Henan Key Laboratory of Polyoxometalates, Institute of Molecular and Crystal Engineering, College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004, China.
Henan Key Laboratory of Polyoxometalates, Institute of Molecular and Crystal Engineering, College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004, China.
Bioorg Med Chem Lett. 2020 Jan 1;30(1):126781. doi: 10.1016/j.bmcl.2019.126781. Epub 2019 Oct 31.
In this article, a new compound H[{Cu(HL)(HO)}(PMoO)]·5HO (1) (HL = 2-acetylpyrazine thiosemicarbazone) has been synthesized and structurally characterized by single-crystal X-ray diffraction of and other detection techniques. Interestingly, the structure of 1 is different from many reported copper-based complexes, in which the [PMoO], two Cu ions and two HL were directly connected by covalent bands. Biological studies demonstrated that 1 indicated moderate antibacterial activity against Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus), and a better cytotoxicity against human hepatic cancer line (SMMC-7721) than Mitoxantrone (Mito), the current clinical anticancer drug. Besides, the antibacterial mechanisms of 1 have been studied by the membrane integrity disruption, the destructive reactive oxygen species generation (ROS), the glutathione (GSH) depletion and the depressed enzymatic activity of respiratory chain dehydrogenases (RCD). These results revealed that the combination of HL, Cu, [PMoO] shows a higher antibacterial and cytotoxic activity.
在本文中，合成了一种新的化合物 H[{Cu(HL)(HO)}(PMoO)]·5HO（1）（HL=2-乙酰基吡嗪硫代缩氨基脲），并通过单晶 X 射线衍射和其他检测技术对其结构进行了表征。有趣的是，1 的结构与许多报道的基于铜的配合物不同，其中[PMoO]、两个 Cu 离子和两个 HL 直接通过共价键连接。生物研究表明，1 对大肠杆菌（E. coli）和金黄色葡萄球菌（S. aureus）表现出中等的抗菌活性，对人肝癌细胞系（SMMC-7721）的细胞毒性优于米托蒽醌（Mito），后者是目前的临床抗癌药物。此外，通过破坏膜完整性、生成破坏性活性氧物种（ROS）、消耗谷胱甘肽（GSH）和抑制呼吸链脱氢酶（RCD）的酶活性，研究了 1 的抗菌机制。这些结果表明，HL、Cu、[PMoO]的结合具有更高的抗菌和细胞毒性活性。
