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Start Over Author "Xia Xichao" Publisher elsevier bv
15 results on '"Xia Xichao"'

5. Single-crystal structure and intracellular localization of Zn(II)-thiosemicarbazone complex targeting mitochondrial apoptosis pathways

Author

Zhao Wei, Chen Qiu, Yunyun Zheng, Wang Ruiya, Huashan Gao, Fan Weiwei, Xia Xichao, Wang Fu'an, and Qi Jinxu

Subjects
Models, Molecular, Thiosemicarbazones, Fluorescence-lifetime imaging microscopy, Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, Apoptosis, Mitochondrion, Crystallography, X-Ray, 01 natural sciences, Biochemistry, Structure-Activity Relationship, chemistry.chemical_compound, Coordination Complexes, Drug Discovery, Humans, Methylene, Molecular Biology, Cell Proliferation, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Ligand, Cell Cycle, Organic Chemistry, Cell cycle, Fluorescence, Mitochondria, 0104 chemical sciences, Zinc, 010404 medicinal & biomolecular chemistry, chemistry, Cancer cell, MCF-7 Cells, Biophysics, Molecular Medicine, Drug Screening Assays, Antitumor
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.

Published
2020

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