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.

中文翻译：

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新型吡啶甲醛硫代半碳酸盐共轭磁铁矿纳米颗粒（MNP）促进人肺癌A549细胞凋亡。

本研究强调了由谷氨酸和2-吡啶甲醛硫代半脲（PTSC）功能化的磁性Fe ₃ O ₄纳米微粒对人肺上皮癌A549细胞的凋亡活性。为此，使用共沉淀法制备了Fe ₃ O ₄纳米颗粒。然后，将谷氨酸和Fe ₃ O ₄纳米颗粒彼此共轭。该产物用生物反应性PTSC部分进一步官能化。另外，合成的Fe ₃ O ₄@ Glu / PTSC纳米粒子的物理化学技术包括扫描电子显微镜（SEM），能量色散X射线（EDX），X射线衍射（XRD），傅立叶变换红外（FT-IR）光谱和Zeta电位分析。Fe3O4 @ Glu / PTSC纳米颗粒中体外细胞活力的影响以剂量依赖性方式显示了抗增殖特性（IC ₅₀  = 135.6 µM / mL）。对肿瘤细胞的高选择性和远低于HEK293非致瘤细胞的活性被认为是该复合物的重要特征（SI，3.48）。根据结果​​，PTSC未能显示出仅针对A549细胞的任何活性。但是，Fe ₃ O ₄纳米颗粒具有抑制肺癌细胞生长的作用。此外，通过实时PCR方法定量Bax和Bcl - 2基因表达。与未处理的A549细胞相比，在135.6 µM / mL的Fe ₃ O ₄ @ Glu / PTSC浓度下，Bax的表达增加1.62倍，而Bcl - 2的表达减少0.76倍。此外，通过Hoechst 33258染色，Caspase-3活化分析和Annexin V /碘化丙锭染色评估了Fe ₃ O ₄ @ Glu / PTSC纳米颗粒诱导的凋亡特性。本研究结果表明，铁₃ O ₄ @ Glu / PTSC纳米颗粒对肺癌细胞表现出有效的抗癌活性。