Comparison of three 18F-labeled carboxylic acids with 18F-FDG of the differentiation tumor from inflammation in model mice

Wang, Hongliang; Tang, Ganghua; Hu, Kongzhen; Huang, Tingting; Xiang, Lei; Wu, Zhiyong; Li, Sijin

doi:10.1186/s12880-016-0110-7

Cited by 10 publications

(5 citation statements)

References 32 publications

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“…Albeit we showed a substantial tumor uptake in vivo with tumor-to-muscle ratio of up to four times for 1-TG (at 4h after injection), the uptake was less pronounced for 1-TG and 5-TG compared with 18 F-FDG for which previous studies using similar cell lines revealed tumor-to-muscle-ratios of 6:1 to 13:1 (15,16). This is in line with our in vitro work and could be a result of lower a nity of 1-TG and 5-TG to GLUT channels as compared to 18 F-FDG.…”

Section: Discussioncontrasting

confidence: 56%

Evaluation of tumor uptake and bio-distribution of 99mTc-labeled 1-thio-β-D-glucose and 5-thio-D-glucose in vivo

Muehlberg,

Mohnike,

Grosser

et al. 2024

Preprint

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Background To investigate the capacity of 99mTc-labeled 1-thio-β-D-glucose (1-TG) and 5-thio-D-glucose (5-TG) to act as a marker for glucose consumption in tumor cells in vivo as well as to evaluate the biodistribution of 1-TG and 5-TG. We investigated the biodistribution, including tumor uptake, of 1-TG and 5-TG at various time points after injection (0.5, 2 and 4 h) in human colorectal carcinoma and human lung adenocarcinoma (HCT-116, A549) xenograft bearing nude mice (N=4 per tracer and time point). Results: In vivo biodistribution studies revealed a maximum tumor-to-muscle ratio of 4.22 ± 2.7 and 2.2 ± 1.3 (HCT-116) and of 3.2 ± 1.1 and 4.1 ± 1.3 (A549) for 1-TG and 5-TG, respectively, with a peak at 4 hours for 1-TG and 5-TG. Biodistribution revealed a high uptake in kidneys and liver for 1-TG and in the lung, liver, and kidneys for 5-TG. Conclusions: 1-TG and 5-TG showed an insufficient tumor uptake for diagnostic use in human colorectal carcinoma and human lung adenocarcinoma xenograft model.

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Section: Discussioncontrasting

confidence: 56%

Evaluation of tumor uptake and bio-distribution of 99mTc-labeled 1-thio-β-D-glucose and 5-thio-D-glucose in vivo

Muehlberg,

Mohnike,

Grosser

et al. 2024

Preprint

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“…It has been reported that 2-[ 18 F]FPA accumulated in prostate cancers with high tumor to background ratios, and it may be useful in the clinical diagnosis of prostate cancer in humans. In general, 18 F labeled fluoro-alkyl fatty acids displayed tumor uptakes. The mechanism(s) of uptake and their relationship with hypoxia conditions has not been reported, although 2-[ 18 F]FPA did not showed preference for in vitro tumor cell uptake under hypoxia condition (Figure D).…”

Section: Results and Discussionmentioning

confidence: 99%

In Vivo Ester Hydrolysis as a New Approach in Development of Positron Emission Tomography Tracers for Imaging Hypoxia

et al. 2019

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Hypoxia is an important biochemical and physiological condition associated with uncontrolled growth of tumor. Measurement of hypoxia in tumor tissue may be useful in characterization of tumor progression and monitoring drug treatment.[ 18 F]FMISO is the most widely employed radiotracer for imaging of hypoxic tissue with positron emission tomography (PET). However, it showed relatively low uptake in hypoxic tissues, which led to low target-to-background contrast in PET images. To overcome these shortcomings, two novel 2-fluoroproprioic acid esters, nitroimidazole derivatives 2-fluoropropionic acid 2-(2nitro-imidazol-1-yl)-ethyl ester (FNPFT, [ 19 F]5) and 2-fluoropropionic acid 2-(2-methyl-5-nitro-imidazol-1-yl)-ethyl ester (FMNPFT, [ 19 F]8), were prepared and tested. Radiolabeling of [ 18 F]5 and [ 18 F]8 was accomplished in 45 min (radiochemical purity >95%, the decay-corrected radiochemical yield of [ 18 F]5 was 11 ± 2%, and that of [ 18 F]8 was 13 ± 2%, n = 5). In vitro cell uptake studies using EMT-6 tumor cells showed that both radiotracers [ 18 F]5 and [ 18 F]8 displayed significantly higher uptake in hypoxic cells than those under normoxic condition, while 2-[ 18 F]fluoropropionic acid (2-[ 18 F]FPA) displayed no difference. Biodistribution studies in mice bearing EMT-6 tumor showed that [ 18 F]5, [ 18 F]8, and 2-[ 18 F]FPA displayed similar tumor and major organ uptakes. Tumor uptake values for all three agents were higher than those of [ 18 F]FMISO, respectively (P < 0.05). This is likely due to a rapid in vivo hydrolysis of [ 18 F]5 and [ 18 F]8 to their metabolite, 2-[ 18 F]FPA. Micro PET imaging studies in the same EMT-6 implanted mice tumor model also demonstrated that both [ 18 F]5 and [ 18 F]8 displayed similar tumor uptake comparable to that of 2-[ 18 F]FPA. In conclusion, two new fluorine-18 labeled nitroimidazole derivatives, [ 18 F]5 and [ 18 F]8, showed good tumor uptakes in mice bearing EMT-6 tumor. However, in vivo biodistribution results suggested that they were more likely reflect the predominance of in vivo produced metabolite, 2-[ 18 F]FPA, which may not be related to tumor hypoxic condition.

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“…However, most of these changes in F-AgÅPs + panipenem co-treatment group were much more obvious than that of mice treated with F-AgÅPs or panipenem alone ( Figure 6 F-H and Figure S2 A-D ). 18F-fluorodeoxyglucose (18F-FDG) is a radiotracer that is used to measure the glycolytic activity and a higher level of 18F-FDG uptake is demonstrated in inflammatory lesions 24 , 25 . Whole body imaging with 18F-FDG-PET/CT further confirmed that the combination of F-AgÅPs and panipenem caused a greater inhibition of inflammation in the E. coli -infected mice, as indicated by the trend of lower level of 18F-FDG uptake in F-AgÅPs + panipenem group compared to F-AgÅPs or panipenem group ( Figure 6 , I and J ).…”

Section: Resultsmentioning

confidence: 99%

Fructose-coated Ångstrom silver prevents sepsis by killing bacteria and attenuating bacterial toxin-induced injuries

Yin¹,

Zhou²,

Chen³

et al. 2021

Theranostics

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Serious infection caused by multi-drug-resistant bacteria is a major threat to human health. Bacteria can invade the host tissue and produce various toxins to damage or kill host cells, which may induce life-threatening sepsis. Here, we aimed to explore whether fructose-coated Ångstrom-scale silver particles (F-AgÅPs), which were prepared by our self-developed evaporation-condensation system and optimized coating approach, could kill bacteria and sequester bacterial toxins to attenuate fatal bacterial infections. Methods: A series of in vitro assays were conducted to test the anti-bacterial efficacy of F-AgÅPs, and to investigate whether F-AgÅPs could protect against multi-drug resistant Staphylococcus aureus ( S. aureus )- and Escherichia coli ( E. coli )-induced cell death, and suppress their toxins ( S. aureus hemolysin and E. coli lipopolysaccharide)-induced cell injury or inflammation. The mouse models of cecal ligation and puncture (CLP)- or E. coli bloodstream infection-induced lethal sepsis were established to assess whether the intravenous administration of F-AgÅPs could decrease bacterial burden, inhibit inflammation, and improve the survival rates of mice. The levels of silver in urine and feces of mice were examined to evaluate the excretion of F-AgÅPs. Results: F-AgÅPs efficiently killed various bacteria that can cause lethal infections and also competed with host cells to bind with S. aureus α-hemolysin, thus blocking its cytotoxic activity. F-AgÅPs inhibited E. coli lipopolysaccharide-induced endothelial injury and macrophage inflammation, but not by directly binding to lipopolysaccharide. F-AgÅPs potently reduced bacterial burden, reversed dysregulated inflammation, and enhanced survival in mice with CLP- or E. coli bloodstream infection-induced sepsis, either alone or combined with antibiotic therapy. After three times injections within 48 h, 79.18% of F-AgÅPs were excreted via feces at the end of the 14-day observation period. Conclusion: This study suggests the prospect of F-AgÅPs as a promising intravenous agent for treating severe bacterial infections.

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Comparison of three 18F-labeled carboxylic acids with 18F-FDG of the differentiation tumor from inflammation in model mice

Abstract: Background: The aim of this study was to compare the properties and feasibility of the glucose analog, 2-18

Cited by 10 publications

References 32 publications

Evaluation of tumor uptake and bio-distribution of 99mTc-labeled 1-thio-β-D-glucose and 5-thio-D-glucose in vivo

Evaluation of tumor uptake and bio-distribution of 99mTc-labeled 1-thio-β-D-glucose and 5-thio-D-glucose in vivo

In Vivo Ester Hydrolysis as a New Approach in Development of Positron Emission Tomography Tracers for Imaging Hypoxia

Fructose-coated Ångstrom silver prevents sepsis by killing bacteria and attenuating bacterial toxin-induced injuries

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