The present study highlights the apoptotic activity of magnetic Fe3O4 nanoparticulates functionalized by glutamic acid and 2-pyridinecarboxaldehyde thiosemicarbazone (PTSC) toward human lung epithelial carcinoma A549 cell line. To this aim, the Fe3O4 nanoparticulates were prepared using co-precipitation method. Then, the glutamic acid and Fe3O4 nanoparticulates were conjugated to each other. The product was further functionalized with bio-reactive PTSC moiety. In addition, the synthesized Fe3O4@Glu/PTSC nanoparticulates were characterized by physico-chemical techniques including scanning electron microscope (SEM), energy dispersive X-ray (EDX), X-ray diffraction (XRD), Fourier-transform infrared (FT-IR) spectroscopy and zeta potential analysis. The effects of in vitro cell viability in Fe3O4@Glu/PTSC nanoparticulate indicated the anti-proliferative properties in a dose-dependent manner (IC50 = 135.6 µM/mL). The high selectivity for tumor cells and far below of activity in HEK293 non-tumorigenic cells is considered as an important feature for this complex (SI, 3.48). Based on the results, PTSC failed to reveal any activity against A549 cells alone. However, Fe3O4 nanoparticulates had some effects in inhibiting the growth of lung cancer cell. Furthermore, Bax and Bcl-2 gene expressions were quantified by real-time PCR method. The expression of Bax increased 1.62-fold, while the expression of Bcl-2 decreased 0.76-fold at 135.6 µM/mL concentration of Fe3O4@Glu/PTSC compared to untreated A549 cells. Furthermore, the Fe3O4@Glu/PTSC nanoparticulate-inducing apoptosis properties were evaluated by Hoechst 33258 staining, Caspase-3 activation assay and Annexin V/propidium iodide staining. The results of the present study suggest that Fe3O4@Glu/PTSC nanoparticulates exhibit effective anti-cancer activity against lung cancer cells.
Keywords: A549 cells; Apoptosis; Fe3O4@Glu/PTSC; Lung cancer.