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

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5837
Author(s):  
Si’an Fang ◽  
Yuhao Jiang ◽  
Qianqian Gan ◽  
Qing Ruan ◽  
Di Xiao ◽  
...  
Keyword(s):  
Bacterial Infection ◽  
Radiochemical Purity ◽  
Binding Assay ◽  
Sterile Inflammation ◽  
Good Stability ◽  
Imaging Agent ◽  
Imaging Agents ◽  
Infection Imaging ◽  
Preparation And Evaluation

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.

scholarly journals Synthesis and Evaluation of Novel Norfloxacin Isonitrile 99mTc Complexes as Potential Bacterial Infection Imaging Agents

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 518
Author(s):  
Si’an Fang ◽  
Yuhao Jiang ◽  
Di Xiao ◽  
Xuran Zhang ◽  
Qianqian Gan ◽  
...  
Keyword(s):  
Bacterial Infection ◽  
Single Photon ◽  
Photon Emission ◽  
Sterile Inflammation ◽  
Imaging Agents ◽  
Emission Computed Tomography ◽  
Infection Imaging ◽  
Spect Image ◽  
Biodistribution Studies

To develop potential technetium-99m single-photon emission computed tomography (SPECT) imaging agents for bacterial infection imaging, the novel norfloxacin isonitrile derivatives CN4NF and CN5NF were synthesized and radiolabeled with a [99mTc][Tc(I)]+ core to obtain [99mTc]Tc-CN4NF and [99mTc]Tc-CN5NF. These compounds were produced in high radiolabeling yields and showed hydrophilicity and good stability in vitro. The bacterial binding assay indicated that [99mTc]Tc-CN4NF and [99mTc]Tc-CN5NF were specific to bacteria. Compared with [99mTc]Tc-CN4NF, biodistribution studies of [99mTc]Tc-CN5NF showed a higher uptake in bacteria-infected tissues than in turpentine-induced abscesses, indicating that [99mTc]Tc-CN5NF could distinguish bacterial infection from sterile inflammation. In addition, [99mTc]Tc-CN5NF had higher abscess/blood and abscess/muscle ratios. SPECT image of [99mTc]Tc-CN5NF showed that there was a clear accumulation in the infection site, suggesting that it could be a potential bacterial infection imaging radiotracer.

scholarly journals Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4552
Author(s):  
Junhong Feng ◽  
Xuran Zhang ◽  
Qing Ruan ◽  
Yuhao Jiang ◽  
Junbo Zhang
Keyword(s):  
Radiochemical Purity ◽  
Tumor Imaging ◽  
Folate Receptor ◽  
Imaging Agents ◽  
Folate Receptors ◽  
Biodistribution Studies ◽  
Specific Tumor ◽  
Folate Receptor Targeting ◽  
Preparation And Evaluation

In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA complexes, which exhibited high radiochemical purity (>95%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specific tumor uptake. Compared with [99mTc]Tc-CN5FA, the tumor/muscle ratios of [99mTc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two 99mTc complexes have potential as tumor imaging agents to target folate receptors.

scholarly journals Bacterial infection imaging with [18F]fluoropropyl-trimethoprim

2017 ◽  
Vol 114 (31) ◽  
pp. 8372-8377 ◽  
Author(s):  
Mark A. Sellmyer ◽  
Iljung Lee ◽  
Catherine Hou ◽  
Chi-Chang Weng ◽  
Shihong Li ◽  
...  
Keyword(s):  
Bacterial Infection ◽  
Soft Tissues ◽  
Imaging Techniques ◽  
Sterile Inflammation ◽  
Diagnostic Features ◽  
Cancer Breast ◽  
Positron Emission ◽  
Live Bacteria ◽  
Pathologic Processes

There is often overlap in the diagnostic features of common pathologic processes such as infection, sterile inflammation, and cancer both clinically and using conventional imaging techniques. Here, we report the development of a positron emission tomography probe for live bacterial infection based on the small-molecule antibiotic trimethoprim (TMP). [18F]fluoropropyl-trimethoprim, or [18F]FPTMP, shows a greater than 100-fold increased uptake in vitro in live bacteria (Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa) relative to controls. In a rodent myositis model, [18F]FPTMP identified live bacterial infection without demonstrating confounding increased signal in the same animal from other etiologies including chemical inflammation (turpentine) and cancer (breast carcinoma). Additionally, the biodistribution of [18F]FPTMP in a nonhuman primate shows low background in many important tissues that may be sites of infection such as the lungs and soft tissues. These results suggest that [18F]FPTMP could be a broadly useful agent for the sensitive and specific imaging of bacterial infection with strong translational potential.

Synthesis ofN4′-[18F]Fluoroalkylated Ciprofloxacin as a Potential Bacterial Infection Imaging Agent for PET Study

2010 ◽  
Vol 21 (12) ◽  
pp. 2282-2288 ◽  
Author(s):  
Kalme Sachin ◽  
Eun-Mi Kim ◽  
Su-Jin Cheong ◽  
Hwan-Jeong Jeong ◽  
Seok Tae Lim ◽  
...  
Keyword(s):  
Bacterial Infection ◽  
Imaging Agent ◽  
Infection Imaging

scholarly journals Use of Cyclic Backbone NGR-Based SPECT to Increase Efficacy of Postmyocardial Infarction Angiogenesis Imaging

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Geert Hendrikx ◽  
Tilman M. Hackeng ◽  
Rick van Gorp ◽  
Matthias Bauwens ◽  
Leon J. Schurgers ◽  
...  
Keyword(s):  
Cyclic Peptide ◽  
Imaging Agent ◽  
Imaging Agents ◽  
Peptide Backbone ◽  
Chemical Ligation ◽  
Infarcted Myocardium ◽  
Standardized Uptake Values ◽  
Ngr Peptide

As CD13 is selectively expressed in angiogenesis, it can serve as a target for molecular imaging tracers to noninvasively visualize angiogenic processes in vivo. The CD13-targeting moiety NGR was synthesized and cyclized by native chemical ligation (NCL) instead of disulfide bridging, leading to a cyclic peptide backbone: cyclo(Cys-Asn-Gly-Arg-Gly) (coNGR). Beside this new monomeric coNGR, a tetrameric NGR peptide co(NGR)4 was designed and synthesized. After radiolabeling, their in vitro and in vivo characteristics were determined. Both coNGR-based imaging agents displayed considerably higher standardized uptake values (SUVs) at infarcted areas compared to the previously reported disulfide-cyclized cNGR imaging agent. Uptake patterns of 111In-coNGR and 111In-co(NGR)4 coincided with CD13 immunohistochemistry on excised hearts. Blood stability tests indicated better stability for both novel imaging agents after 50 min blood incubation compared to the disulfide-cyclized cNGR imaging agent. In mice, both coNGR peptides cleared rapidly from the blood mainly via the kidneys. In addition, co(NGR)4 showed a significantly higher specific uptake in infarcted myocardium compared to coNGR and thus is a promising sensitive imaging agent for detection of angiogenesis in infarcted myocardium.

scholarly journals A Novel Method for the Synthesis ofTc99m-Ofloxacin Kits Using D-Penicillamine as Coligand and Their Application as Infection Imaging Agent

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Muhammad Abdul Qadir ◽  
Shabnam Shahzad ◽  
Rashid Rasheed ◽  
Mahmood Ahmed ◽  
Shahzad Anwar ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Pseudomonas Aeruginosa ◽  
Radiochemical Purity ◽  
Salmonella Typhi ◽  
Gram Negative Bacteria ◽  
Infection Imaging ◽  
Vitro Binding ◽  
Novel Method ◽  
In Vitro Stability

The employment of radiopharmaceuticals is increasing nowadays for infection imaging and early execution of patients having infectious or inflammatory complaints. The main aim of this study was to discover a novel method for the labeling of ofloxacin withTc99m, optimization of labelling conditions to get higher percent yield, to assess kits radiochemical purity, in vitro stability, partition coefficient, protein binding, and intracellular accumulation inPseudomonas aeruginosa,Salmonella typhi, andEscherichia coliin infected rabbits. Maximum labeling efficiency was achieved when 1.5 mg ofloxacin was labeled with 10–20 mCi sodium pertechnetate in the presence of 3 mg D-penicillamine, 75 μg SnCl2. In vitro binding and biodistribution inPseudomonas aeruginosa, Salmonella typhi,andEscherichia colishowed good results. This new complex is efficient for the imaging of infections caused by Gram-positive and Gram-negative bacteria.

scholarly journals Synthesis and Preliminary Assessment of 99m tc-HYNIC-Fab´s (Rituximab) for Non-Hodgkin Lymphoma Diagnosis

Blood ◽  
2014 ◽  
Vol 124 (21) ◽  
pp. 5373-5373
Author(s):  
Ximena Camacho ◽  
Camila Machado ◽  
Agustina Banchero ◽  
Maria Fernanda García ◽  
Victoria Calzada ◽  
...  
Keyword(s):  
Lymph Node ◽  
Molecular Imaging ◽  
Hodgkin Lymphoma ◽  
Radiochemical Purity ◽  
Biological Evaluation ◽  
Imaging Agent ◽  
Non Hodgkin Lymphoma ◽  
Molecular Imaging Agent ◽  
Competition Assays

Abstract Introduction: Non-Hodgkin lymphoma (NHL) is the most common hematologic malignancy; more than 90% are B cell lymphomas and express CD-20 antigen. Rituximab® (RTX) is an IgG1κ chimeric anti-CD20 mAb that binds specifically to the CD20-antigen on B lymphocytes. Our group previously reported that 99mTc-RTX represents a promising molecular imaging agent for NHL [1]. When used for tumor imaging, intact IgG exhibits high liver uptake. Antibody fragments (Fab´s) are quickly eliminated from blood and normal tissues (except kidneys), achieving high tumor/blood and tumor/normal tissue ratios with renal clearance. The development of radiolabeled Fab´s directed against specific targets may become a new strategy for NHL staging and surveillance. Objective: To radiolabel Fab´s (RTX) with 99mTc and to perform its chemical and biological evaluation. Methodology: We performed antibody fragmentation with papain and, once purified, fragments were identified by MaldiTOF/TOF and derivatized with Suc-HYNIC as a bifunctional coupling agent. A mixture of Tricine/SnCl2.2H2O was added to Fab´s (RTX)-HYNIC and radiolabeled with 99mTcO4-. Radiochemical purity was determined by HPLC. The in-vitro radiochemical stability of the radiolabeled Fab´s were analyzed in saline and serum up to 4 h. In-vitrobinding and competition assays were performed using Ramos and Raji cell lines up to 90 min. Biodistribution studies were evaluated in normal Balb/c mice and in Raji tumor-bearing Nude mice at 0.5 and 1 h. Results: Radiochemical purity of radiolabeled Fab´s were ≥90%. The in-vitro radiochemical stability studies showed that the radioconjugate was stable and no significant transchelation was detected. In-vitro binding and competition assays confirm that after its derivatization and radiolabeling, Fab´s (RTX) retained its specificity of binding to CD-20 antigen. This results confirm that Fab´s (RTX) affinity for CD20+ NHL cells remained unaffected after its derivatization. In-vivobiodistribution studies show that radiolabeled Fab´s has renal uptake with neglectable uptake in other organs, indicating that the primary route of clearance is renal. Lymph-node/muscle ratios of 4.00 and 2.55 at 0.5 and 1 h post injection, respectively. Conclusions: Fab´s (RTX) were easily and rapidly labeled demonstrating good stability and radiochemical purity. Based on lymph-node uptake and lymph-node/muscle ratios, 99mTc-HYNIC-Fab´s (RTX) may be useful for tumor molecular imaging agent for NHL. Disclosures No relevant conflicts of interest to declare.

scholarly journals 99mTc radiolabeled archaeosomes as a potential melanoma imaging agent

2018 ◽  
Vol 2 (3) ◽  
Author(s):  
Pablo Cabral ◽  
Mirel Cabrera ◽  
Marcos Tassano ◽  
Marcelo Fernadez ◽  
Juan Pablo Gambini
Keyword(s):  
Potential Role ◽  
Radiochemical Purity ◽  
Laser Light ◽  
Imaging Agent ◽  
Renal Elimination ◽  
Imaging Studies ◽  
Scintigraphic Imaging ◽  
In Vitro Stability ◽  
High Liver

Background: Melanoma incidence is growing worldwide. Although recent advances in imaging, there isn`t still available a specific melanoma agent that can be used for melanoma staging. Archaeosomes may be defined as liposomes composed of one or more polar lipids extracted from the Archaea domain (Archaebacterium). Objective:  As liposomes have been used as vehicles for drugs and isotopes, the aim of this work was to 99mTc radiolabel archaeosomes and evaluates its potential role as a melanoma imaging agent.Methods: Archaeosomes were prepared by hand shaken method and were radiolabeled with 99mTc; Radiolabelling efficiency and purity was evaluated through different chromatographic systems. In vitro stability of 99mTc-DTPA-archaeosomes was performed through L-cysteine challenge.Results: Archaeosomes size distribution was determined by laser light scattering, having nanometer size between 90 and 120 nm. Radiolabelling efficiency was greater than 90%; 99mTc-DTPA-Archaeosomes presented a radiochemical purity superior to 80% evaluated 24 hours post radiolabelling. For the highest concentration of L-cysteine (30mM) and 1h incubation,  radiochemical purity was 92.90 %, 6.41 % was bound to cysteine and 0.69 % remained as 99mTcO4- . Biodistribution and scintigraphic imaging studies in healthy C57 black mice showed high liver, spleen uptake and renal elimination. Melanoma bearing mice, had similar biodistribution as healthy mice but increased melanoma uptake, with T/M ratio of 46 ±3.7.Conclusions:  Our results show the feasibility of 99mTc radiolabelling archaeosomes and their potential role as a melanoma imaging agent.

scholarly journals Biological Evaluation of 99mTc-Kanamycin for Infection Imaging

2017 ◽  
Vol 2 (1) ◽  
pp. 34
Author(s):  
Eva Maria Widyasari ◽  
Iim Halimah ◽  
Rizky Juwita Sugiharti ◽  
Maula Eka Sriyani ◽  
Isti Daruwati ◽  
...  
Keyword(s):  
Stationary Phase ◽  
Mobile Phase ◽  
Radiochemical Purity ◽  
Biological Evaluation ◽  
Alkaline Condition ◽  
Infection Imaging ◽  
E Coli ◽  
Technetium 99M ◽  
Direct Labelling

Kanamycin antibiotic was radiolabeled successfully with radioisotope technetium-99m for the potential use as radiopharmaceuticals for infection imaging. <sup>99m</sup>Tc-kanamycin complexes was prepared 93 % radiochemical purities by direct labelling using 5 mg kanamycin and 30 µg SnCl2. The reaction occurred at alkaline condition (pH=9) and under room temperature for 30 min to achieve high radiochemical purity. Radiochemical purity and stability of <sup>99m</sup>Tc-kanamycin was determined by ascending paper chromatography using Whatman 3 paper as the stationary phase, and acetone as the mobile phase to separate the radiochemical impurities in the form of <sup>99m</sup>Tc-pertechnetate. While impurities in the form of <sup>99m</sup>Tc-reduced were separated using the stationary phase ITLC-SG and 0.5 N NaOH as mobile phase. This study aimed to determine biological characteristic of <sup>99m</sup>Tc-kanamycin radiopharmaceutical. In vitro cell studies showed that the change of kanamycin structure after labeling with technetium-99m did not give a specific influence to the potency of kanamycin as an antibiotic. In addition on uptake study, a significantly higher uptake of <sup>99m</sup>Tc-kanamycin with S. aureus than E. coli. Biodistribution of <sup>99m</sup>Tc-kanamycin complexes was studied on normal and infection mice at 15, 30, 60 and 120 min post-injections. The biodistribution of <sup>99m</sup>Tc-kanamycin in infection mice showed that the complex accumulated in the infection sites. These results show that <sup>99m</sup>Tc-Kanamycin radiopharmaceutical have a potential application for infection diagnosis.

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