Developing new anticancer agents can be useful, with the ability to diagnose and treat cancer worldwide. Previously, we focused on examining the effects of nonoxidovanadium(IV) complexes on insulin mimetic and cytotoxicity activity. In this study, in addition to the cytotoxic activity, we evaluated their bioimaging properties. This study investigates the synthesis of four stable nonoxido V^IV complexes [V^IV(L^1–4)₂] (1–4) using aroylhydrazone ligands (H₂L^1–4) and their full characterization in solid state and the solution phase stability using various physicochemical techniques. The biomolecular (DNA/HSA) interaction of the complexes was evaluated by using conventional methods. The in vitro cytotoxicity of 1–4 was studied against A549 and LN-229 cancer cell lines and found that drug 2 displayed the highest activity among the four. Since 1–4 are fluorescently active, live cell imaging was used to evaluate their cellular localization activity. Complexes specifically target the lysosome and damage lysosome integrity by producing an excessive amount (9.7-fold) of reactive oxygen species (ROS) compared to the control, which may cause cell apoptosis. Overall, this study indicates that 2 has the greatest potential for the development of multifunctional theranostic agents that combine imaging capabilities and anticancer properties of nonoxidovanadium(IV)-based metallodrugs.

中文翻译：

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深入了解 Nonoxido VIV 的治疗诊断活性：溶酶体靶向抗癌金属药物


开发新的抗癌药物可能很有用，能够在全球范围内诊断和治疗癌症。以前，我们专注于研究壬氧钒 （IV） 复合物对胰岛素模拟物和细胞毒性活性的影响。在这项研究中，除了细胞毒活性外，我们还评估了它们的生物成像特性。本研究研究了使用芳基腙配体 （H₂L^1-4） 合成四种稳定的壬氧 V^IV 复合物 [V^IV（L^1–4）₂] （1–4），以及它们在固态和液相稳定性下使用各种物理化学技术的完整表征。使用常规方法评估复合物的生物分子 （DNA/HSA） 相互作用。研究了 1-4 对 A549 和 LN-229 癌细胞系的体外细胞毒性，发现药物 2 在四种细胞系中表现出最高的活性。由于 1-4 具有荧光活性，因此使用活细胞成像来评估其细胞定位活性。与对照相比，复合物特异性靶向溶酶体并通过产生过量（9.7 倍）的活性氧 （ROS） 来破坏溶酶体的完整性，这可能会导致细胞凋亡。总体而言，这项研究表明 2 在开发多功能治疗诊断剂方面具有最大的潜力，这些药物结合了基于非氧化钒 （IV） 的金属药物的成像能力和抗癌特性。