Design, Preparation, and Evaluation of a Novel 99mTcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent.

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

doi:10.3390/molecules25245837

Si’An Fang, Yuhao Jiang + Show 4 more

Open Access

https://doi.org/10.3390/molecules25245837

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Journal: Molecules (Basel, Switzerland)	Publication Date: Dec 10, 2020
Citations: 4	License type: CC BY 4.0

Affiliation: Beijing Normal University

Abstract

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.

Highlights

Public health advanced during the eighteenth and nineteenth centuries and with antibiotics discovered in the twentieth century, treatment of infection has been highly improved
Ciprofloxacin xanthate containing two sulfur atoms could conjugate with the [99m TcN]2+ core to obtain a stable complex in the form of 99m TcN(L)2 (L = bidentate ligand). [99m TcO4 ]− and the Succinic dihydrazide (SDH) kit were mixed to form a [99m TcN]2+ intermediate
99m TcN-CPF2XT remains the pharmacophores of ciprofloxacin, which bind to bacteria

Summary

Introduction

Public health advanced during the eighteenth and nineteenth centuries and with antibiotics discovered in the twentieth century, treatment of infection has been highly improved. Bacterial infection is one of the most common causes of morbidity and mortality in developing countries [1]. It is predicted that infections of antibiotic resistance would be the first cause of human death by 2050 [2]. Considering the patients carrying inflammation may have different disease processes occurring at the same time, the clinic assessments do not always find a clear pathogen, which leads to delay in treatment and antibiotic abuse. Early detection of infections can allow for the timely and appropriate treatment of patients, avoiding the overuse of antibiotics [3]

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Discussion

Conclusion