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Radiosynthesis and Bioevaluation of 99mTc-Labeled Isocyanide Ubiquicidin 29-41 Derivatives as Potential Agents for Bacterial Infection Imaging.


ABSTRACT: To develop a novel 99mTc-labeled ubiquicidin 29-41 derivative for bacterial infection single-photon emission computed tomography (SPECT) imaging with improved target-to-nontarget ratio and lower nontarget organ uptake, a series of isocyanide ubiquicidin 29-41 derivatives (CNnUBI 29-41, n = 5-9) with different carbon linkers were designed, synthesized and radiolabeled with the [99mTc]Tc(I)+ core, [99mTc][Tc(I)(CO)3(H2O)3]+ core and [99mTc][Tc(V)N]2+ core. All the complexes are hydrophilic, maintain good stability and specifically bind Staphylococcus aureus in vitro. The biodistribution in mice with bacterial infection and sterile inflammation demonstrated that [99mTc]Tc-CN5UBI 29-41 was able to distinguish bacterial infection from sterile inflammation, which had an improved abscess uptake and a greater target-to-nontarget ratio. SPECT imaging study of [99mTc]Tc-CN5UBI 29-41 in bacterial infection mice showed that there was a clear accumulation in the infection site, suggesting that this radiotracer could be a potential radiotracer for bacterial infection imaging.

SUBMITTER: Jiang Y 

PROVIDER: S-EPMC10816394 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature

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Radiosynthesis and Bioevaluation of <sup>99m</sup>Tc-Labeled Isocyanide Ubiquicidin 29-41 Derivatives as Potential Agents for Bacterial Infection Imaging.

Jiang Yuhao Y   Han Peiwen P   Yin Guangxing G   Wang Qianna Q   Feng Junhong J   Ruan Qing Q   Xiao Di D   Zhang Junbo J  

International journal of molecular sciences 20240115 2


To develop a novel <sup>99m</sup>Tc-labeled ubiquicidin 29-41 derivative for bacterial infection single-photon emission computed tomography (SPECT) imaging with improved target-to-nontarget ratio and lower nontarget organ uptake, a series of isocyanide ubiquicidin 29-41 derivatives (CNnUBI 29-41, <i>n</i> = 5-9) with different carbon linkers were designed, synthesized and radiolabeled with the [<sup>99m</sup>Tc]Tc(I)<sup>+</sup> core, [<sup>99m</sup>Tc][Tc(I)(CO)<sub>3</sub>(H<sub>2</sub>O)<sub>  ...[more]

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