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Tc-甲硝唑的放射性合成与生物分布作为大肠杆菌感染的影像学放射性药物。

Radiosynthesis and Biodistribution of Tc-Metronidazole as an Escherichia coli Infection Imaging Radiopharmaceutical.

机构信息

Department of Chemistry, Government College University, Faisalabad, -38000, Pakistan.

Department of Nuclear Medicine, Institute of Nuclear Medicine Oncology and Radiotherapy (INOR), Abbottabad, Pakistan.

出版信息

Appl Biochem Biotechnol. 2018 May;185(1):127-139. doi: 10.1007/s12010-017-2641-y. Epub 2017 Nov 2.

Abstract

Bacterial infection poses life-threatening challenge to humanity and stimulates to the researchers for developing better diagnostic and therapeutic agents complying with existing theranostic techniques. Nuclear medicine technique helps to visualize hard-to-diagnose deep-seated bacterial infections using radionuclide-labeled tracer agents. Metronidazole is an antiprotozoal antibiotic that serves as a preeminent anaerobic chemotherapeutic agent. The aim of this study was to develop technetium-99m-labeled metronidazole radiotracer for the detection of deep-seated bacterial infections. Radiosynthesis of Tc-metronidazole was carried by reacting reduced technetium-99m and metronidazole at neutral pH for 30 min. The stannous chloride dihydrate was used as the reducing agent. At optimum radiolabeling conditions, ~ 94% radiochemical was obtained. Quality control analysis was carried out with a chromatographic paper and instant thin-layer chromatographic analysis. The biodistribution study of radiochemical was performed using Escherichia coli bacterial infection-induced rat model. The scintigraphic study was performed using E. coli bacterial infection-induced rabbit model. The results showed promising accumulation at the site of infection and its rapid clearance from the body. The tracer showed target-to-non-target ratio 5.57 ± 0.04 at 1 h post-injection. The results showed that Tc-MNZ has promising potential to accumulate at E. coli bacterial infection that can be used for E. coli infection imaging.

摘要

细菌感染对人类构成生命威胁,促使研究人员开发符合现有治疗技术的更好的诊断和治疗药物。核医学技术有助于使用放射性核素标记示踪剂可视化难以诊断的深部细菌性感染。甲硝唑是一种抗原生动物抗生素,可用作卓越的厌氧化学治疗剂。本研究旨在开发用于检测深部细菌性感染的锝-99m 标记甲硝唑放射性示踪剂。通过在中性 pH 值下将还原的锝-99m 和甲硝唑反应 30 分钟来进行 Tc-甲硝唑的放射合成。使用二水合氯化亚锡作为还原剂。在最佳标记条件下,可获得约 94%的放射化学纯度。通过纸色谱和即时薄层色谱分析进行质量控制分析。使用大肠杆菌细菌感染诱导的大鼠模型进行放射性示踪剂的生物分布研究。使用大肠杆菌细菌感染诱导的兔模型进行闪烁照相研究。结果表明,在感染部位有很好的蓄积,并且很快从体内清除。示踪剂在注射后 1 小时的靶标与非靶标比值为 5.57±0.04。结果表明,Tc-MNZ 具有在大肠杆菌感染部位蓄积的良好潜力,可用于大肠杆菌感染成像。

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