A Gold(III) Complex with Potential Anticancer Properties

Breast cancer is the most frequently diagnosed cancer among women and is a leading cause of cancer-related mortality in women worldwide. It is important to develop novel anticancer drugs with greater potency and fewer side effects. We synthesized a new gold(III) complex, dibenzyldithiocarbamato 2,2′-bipyridine-4,4′-dicarboxaldehyde gold (DDBDG), that showed significant binding with peroxisome proliferator-activated receptor-gamma (PPARγ) in molecular docking analysis and demonstrated pro-apoptotic properties in cell based assay. The IC₅₀ values for DDBDG and sorafenib were found to be 0.875 μM and 4.445 μM, respectively. We evaluated the apoptotic effects of DDBDG and sorafenib on MCF-7 breast cancer cell line. The results showed that DDBDG induced 2.2 folds, 4.4 folds, 5.5 folds apoptosis for 1 μM, 3 μM, and 10 μM concentrations, respectively. The induction of apoptosis for sorafenib was found to be 1.2-folds (1 μM), 1.5-folds (3 μM) and 1.6-folds (10 μM). At low concentration (1 μM), DDBDG significantly increased the mitochondrial membrane potential depolarization as well as generation of reactive oxygen species in cancer cells. The in-silico approaches showed that DDBDG is neither irritant nor having mutagenic, tumorigenic or reproductive toxicity. In conclusion, the drug-like characteristics and potentially high apoptotic activity of DDBDG at low concentrations suggest its possible application in affordable chemotherapy of cancer.