Antitumor activity for gold (III) complex by high content screening technique (HCS) and cell viability assay

Abstract

Multipara metric analysis of compound toxicity at the level of individual cells using flow cytometry and cellular imaging-based approaches such as High Content Screening (HCS) have played key roles in the detection of toxicity and classification of compounds based on observed patterns of reversible and irreversible cellular injury. Gold III complex (AuL2) of bidentate ligand derived from the cyclization reaction of Schiff base of 4-amino-5-phenyl-4h-1,2,4-triazole-3-thiol with thioglycolic acid was synthesized and characterized by using melting point, FTIR spectroscopy, 1HNMR, UV-Visible spectroscopy and elemental analysis. The presence of chloride counter ion in complex was supported by conductivity measurement and the presence of hydrated water was supported by thermal gravimetric studies. We examine the cytotoxic effects of gold complex and its ligand in one cultured cellular models (MCF7 cell line) by High Content Screening (HCS) and analysis and cell viability assay (MMT assay). The inhibitory effect of AuL2 on breast cancer cell growth was due to induction of apoptosis as evidenced by annexin V staining and cell shrinkage. The study found that AuL2-mediated lead to disruption of Mitochondrial Membrane Potential (MMP), cell membrane permeability, nuclear condensation, fragmentation and release of cytochrome c from the mitochondria into the cytosol and also suggesting AuL2 as a potential MCF7 inhibitor compared to doxorubicin as positive control. In this study, data showed that gold (III) complex AuL2 may have therapeutic value in breast cancer treatment worthy of further development.