The effects of genistein concentrations on Hep-2 cellular function

Genistein is a phytoestrogen that has shown potential as a chemotherapeutic agent, which acts by inhibiting protein-tyrosine kinase and topoisomerase II enzymes. These particular enzymes are crucial for cellular proliferation. The goal of this study was to evaluate the effect of genistein concentration (0.5, 0.05 or 0.005 mg/mL) on Hep-2 cells functional capacity. Specifically, to evaluate cellular number, protein, damage and morphology at 24, 48, and 72 hours phases. Data obtained from this study revealed that cell numbers were significantly reduced in low and medium concentrations after 24hrs, and cell numbers appeared to rebound at 48 and 72hrs in an inverse fashion. This data suggests continuous administration of the drug at therapeutic levels would serve as a better chemotherapeutic agent. Cellular damage was not evidenced and suggesting that the drug did not target the cellular membrane site. Morphological changes such as anucleation were seen at 24 hrs in all doses suggesting that genistein targets the genome directly. Interestingly, cellular function was able to recover in the lower doses of genistein treatment indicating cellular metabolism of the drug. Also, this information suggests that genistein mode of action by targeting enzymatic activity, as opposed to causing alterations within the cellular membrane, leading to leakage of cellular contents and ultimately cellular death since the membrane did not show evidence of lipid peroxidation.