<p>The anticancer activity of ruthenium(II) complexes can be enhanced by incorporating the amphiphilic ligands that possess higher solubility, cellular intake, and targeted drug delivery in comparison to other complexes. Homoleptic ruthenium(II) complexes of amphiphilic poly (aryl ether) dendrimer based bipyridine ligands were prepared and their anticancer activity was evaluated against three cancer cell lines (A549 lung adenocarcinoma cell line, MDA MB 231 human breast epithelial adenocarcinoma cell lines, and HepG2 liver cancer cell). The selectivity indices of complexes against the cancer cell lines infers that RuG03 exhibits consistent and greater selectivity across all the three cell lines, while RuG13 demonstrates notable potency against HepG2 cells, suggesting its potential for liver cancer treatment. Fluorescence staining assays, AO − EB, DAPI, cell death analysis by PI staining, reactive oxygen species (ROS), mitochondrial membrane potential (MMP) assays and DNA ladder assay were performed for the complexes to understand the anticancer mechanism. The results indicates that these complexes, induces apoptosis in cancer cells through action of DNA and ROS-mediated mitochondrial dysfunction pathways. Molecular docking analysis with DNA and anti-apoptotic Bcl-2 protein supports the experimental observations.</p> Graphical Abstract <p></p>

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Exploring the anticancer potential of amphiphilic dendritic ligands of homoleptic ruthenium(II) complexes

  • Liju Raju,
  • Eswaran Rajkumar

摘要

The anticancer activity of ruthenium(II) complexes can be enhanced by incorporating the amphiphilic ligands that possess higher solubility, cellular intake, and targeted drug delivery in comparison to other complexes. Homoleptic ruthenium(II) complexes of amphiphilic poly (aryl ether) dendrimer based bipyridine ligands were prepared and their anticancer activity was evaluated against three cancer cell lines (A549 lung adenocarcinoma cell line, MDA MB 231 human breast epithelial adenocarcinoma cell lines, and HepG2 liver cancer cell). The selectivity indices of complexes against the cancer cell lines infers that RuG03 exhibits consistent and greater selectivity across all the three cell lines, while RuG13 demonstrates notable potency against HepG2 cells, suggesting its potential for liver cancer treatment. Fluorescence staining assays, AO − EB, DAPI, cell death analysis by PI staining, reactive oxygen species (ROS), mitochondrial membrane potential (MMP) assays and DNA ladder assay were performed for the complexes to understand the anticancer mechanism. The results indicates that these complexes, induces apoptosis in cancer cells through action of DNA and ROS-mediated mitochondrial dysfunction pathways. Molecular docking analysis with DNA and anti-apoptotic Bcl-2 protein supports the experimental observations.

Graphical Abstract