Synthesis, characterization and bioactivities of a new covalent copper(II) compound derived from {P2Mo5O23}6− and thiosemicarbazones. Issue 1 (1st January 2020)

• Record Type: Journal Article
• Authors: Zhao, Haiyan; Li, Jie; Fang, Yan; Chang, Bowen; Meng, Qingxi; Li, Mingxue; Wang, Chunzhang; Zhu, Xianfeng
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 1(2020)
• Publication Date: 2020-01-01
• Subjects: Polyoxometalate -- Thiosemicarbazone -- Structures -- Bioactivity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2019.126781
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: A new compound H2 [{Cu(HL)(H2 O)}2 (P2 Mo5 O23 )]·5H2 O (1 ) (HL = 2-acetylpyrazine thiosemicarbazone) has been synthesized and structurally characterized. The antibacterial mechanisms of 1 have been studied. The combination of HL, Cu 2+ and [P2 Mo5 O23 ] 6– result in a higher antibacterial and cytotoxic activity. Highlights: Compound 1 has been synthesized and structurally characterized. In 1, the [P2 Mo5 O23 ] 6−, two Cu 2+ and two HL were directly connected by covalent bands. The antibacterial activity and action mechanisms of 1 were studied. The cytotoxicity of 1 against human hepatic cancer line (SMMC-7721) is better than that of clinical anticancer drug Mito. Abstract: In this article, a new compound H2 [{Cu(HL)(H2 O)}2 (P2 Mo5 O23 )]·5H2 O (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 [P2 Mo5 O23 ] 6−, two Cu 2+ 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 2+, [P2 Mo5 O23 ] 6− shows a higher antibacterial and cytotoxic activity.