MicroPET imaging of bacterial infection with nitroreductase-specific responsive 18F-labelled nitrogen mustard analogues.

Purpose: Bacterial infection and antibiotic resistance are serious threats to human health. This study aimed to develop two novel radiotracers, 18F-NTRP and 18F-NCRP, that possess a specific nitroreductase (NTR) response to image deep-seated bacterial infections using positron emission tomography (P...

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Publicado en:European Journal of Nuclear Medicine & Molecular Imaging Vol. 49; no. 8; pp. 2645 - 2655
Autores principales: Huang, Lumei, Fang, Jianyang, Hong, Shouqiang, Liu, Huanhuan, Zhu, Haotian, Feng, Lixia, Zhuang, Rongqiang, Zhao, Xilin, Guo, Zhide, Zhang, Xianzhong
Formato: Journal Article
Publicado: Springer Nature Jul2022
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Jul2022
      vid: 49
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      pub: Springer Nature
      place: New York, New York
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        157529115
        155054573
        10.1007/s00259-022-05710-2
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        atl: MicroPET imaging of bacterial infection with nitroreductase-specific responsive 18F-labelled nitrogen mustard analogues.
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          Huang, Lumei
          Fang, Jianyang
          Hong, Shouqiang
          Liu, Huanhuan
          Zhu, Haotian
          Feng, Lixia
          Zhuang, Rongqiang
          Zhao, Xilin
          Guo, Zhide
          Zhang, Xianzhong
        affil: State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, 361102, Xiamen, Fujian, China
      sug:
      ab: Purpose: Bacterial infection and antibiotic resistance are serious threats to human health. This study aimed to develop two novel radiotracers, 18F-NTRP and 18F-NCRP, that possess a specific nitroreductase (NTR) response to image deep-seated bacterial infections using positron emission tomography (PET). This method can distinguish infection from sterile inflammation. Methods: 18F-NTRP and 18F-NCRP were synthesized via a one-step method; all the steps usually involved in tracer radiosynthesis were successfully adapted in the All-In-One automated module. After the physiochemical properties of 18F-NTRP and 18F-NCRP were characterized, their specificity and selectivity for NTR were verified in E. coli and S. aureus. The ex vivo biodistribution of the tracers was evaluated in normal mice. MicroPET-CT imaging was performed in mouse models of bacterial infection and inflammation after the administration of 18F-NTRP or 18F-NCRP. Results: Fully automated radiosynthesis of 18F-NTRP and 18F-NCRP was achieved within 90–110 min with overall decay-uncorrected, isolated radiochemical yields of 21.24 ± 4.25% and 11.3 ± 3.78%, respectively. The molar activities of 18F-NTRP and 18F-NCRP were 320 ± 40 GBq/μmol and 275 ± 33 GBq/µmol, respectively. In addition, 18F-NTRP and 18F-NCRP exhibited high selectivity and specificity for NTR response. PET-CT imaging in bacteria-infected mouse models with 18F-NTRP or 18F-NCRP showed significant radioactivity uptake in either E. coli– or S. aureus–infected muscles. The uptake for E. coli–infected muscles, 2.4 ± 0.2%ID/g with 18F-NTRP and 4.05 ± 0.49%ID/g with 18F-NCRP, was up to three times greater than that for uninfected control muscles. Furthermore, for both 18F-NTRP and 18F-NCRP, the uptake in bacterial infection was 2.6 times higher than that in sterile inflammation, allowing an effective distinction of infection from inflammation. Conclusion: 18F-NTRP and 18F-NCRP are worth further investigation to verify their potential clinical application for distinguishing bacterial infection from sterile inflammation via their specific NTR responsiveness.
      pubtype: Academic Journal
      doctype: Journal Article
      ougenre: Article
    language: English
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