The development of functional imaging is a promising strategy for diagnosis and treatment of infectious and cancerous diseases. In this study, epirubicin was developed as a [^99mTc]‐labeled radiopharmaceutical for the imaging of multi‐drug‐resistant Staphylococcus aureus infections. The labeling was carried out using sodium pertechnetate (Na^99mTcO₄; ~370 MBq). The other parameters such as amount of ligand, reducing agent (SnCl₂.2H₂O), and pH were optimized. The highest labeling yield ≥96.98% was achieved when 0.3 mg epirubicin, 13 μg SnCl₂.2H₂O, and ~370 MBq Na^99mTcO₄ were incubated at pH 7 for 15 min in the presence of ascorbic acid at room temperature. Radiochemical purity, stability, charge, and glomerular filtration rate were studied to evaluate the biological compatibility for in vivo administration. Biodistribution investigations showed radiotracer uptake (13.89 ± 1.56% ID/gm organ) by liver and 7.79 ± 0.38% ID/gm organ by kidneys at 30 min post‐injection which promisingly wash out at 24 hr post‐injection. Scintigraphy study showed selective uptake in S. aureus‐infected tissues in contrast to turpentine oil‐induced inflamed tissues. Target‐to‐non‐target ratio (6.7 ± 0.05) was calculated at 1 hr post‐injection using SPECT gamma camera. The results of this study reveal that the [^99mTc]‐epirubicin can be a choice of imaging and monitoring the treatment process of multi‐drug resistant S. aureus bacterial infections.

中文翻译：

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net 99m放射标记和表柔比星的生物学研究，用于通过单光子发射计算机断层摄影术对多药耐药金黄色葡萄球菌感染进行体内成像

功能成像的发展是诊断和治疗传染性和癌性疾病的有前途的策略。在这项研究中，表柔比星被开发为一种[ ^99m Tc]标记的放射性药物，用于对多药耐药的金黄色葡萄球菌感染进行成像。使用高was酸钠（Na ^99m TcO ₄；〜370 MBq）进行标记。优化了其他参数，例如配体的量，还原剂（SnCl ₂ .2H ₂ O）和pH。当0.3 mg表柔比星，13μgSnCl ₂ .2H ₂ O和〜370 MBq Na ^99m TcO ₄时，达到最高标记产率≥96.98％。在室温下在抗坏血酸存在下将其在pH 7下温育15分钟。研究了放射化学纯度，稳定性，电荷和肾小球滤过率，以评估体内给药的生物相容性。生物分布调查显示，注射后30分钟，肝脏吸收放射性示踪剂（13.89±1.56％ID / gm器官），肾脏摄取7.79±0.38％ID / gm器官，有望在注射后24小时冲洗掉。闪烁扫描研究表明，与松节油引起的发炎组织相比，金黄色葡萄球菌感染的组织有选择性摄取。在注射后1小时使用SPECT伽玛相机计算目标与非目标的比率（6.7±0.05）。这项研究的结果表明，[ ^99mTc]-厄比霉素可能是对多种药物耐药的金黄色葡萄球菌细菌感染进行成像和监测治疗过程的一种选择。