and the relative fluorescence intensity is significantly enhanced. The compounds can increase the thermal transition temperature (Tm) and viscosity of the DNA; the corresponding binding constants are calculated by fluorescence titration data (10 ~ 4-10 ~ 5L / mol) .CONCLUSION Quinoline organogermanium sesquioxide can be inserted into DNA, and the synergistic effect of quinoline group and organic germanium enhances the anticancer activity. DNA may be its role These results are for further synthesis of highly efficient and low toxicity organic germanium Cancer drugs, anti-cancer reveal their mechanism of action has important reference value.