Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 193, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112234
Keywords
Gold(III) Schiff base complexes; Thioredoxin reductase; Reactive oxygen species; Endoplasmic reticulum stress; Hepatocellular carcinoma
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Funding
- National Natural Science Foundation of China [81703337]
- Priority Academic Program Development of Jiangsu Higher Education Institutions (Integration of Chinese andWestern Medicine)
- Jiangsu Specially-Appointed Professors program
- Open Project of State Key Laboratory of Natural Medicines [SKLNMKF201808, SKLNMKF201712]
- State Key Laboratory of Coordination Chemistry, Nanjing University
- Six Talent Peaks Project in Jiangsu Province of China [SWYY-069]
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Hepatocellular carcinoma (HCC) is one of the most common cancers and a leading cause of death worldwide. Increased thioredoxin reductase (TrxR) levels were recently identified as possible prognostic markers for HCC. Here, four gold(III) complexes 1b-4b bearing Schiff base ligands were synthesized, characterized, and screened for antitumor activity against HCC. All complexes triggered significant antiproliferative effects against HCC cells, especially the most active complex 1b induced HepG2 cells apoptosis by activating the endoplasmic reticulum stress (ERS). 1b could clearly inhibit the TrxR activity to elevate reactive oxygen species (ROS), mediate ERS and lead to mitochondrial dysfunction. Notably, treatment of 1b improved the CCl4-induced liver damage in vivo by down-regulation of TrxR expression and inflammation level. (c) 2020 Elsevier Masson SAS. All rights reserved.
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