Encapsulation of the Dinuclear Trithiolato-Bridged Arene Ruthenium Complex Diruthenium-1 in an Apoferritin Nanocage: Structure and Cytotoxicity

ChemMedChem. 2019 Mar 5;14(5):594-602. doi: 10.1002/cmdc.201800805. Epub 2019 Feb 11.

Abstract

The effects of encapsulating the cytotoxic dinuclear trithiolato-bridged arene ruthenium complex [(η6 -p-MeC6 H4 iPr)2 Ru22 -S-p-C6 H4 tBu)3 ]Cl (DiRu-1) within the apoferritin (AFt) nanocage were investigated. The DiRu-1-AFt nanocarrier was characterized by UV/Vis spectroscopy, ICP-MS, CD and X-ray crystallography. In contrast to previously reported Au- and Pt-based drug-loaded AFt carriers, we found no evidence of direct interactions between DiRu-1 and AFt. DiRu-1-AFt is cytotoxic toward immortalized murine BALB/c-3T3 fibroblasts transformed with SV40 virus (SVT2) and human epidermoid carcinoma A431 malignant cells, and exhibits moderate selectivity for these cancer cells over normal BALB/c-3T3 cells. DiRu-1-AFt triggers the production of reactive oxygen species, depolarization of mitochondrial membrane potential, and induces cell death via p53-mediated apoptosis. Comparison between our data and previous results suggests that the presence of specific interactions between a metal-based drug and AFt within the protein cage is not essential for drug encapsulation.

Keywords: anticancer; diruthenium; drug delivery; ferritin; protein cages.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Apoferritins / chemistry*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Coordination Complexes / chemistry*
  • Coordination Complexes / pharmacology
  • Crystallography, X-Ray
  • Humans
  • Mice
  • Mitochondrial Membranes / metabolism
  • Molecular Conformation
  • Nanocapsules / chemistry*
  • Reactive Oxygen Species / metabolism
  • Sulfhydryl Compounds / chemistry*

Substances

  • Antineoplastic Agents
  • Coordination Complexes
  • Nanocapsules
  • Reactive Oxygen Species
  • Sulfhydryl Compounds
  • diruthenium-1
  • Apoferritins