Naqvi Syed Ali Raza, Roohi Samina, Iqbal Anam, Sherazi Tauqir A, Zahoor Ameer Fawad, Imran Muhammad
Department of Chemistry, Government College University, Faisalabad, 38000, Pakistan.
Isotope Production Division, Pakistan Institute of Nuclear Science and Technology (PINSTECH), Nilore-Islamabad, Pakistan.
Mol Biol Rep. 2018 Oct;45(5):1457-1468. doi: 10.1007/s11033-018-4220-x. Epub 2018 Jul 4.
Diagnosis of deep-seated bacterial infection remains a serious medical challenge. The situation is becoming more severe with the increasing prevalence of bacteria that are resistant to multiple antibiotic classes. Early efforts to develop imaging agents for infection, such as technetium-99m (Tc) labeled leukocytes, were encouraging, but they failed to differentiate between bacterial infection and sterile inflammation. Other diagnostic techniques, such as ultrasonography, magnetic resonance imaging, and computed tomography, also fail to distinguish between bacterial infection and sterile inflammation. In an attempt to bypass these problems, the potent, broad-spectrum antibiotic ciprofloxacin was labeled with Tc to image bacterial infection. Initial results were encouraging, but excitement declined when controversial results were reported. Subsequent radiolabeling of ciprofloxacin with Tc using tricarbonyl and nitrido core, fluorine and rhenium couldn't produce robust infection imaging agent and remained in discussion. The issue of developing a robust probe can be approached by reviewing the broad-spectrum activity of ciprofloxacin, labeling strategies, potential for imaging infection, and structure-activity (specificity) relationships. In this review we discuss ways to accelerate efforts to improve the specificity of ciprofloxacin-based imaging.
深部细菌感染的诊断仍然是一项严峻的医学挑战。随着对多种抗生素耐药的细菌患病率不断上升，情况变得愈发严峻。早期开发用于感染的成像剂的努力，如锝-99m（Tc）标记的白细胞，令人鼓舞，但它们无法区分细菌感染和无菌性炎症。其他诊断技术，如超声检查、磁共振成像和计算机断层扫描，也无法区分细菌感染和无菌性炎症。为了绕过这些问题，强效广谱抗生素环丙沙星用Tc进行标记以成像细菌感染。初步结果令人鼓舞，但当有争议的结果被报道时，热情有所下降。随后使用三羰基和氮化物核心、氟和铼对环丙沙星进行Tc放射性标记，未能产生强大的感染成像剂，仍在讨论中。开发一种强大探针的问题可以通过回顾环丙沙星的广谱活性、标记策略、感染成像潜力以及构效（特异性）关系来解决。在本综述中，我们讨论了加速提高基于环丙沙星成像特异性的努力的方法。
