A Gold(III) Complex with Potential Anticancer Properties

Abstract

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.