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Updated: Dec 15, 2025

Detection of Mitochondria Membrane Potential to Study CLIC4 Knockdown-induced HN4 Cell Apoptosis In Vitro
Published on: July 17, 2018
Single-crystal structure and intracellular localization of Zn(II)-thiosemicarbazone complex targeting mitochondrial
Jinxu Qi1, Wei Zhao1, Yunyun Zheng1
1Medcine College of Pingdingshan University, Pingdingshan, Henan 467000, China.
Abstract:
Tracking of drugs in cancer cells is important for basic biology research and therapeutic applications. Therefore, we designed and synthesised a Zn(II)-thiosemicarbazone complex with photoluminescent property for organelle-specific imaging and anti-cancer proliferation. The Zn(AP44eT)(NO3)2 coordination ratio of metal to ligand was 1:1, which was remarkably superior to 2-((3-aminopyridin-2-yl) methylene)-N, N-diethylhydrazinecarbothioamide (AP44eT·HCl) in many aspects, such as fluorescence and anti-tumour activity. Confocal fluorescence imaging showed that the Zn(AP44eT)(NO3)2 was aggregated in mitochondria. Moreover, Zn(AP44eT)(NO3)2 was more effective than the metal-free AP44eT·HCl in shortening the G2 phase in the MCF-7 cell cycle and promoting apoptosis of cancer cells. Supposedly, the effects of these complexes might be located mainly in the mitochondria and activated caspase-3 and 9 proteins.
Insights
A novel zinc(II)-thiosemicarbazone complex, Zn(AP44eT)(NO3)2, effectively targets cancer cell mitochondria for imaging and inhibits proliferation. This photoluminescent compound shows superior anti-cancer activity compared to its metal-free counterpart.
Area of Science:
- Chemical Biology
- Cancer Research
- Mitochondrial Targeting
Background:
- Tracking drug distribution in cancer cells is crucial for developing effective cancer therapies.
- Thiosemicarbazone complexes are investigated for their potential anti-cancer properties.
Purpose of the Study:
- To design and synthesize a photoluminescent zinc(II)-thiosemicarbazone complex for organelle-specific imaging.
- To evaluate the anti-cancer proliferation activity of the synthesized complex.
Main Methods:
- Synthesis of a Zn(II)-thiosemicarbazone complex (Zn(AP44eT)(NO3)2) with a 1:1 metal-to-ligand ratio.
- Confocal fluorescence imaging to determine cellular localization.
- Cell cycle analysis (G2 phase) and apoptosis assays in MCF-7 cancer cells.
Main Results:
- The Zn(AP44eT)(NO3)2 complex exhibited superior fluorescence and anti-tumor activity compared to the metal-free ligand (AP44eT·HCl).
- Confocal imaging revealed mitochondrial aggregation of the complex.
- Zn(AP44eT)(NO3)2 effectively shortened the G2 phase and promoted apoptosis in MCF-7 cells.
Conclusions:
- The synthesized Zn(AP44eT)(NO3)2 complex is a promising photoluminescent agent for mitochondrial imaging in cancer cells.
- The complex demonstrates significant anti-cancer proliferation effects, likely mediated through mitochondrial pathways and caspase activation.
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