Novel pyridinecarboxaldehyde thiosemicarbazone conjugated magnetite nanoparticulates (MNPs) promote apoptosis in human lung cancer A549 cells

The present study highlights the apoptotic activity of magnetic Fe 3 O 4 nanoparticulates functionalized by glutamic acid and 2-pyridinecarboxaldehyde thiosemicarbazone (PTSC) toward human lung epithelial carcinoma A549 cell line. To this aim, the Fe 3 O 4 nanoparticulates were prepared using co-precipitation method. Then, the glutamic acid and Fe 3 O 4 nanoparticulates were conjugated to each other. The product was further functionalized with bio-reactive PTSC moiety. In addition, the synthesized Fe 3 O 4 @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 (IC 50 = 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, Fe 3 O 4 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 Fe 3 O 4 @Glu/PTSC compared to untreated A549 cells. Furthermore, the Fe 3 O 4 @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 Fe 3 O 4 @Glu/PTSC nanoparticulates exhibit effective anti-cancer activity against lung cancer cells.