Many cancer cells critically rely on antioxidant systems for cell survival and are vulnerable to further oxidative impairment triggered by reactive oxygen species (ROS) generating agents. Therefore, the classical design and development of inhibitors that target the antioxidant defense enzymes such as thioredoxin reductase (TrxR) could be a promising anticancer strategy. Here, we showed the synthesis, characterization and anti-proliferative activity of gold(I) complexes with pentacyclic triterpene derivatives. Among them, gold(I) complex containing an oleanolic acid derivative (4b) induced ovarian cancer A2780 cells apoptosis by activating endoplasmic reticulum stress (ERS). It could inhibit TrxR enzyme activity to elevate ROS, mediate ERS and mitochondrial dysfunction, finally leading to the A2780 cells cycle arrest and apoptosis. Moreover, 4b inhibited A2780 xenograft tumor growth accompanied with increased ROS level and decreased TrxR activity in tumor tissues. This study might pave a new avenue for the design of TrxR inhibitors in anti-ovarian cancer drugs.

Gold(I) complexes containing pentacyclic triterpene derivatives as potential anti-ovarian cancer agents via inhibiting TrxR and activating ROS-mediated ERS

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.