目的探究氨基噻唑酮Cu(Ⅱ)核酸酶的合成、晶体结构及其活性,预期得到一种高效的体外化学核酸酶试剂。方法:利用单晶衍射、琼脂糖凝胶电泳分别确定氨基噻唑酮Cu(Ⅱ)核酸酶试剂的空间结构及其活性。结果:氨基噻唑酮Cu(Ⅱ)核酸酶试剂为单斜晶系,空间群为P2(1)/n,由单个[Cu(TZD)Br2](1)(TZD=(z)-3-methyl-2-((E)-(1-phenylethylidene)hydrazone)-thiazolidin-4-one)单元组成,相比原来配合物[Cu(4ML)C1],经改造后的1在外界诱导剂的存在下30 μmol/L即可将DNA由Form I完全转变为Form Ⅱ,核酸酶活性提高10倍以上,核酸酶机制以氧化切割为主。结论:该研究获得一种氨基噻唑酮配体和一个新颖的氨基噻唑酮Cu(II)配合物,并表征其晶体结构,1作为一种高效的核酸酶试剂,其能力比[Cu(4ML)C1]提高一个数量级,可作为一种潜在的抗肿瘤药物。
Objective To study the synthesis, crystal structure and nuclease activity of the amino-thiazolidinone Cu (Ⅱ) nuclease reagent,and to obtain an efficient chemical nuclease reagent in vitro. Methods: The crystal structure and nuclease actieity of Cu (Ⅱ) nucleasereagent were discussed by X-ray and agarose gel electrophoresis. Results: The Cu(Ⅱ) complex was monoelinic, space group P2(1)/n, and itconsisted of a [Cu (TZD)Br2] (1) (TZD = (Z)-3-methyl-2-((E)-(1-phenylethylidene)hydrazono) -thiazolidin-4-one) unit; the nucleaseactivity of 1(30 txmol/L) could make most of Form I transform into Form II with inducer, and it was increased over 10-fold compared with [Cu(4ML)C1]; its nuelease mechanism was oxidative cleavage. Conclusion: An amino-thiazolidinone ligand and a novel amino-thiazolidinoneCu(II) nuclease reagent could be acquired. Cu(TZD)Br2 capability is on a higher magnitude compared with [Cu(4ML)C1], which can be usedas a potential anti-tumor drug.