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《天津医科大学学报》[ISSN:1006-8147/CN:12-1259/R]

卷:

22卷

期数:

2016年06期

页码:

474-477

栏目:

基础医学

出版日期:

2016-11-20

文章信息/Info

Title:

Nuclease of amino-thiazolidinone Cu (II): synthesis, structure and activity

文章编号:

1006-8147（2016）06-0474-4

作者:

邵 佳¹; 徐靖源²

(1.天津市第一中心医院药学部,天津 300192; 2.天津医科大学药学院,天津市临床药物关键技术重点实验室,天津 300070)

Author(s):

SHAO Jia¹;  XU Jing-yuan²

(1. Department of Pharmacy，Tianjin First Central Hospital, Tianjin 300192, China; 2. School of Pharmacy, Tianjin Medical University, Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, Tianjin 300070, China)

关键词:

氨基噻唑酮; Cu(II)配合物; 晶体结构; 核酸酶

Keywords:

amino-thiazolidinone;  Cu(II) complex;  crystal structure;  nuclease

分类号:

R9

DOI:

-

文献标志码:

A

摘要:

目的：探究氨基噻唑酮Cu(II)核酸酶试剂的合成、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)hydrazono)-thiazolidin-4-one)单元组成，相比原来配合物[Cu(4ML)Cl]，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)Cl]提高一个数量级，可作为一种潜在的抗肿瘤药物。

Abstract:

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 study discussed the crystal structure and nuclease acticity of Cu(II) nuclease reagent by X-ray and agarose gel electrophoresis,. Results: The Cu(II) complex was monoclinic, space group P2(1)/n, and it consisted of a [Cu(TZD)Br₂] (1) (TZD = (Z)-3-methyl-2-((E)-(1-phenylethylidene)hydrazono) -thiazolidin-4-one) unit; the nuclease activity of 1 (30 μMol/L) could make most of Form I transform into Form II with inducer, and it was increased over 10-fold compared with [Cu(4ML)Cl]; its nuclease mechanism was oxidative cleavage. Conclusion: An amino-thiazolidinone ligand and a novel amino-thiazolidinone Cu(II) nuclease reagent could be acquired . Cu(TZD)Br₂ capability is on a higher magnitude compared with [Cu(4ML)Cl], which can be used as a potential anti-tumor drug.