具有荧光示踪与细胞毒性双功能的金属铱配位化合物的研究

可示踪药物能在治疗的同时提供药物、病灶的实时动态信息，具有广泛应用前景。但面临标记过程繁琐、标记分子影响药物活性、标记物与药物分子易解离等问题。部分金属铱配位化合物具有独特的光学特性和潜在的药物活性，有望用于免标记可示踪药物的研发。目前，综合利用铱配合物光学特征和药物活性的研究还处于起步阶段。本项目根据课题组前期工作基础，筛选与优化同时具有荧光特征、细胞毒性的金属铱配合物，归纳外周配体结构对其荧光特性及细胞毒性的影响，以期获得"荧光示踪-细胞毒性"双功能金属铱配位化合物结构。在此基础上，通过荧光金属铱药物分子的生物功能化和载体纳米化，构建此类金属铱药物的复合体系，在保持"荧光示踪-细胞毒性"双功能同时实现药物的靶向性、专一性和稳定性。本项目为发光金属铱抗癌药物的研发提供早期实验数据，有助于推动其在生物医学领域的进一步应用。

Traceable drugs provide visual and accurate information for real-time monitoring of therapeutic responses. But the conventional labeling technique has several disadvantages, such as multi-step and time-consuming procedure, often compromised drug activity, instability of molecule conjugates in vivo. Recently, some iridium (III) complexes with potential anti-tumor activities were reported. If combined with their unique luminescent properties, the iridium (III) complexes can be exploited as label-free traceable luminescent metal drugs. This project will screen and optimize a series of iridium (III) complexes with luminescent properties and cytotoxicity on the basis of previous work. Specifically, we will investigate the influence of ligand structure on the luminescence and cytotoxicity of complexes. Furthermore, such a metal iridium drug compound system by biological function and carrier nanocrystallization, were constructed to achieve targeting, specificity and stability. This project will provide early experimental data for the development of luminescent iridium (III) metal drugs, and help promote its further application in biomedical field.