Design, Preparation, and Evaluation of a Novel <sup>99m</sup>TcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent

Si’an Fang; Yuhao Jiang; Qianqian Gan; Qing Ruan; Di Xiao; Junbo Zhang

doi:10.3390/molecules25245837

Molecules (Dec 2020)

Design, Preparation, and Evaluation of a Novel <sup>99m</sup>TcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent

Si’an Fang,
Yuhao Jiang,
Qianqian Gan,
Qing Ruan,
Di Xiao,
Junbo Zhang

Affiliations

Si’an Fang: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
Yuhao Jiang: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
Qianqian Gan: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
Qing Ruan: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
Di Xiao: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
Junbo Zhang: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China

DOI: https://doi.org/10.3390/molecules25245837
Journal volume & issue: Vol. 25, no. 24
p. 5837

Abstract

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In order to seek novel technetium-99m bacterial infection imaging agents, a ciprofloxacin xanthate (CPF2XT) was synthesized and radiolabeled with [99mTcN]2+ core to obtain the 99mTcN-CPF2XT complex, which exhibited high radiochemical purity, hydrophilicity, and good stability in vitro. The bacteria binding assay indicated that 99mTcN-CPF2XT had specificity to bacteria. A study of biodistribution in mice showed that 99mTcN-CPF2XT had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses, indicating that it could distinguish bacterial infection from sterile inflammation. Compared to 99mTcN-CPFXDTC, the abscess/blood and abscess/muscle ratios of 99mTcN-CPF2XT were higher and the uptakes of 99mTcN-CPF2XT in the liver and lung were obviously decreased. The results suggested that 99mTcN-CPF2XT would be a potential bacterial infection imaging agent.

Published in Molecules

ISSN: 1420-3049 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Chemistry: Organic chemistry
Website: http://www.mdpi.com/journal/molecules

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