Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 158, Issue -, Pages 853-862Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.09.034
Keywords
Copper complex; Thiosemicarbazone; Reactive oxygen species; DNA degradation; Apoptosis
Categories
Funding
- National Natural Science Foundation of China [81571812]
- Priority Academic Program Development of Jiangsu Higher Education Institutions [1107047002]
- Fundamental Research Funds for the Central Universities
- Postgraduate Research& Practice Innovation Program of Jiangsu Province [KYCX17_0135]
- Scientific Research Foundation of Graduated School of Southeast University [YBJJ1787]
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Copper(II) complexes efficiently catalyze hydrogen peroxide to generate reactive oxygen species (ROS), which is the major reason for its significant anti-tumor activity. We synthesized three Cu(II) piperidylthiosemicarbazone complexes and examined their structures by X-ray single crystal diffraction. These Cu(II) complexes have significant apoptosis-promoting activity at nanomolar concentrations. The antitumor activity of these Cu(II) complexes is increased by more than 40-fold relative to that of the ligand. The binding experiment results demonstrated that the Cu(II) complexes interact with DNA with moderate binding affinity by in situ intercalation. Gel electrophoresis analysis indicated that DNA is degraded when the copper complex catalyzes hydrogen peroxide to produce reactive oxygen species (ROS). Apoptosis mechanism results showed that excessive ROS leads to mitochondrial membrane potential dissipation and promote the release of apoptotic factors from mitochondria. (C) 2018 Elsevier Masson SAS. All rights reserved.
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