Real-time monitoring of drug metabolism in vivo is of great significance to drug development and toxicology research. The purpose of this study is to establish a rapid and visual in vivo detection method for the detection of an intermediate metabolite of the gold (I) drug. Gold (I) drugs such as sodium aurothiomalate (AuTM) have anti-inflammatory effects in the treatment of rheumatoid arthritis. Gold(III) ions (Au³⁺) are the intermediate metabolite of gold medicine, and they are also the leading factor of side effects in the treatment of patients. However, the rapid reduction of Au³⁺ to Au⁺ by thiol proteins in organisms limits the in-depth study of metabolism of gold drugs in vivo. Here we describe a luminescence Au³⁺ probe (RA) based on ruthenium (II) complex for detecting Au³⁺ in vitro and in vivo. RA with large Stokes shift, good water solubility and biocompatibility was successfully applied to detect Au³⁺ in living cells and vivo by luminescence imaging, and to trap the fluctuation of Au³⁺ level produced by gold (I) medicine. More importantly, the luminescent probe was used to the detection of the intermediate metabolites of gold (I) drugs for the first time. Overall, this work offers a new detection tool/method for a deeper study of gold (I) drugs metabolite.

实时监测体内药物代谢对药物开发和毒理学研究具有重要意义。本研究的目的是建立一种快速、可视化的体内检测方法，用于检测金（I）药物的中间代谢物。金 (I) 药物如金硫苹果酸钠 (AuTM) 在治疗类风湿性关节炎方面具有抗炎作用。金(III)离子(Au ³⁺ )是金药的中间代谢产物，也是患者治疗中出现副作用的首要因素。然而，快速降低的Au ³⁺与Au ⁺生物体通过硫醇蛋白限制了金药物在体内代谢的深入研究。在这里，我们描述了一个发光 Au ³⁺探针（RA ) 基于钌 (II) 络合物，用于体外和体内检测 Au ³⁺。RA具有大的斯托克斯位移，良好的水溶性和生物相容性成功地应用于检测的Au ³⁺在活细胞和体内通过发光成像，并且套住Au构成的波动³⁺水平由金（I）药制造。更重要的是，该发光探针首次用于金（I）类药物中间代谢物的检测。总的来说，这项工作为更深入地研究金 (I) 药物代谢物提供了一种新的检测工具/方法。