The ability of some tumours to impart radioresistance serves as a barrier in the cancer therapeutics. Mitochondrial metabolism significantly persuades this cancer cell survival, incursion and plays a crucial role in conferring radioresistance. It would be of great importance to target the active mitochondria to overcome this resistance and achieve tumoricidal efficacy. The current report investigates the improved radiosensitization effect (under Gamma irradiation) in hepatocellular carcinoma through active mitochondrial targeting of alpha-ketoglutarate decorated iron oxide-gold core-shell nanoparticles (GNP). The loading of a chemotherapeutic drug N-(4-hydroxyphenyl)retinamide in GNP allows adjuvant chemotherapy, which further sensitizes cancerous cells for radiotherapy. The GNP shows a drug loading efficiency of 8.5 wt% with a sustained drug release kinetics. The X-Ray diffraction (XRD) pattern and High-Resolution Transmission Electron microscopy (HRTEM) indicates the synthesis of core iron oxide nanoparticles with indications of a thin layer of gold shell on the surface with 1:7 ratios of Fe: Au. The GNP application significantly reduced per cent cell viability in Hepatocellular carcinoma cells through improved radiosensitization at 5 Gy gamma radiation dose. The molecular mechanism revealed a sharp increment in reactive oxygen species (ROS) generation and DNA fragmentation. The mitochondrial targeting probes confirm the presence of GNP in the mitochondria, which could be the possible reason for such improved cellular damage. In addition to the active mitochondrial targeting, the currently fabricated nanoparticles work as a potent Magnetic Resonance Imaging (MRI)/Computed Tomography (CT) contrast agent. This multifunctional therapeutic potential makes GNP as one of the most promising theragnostic molecules in cancer therapeutics.

一些肿瘤赋予放射抗性的能力是癌症治疗中的障碍。线粒体代谢显着说服了这种癌细胞的存活、侵袭，并在赋予放射抗性方面发挥着至关重要的作用。靶向活性线粒体以克服这种抗性并实现杀瘤功效将是非常重要的。目前的报告研究了通过α-酮戊二酸修饰的氧化铁金核壳纳米粒子 (GNP) 的活性线粒体靶向改善肝细胞癌的放射增敏作用（在伽马照射下）。在 GNP 中加入化疗药物 N-(4-羟基苯基) 视黄酰胺允许辅助化疗，这进一步使癌细胞对放疗敏感。GNP 显示载药效率为 8。5 wt% 具有持续的药物释放动力学。X 射线衍射 (XRD) 图案和高分辨率透射电子显微镜 (HRTEM) 表明合成了核心氧化铁纳米粒子，并显示表面有一层薄薄的金壳，Fe:Au 的比例为 1:7。GNP 应用通过提高 5 Gy 伽马辐射剂量的放射增敏作用，显着降低了肝细胞癌细胞的细胞活力百分比。分子机制揭示了活性氧 (ROS) 生成和 DNA 断裂的急剧增加。线粒体靶向探针证实了线粒体中 GNP 的存在，这可能是细胞损伤改善的可能原因。除了主动的线粒体靶向，目前制造的纳米颗粒可用作有效的磁共振成像 (MRI)/计算机断层扫描 (CT) 造影剂。这种多功能治疗潜力使 GNP 成为癌症治疗中最有前途的治疗诊断分子之一。