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锝-99m标记的磺胺嘧啶:一种用于小鼠和兔模型中大肠杆菌感染灶闪烁成像的靶向放射性药物。

Technetium-99m-Labeled Sulfadiazine: a Targeting Radiopharmaceutical for Scintigraphic Imaging of Infectious Foci Due To Escherichia coli in Mouse and Rabbit Models.

作者信息

Ahmed Muhammad Tauqeer, Naqvi Syed Ali Raza, Rasheed Rashid, Zahoor Ameer Fawad, Usman Muhammad, Hussain Zaib

机构信息

Department of Chemistry, Government College University, Faisalabad, 38040, Pakistan.

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

出版信息

Appl Biochem Biotechnol. 2017 Sep;183(1):374-384. doi: 10.1007/s12010-017-2451-2. Epub 2017 Mar 11.

Abstract

Bacterial infection is one of the vital reasons of morbidity and mortality, especially in developing countries. It appears silently without bothering the geological borders and imposes a grave threat to humanity. Nuclear medicine technique has an important role in helping early diagnosis of deep-seated infections. The aim of this study was to develop a new radiopharmaceutical Tc-labeling sulfadiazine as an infection imaging agent. Radiolabeling of sulfadiazine with technetium-99m (Tc) was carried out using stannous tartrate as a reducing agent in the presence of gentistic acid at pH = 5. The quality control tests revealed ~98% labeling efficiency. Paper chromatographic (PC) and instant thin-layer chromatographic (ITLC) techniques were used to analyze radiochemical yield. Biodistribution and infection specificity of the radiotracer were performed with Escherichia coli (E. coli) infection-induced rats. Scintigraphy and glomerular filtration rate (GFR) study was performed in E. coli-infected rabbits. Scintigraphy indicated E. coli infection targeting potential of Tc-SDZ, while biodistribution study showed minimal uptake of Tc-SDZ in non-targeted tissues. The uptake in the kidneys was found 2.56 ± 0.06, 2.09 ± 0.10, and 1.68 ± 0.09% at 30 min, 1 h, and 4 h, respectively. The infected muscle (target) to non-infected muscle (non-target) ratio (T/NT) was found 4.49 ± 0.04, 6.78 ± 0.07, and 5.59 ± 0.08 at 30 min, 1 h, and 4 h, respectively.

摘要

细菌感染是发病和死亡的重要原因之一,尤其是在发展中国家。它悄然出现,不受地理边界的限制,对人类构成严重威胁。核医学技术在帮助早期诊断深部感染方面具有重要作用。本研究的目的是开发一种新的放射性药物——锝标记磺胺嘧啶作为感染显像剂。在pH = 5的条件下,以酒石酸亚锡作为还原剂,在龙胆酸存在的情况下,用锝-99m(Tc)对磺胺嘧啶进行放射性标记。质量控制测试显示标记效率约为98%。采用纸色谱(PC)和即时薄层色谱(ITLC)技术分析放射化学产率。用大肠杆菌(E. coli)感染诱导的大鼠进行放射性示踪剂的生物分布和感染特异性研究。在大肠杆菌感染的兔子身上进行闪烁扫描和肾小球滤过率(GFR)研究。闪烁扫描表明Tc-SDZ具有靶向大肠杆菌感染的潜力,而生物分布研究显示非靶向组织中Tc-SDZ的摄取量极少。在30分钟、1小时和4小时时,肾脏的摄取量分别为2.56±0.06%、2.09±0.10%和1.68±0.09%。在30分钟、1小时和4小时时,感染肌肉(靶组织)与未感染肌肉(非靶组织)的比值(T/NT)分别为4.49±0.04、6.78±0.07和5.59±0.08。

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