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Title: Study of potential utility of new radiopharmaceuticals based on technetium-99m labeled derivative of glucose

Abstract

Purpose: to study the potential utility of 1-thio-D-glucose labeled with {sup 99m}Tc for cancer imaging in laboratory animals. Materials and method: the study was carried out in cell cultures of normal CHO (Chinese hamster ovary cells CHO) and malignant tissues MCF-7 (human breast adenocarcinoma MCF-7). To evaluate the uptake of {sup 99m}Tc-1-thio-D-glucose in normal and tumor tissue cells, 25 MBq of 1-thio-D-glucose labeled with {sup 99m}Tc was added to the vials with 3 million cells and incubated for 30 min at room temperature. After centrifugation of the vials with cells, the supernatant was removed. The radioactivity in vials with normal and tumor cells was then measured. In addition, the study included 40 mice of C57B1/6j lines with tumor lesion of the right femur. For neoplastic lesions, Lewis lung carcinoma model was used. Following anesthesia, mice were injected intravenously with 25 MBq of {sup 99m}Tc-1-thio-D-glucose. Planar scintigraphy was performed 15 minutes later in a matrix of 512x512 pixels for 5 min. Results: when measuring the radioactivity of normal and malignant cells after incubation with {sup 99m}Tc-1-thio-D-glucose, it was found that the radioactivity of malignant cells was higher than that of normal cells. The mean values of radioactivity levels in normal andmore » malignant cells were 0.3 ± 0.15 MBq and 1.07 ± 0.6 MBq, respectively. All examined animals had increased accumulation of {sup 99m}Tc-1-thio-D-glucose at the tumor site. The accumulation of {sup 99m}Tc-1-thio-D-glucose in the tumor was on average twice as high as compared to the symmetric region. Conclusion: The present study demonstrated that {sup 99m}Tc-1-thio-D-glucose is a prospective radiopharmaceutical for cancer visualization. In addition, high accumulation of {sup 99m}Tc-1-thio-D-glucose in the culture of cancer cells and in tumor tissue of animals demonstrates tumor tropism of the radiopharmaceutical.« less

Authors:
; ; ;  [1];  [2]; ; ; ; ;  [3]
  1. Tomsk Cancer Research Institute, Tomsk, 634050 (Russian Federation)
  2. (Russian Federation)
  3. Tomsk Polytechnic University, Tomsk, 634050 (Russian Federation)
Publication Date:
OSTI Identifier:
22608296
Resource Type:
Journal Article
Resource Relation:
Journal Name: AIP Conference Proceedings; Journal Volume: 1760; Journal Issue: 1; Conference: PC'16: International conference on physics of cancer: Interdisciplinary problems and clinical applications 2016, Tomsk (Russian Federation), 22-25 Mar 2016; Other Information: (c) 2016 Author(s); Country of input: International Atomic Energy Agency (IAEA)
Country of Publication:
United States
Language:
English
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; ANESTHESIA; ANIMAL TISSUES; BIOMEDICAL RADIOGRAPHY; CARCINOMAS; CELL CULTURES; CENTRIFUGATION; CHO CELLS; COMPARATIVE EVALUATIONS; FEMUR; GLUCOSE; LABORATORY ANIMALS; LUNGS; MAMMARY GLANDS; OVARIES; RADIOACTIVITY; RADIOPHARMACEUTICALS; SCINTISCANNING; TECHNETIUM 99; TUMOR CELLS

Citation Formats

Zeltchan, R., E-mail: r.zelchan@yandex.ru, Medvedeva, A., Sinilkin, I., Chernov, V., Tomsk Polytechnic University, Tomsk, 634050, Stasyuk, E., Rogov, A., Il’ina, E., Larionova, L., and Skuridin, V. Study of potential utility of new radiopharmaceuticals based on technetium-99m labeled derivative of glucose. United States: N. p., 2016. Web. doi:10.1063/1.4960291.
Zeltchan, R., E-mail: r.zelchan@yandex.ru, Medvedeva, A., Sinilkin, I., Chernov, V., Tomsk Polytechnic University, Tomsk, 634050, Stasyuk, E., Rogov, A., Il’ina, E., Larionova, L., & Skuridin, V. Study of potential utility of new radiopharmaceuticals based on technetium-99m labeled derivative of glucose. United States. doi:10.1063/1.4960291.
Zeltchan, R., E-mail: r.zelchan@yandex.ru, Medvedeva, A., Sinilkin, I., Chernov, V., Tomsk Polytechnic University, Tomsk, 634050, Stasyuk, E., Rogov, A., Il’ina, E., Larionova, L., and Skuridin, V. 2016. "Study of potential utility of new radiopharmaceuticals based on technetium-99m labeled derivative of glucose". United States. doi:10.1063/1.4960291.
@article{osti_22608296,
title = {Study of potential utility of new radiopharmaceuticals based on technetium-99m labeled derivative of glucose},
author = {Zeltchan, R., E-mail: r.zelchan@yandex.ru and Medvedeva, A. and Sinilkin, I. and Chernov, V. and Tomsk Polytechnic University, Tomsk, 634050 and Stasyuk, E. and Rogov, A. and Il’ina, E. and Larionova, L. and Skuridin, V.},
abstractNote = {Purpose: to study the potential utility of 1-thio-D-glucose labeled with {sup 99m}Tc for cancer imaging in laboratory animals. Materials and method: the study was carried out in cell cultures of normal CHO (Chinese hamster ovary cells CHO) and malignant tissues MCF-7 (human breast adenocarcinoma MCF-7). To evaluate the uptake of {sup 99m}Tc-1-thio-D-glucose in normal and tumor tissue cells, 25 MBq of 1-thio-D-glucose labeled with {sup 99m}Tc was added to the vials with 3 million cells and incubated for 30 min at room temperature. After centrifugation of the vials with cells, the supernatant was removed. The radioactivity in vials with normal and tumor cells was then measured. In addition, the study included 40 mice of C57B1/6j lines with tumor lesion of the right femur. For neoplastic lesions, Lewis lung carcinoma model was used. Following anesthesia, mice were injected intravenously with 25 MBq of {sup 99m}Tc-1-thio-D-glucose. Planar scintigraphy was performed 15 minutes later in a matrix of 512x512 pixels for 5 min. Results: when measuring the radioactivity of normal and malignant cells after incubation with {sup 99m}Tc-1-thio-D-glucose, it was found that the radioactivity of malignant cells was higher than that of normal cells. The mean values of radioactivity levels in normal and malignant cells were 0.3 ± 0.15 MBq and 1.07 ± 0.6 MBq, respectively. All examined animals had increased accumulation of {sup 99m}Tc-1-thio-D-glucose at the tumor site. The accumulation of {sup 99m}Tc-1-thio-D-glucose in the tumor was on average twice as high as compared to the symmetric region. Conclusion: The present study demonstrated that {sup 99m}Tc-1-thio-D-glucose is a prospective radiopharmaceutical for cancer visualization. In addition, high accumulation of {sup 99m}Tc-1-thio-D-glucose in the culture of cancer cells and in tumor tissue of animals demonstrates tumor tropism of the radiopharmaceutical.},
doi = {10.1063/1.4960291},
journal = {AIP Conference Proceedings},
number = 1,
volume = 1760,
place = {United States},
year = 2016,
month = 8
}
  • /sup 18/F-2-Deoxy-2-fluoro-D-glucose (/sup 18/FDG) is rapidly extracted by the mouse heart, and the radioactivity in heart (3 to 4% per organ) remains relatively constant for 2 hr post injection. The brain uptake (2 to 3% per organ) remained relatively constant throughout the time course of the study. Liver, lungs, kidneys, small intestine, and blood all showed a rapid clearance of radioactivity after injection of /sup 18/FDG. At 120 min the heart-to-lung ratio was 12 and heart-to-liver ratio was 32. Urinary excretion of activity was approximately 16% of the injected dose at 60 min. The uptake of radioactivity by dog heartmore » following the intravenous administration of /sup 18/FDG was 2.8 to 4.1% at 60 min and 2.4% at 135 min; it was regionally distributed, the areas of highest activity being the left ventricle and the interventricular septum. The brain activity was 2.1 to 3.5% at 120 min, with a ratio of gray matter-to-white matter of 2 to 3:1. Urinary excretion in dogs was 16% and 50% of the injected dose at 60 and 135 min. The chemical form of the activity in the urine, although unidentified, was not /sup 18/F/sup -/. Cross-sectional images of the mycardium of the dog after intravenous injection of /sup 18/FDG were obtained using emission tomography.« less
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