4.7 Article

A cytotoxic nitrido-osmium(VI) complex induces caspase-mediated apoptosis in HepG2 cancer cells

Journal

DALTON TRANSACTIONS
Volume 49, Issue 47, Pages -

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d0dt02715d

Keywords

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Funding

  1. Guangdong Major Project of Basic and Applied Basic Research [2019B030302009]
  2. National Natural Science Foundation of China [21401125, 201627025, 201635031]
  3. Li Ka Shing Foundation Cross-Disciplinary Research Grant [2020LKSFG01F]
  4. Hong Kong Baptist University [RC-ICRS-18-19-01A]
  5. Shantou University Medical College

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The osmium(vi) nitrido complex [Os-VI(N)(sap)(py)Cl] is a potential anti-cancer drug with promising in vitro antiproliferative activities toward a panel of cancer cell lines, including cisplatin-resistant cells (IC50 values of 2.8-13.8 mu M). This drug targets DNA and changes its conformation via covalent binding and insertion. In vitro studies indicate that the drug induces HepG2 cells G2/M phase arrest, disrupts the mitochondrial membrane potential and causes caspase-mediated apoptosis. Further in vivo studies using HepG2-bearing nude mice reveal that this drug not only shows good antitumor efficacy of inhibiting tumor growth, but also does not show the side effect of weight loss.

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