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Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent
To develop novel tumor imaging agents with high tumor uptake and excellent tumor/non-target ratios, a glucose derivative containing cyclohexane (CNMCHDG) was synthesized and labeled with Tc-99m. [(99m)Tc]Tc-CNMCHDG was prepared by a kit formulation that was straightforward to operate and fast. Witho...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10144323/ https://www.ncbi.nlm.nih.gov/pubmed/37111368 http://dx.doi.org/10.3390/ph16040612 |
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author | Feng, Junhong Zhang, Xuran Jiang, Yuhao Ruan, Qing Wang, Qianna Zhang, Junbo |
author_facet | Feng, Junhong Zhang, Xuran Jiang, Yuhao Ruan, Qing Wang, Qianna Zhang, Junbo |
author_sort | Feng, Junhong |
collection | PubMed |
description | To develop novel tumor imaging agents with high tumor uptake and excellent tumor/non-target ratios, a glucose derivative containing cyclohexane (CNMCHDG) was synthesized and labeled with Tc-99m. [(99m)Tc]Tc-CNMCHDG was prepared by a kit formulation that was straightforward to operate and fast. Without purification, [(99m)Tc]Tc-CNMCHDG had a high radiochemical purity of over 95% and great in vitro stability and hydrophilicity (log P = −3.65 ± 0.10). In vitro cellular uptake studies showed that the uptake of [(99m)Tc]Tc-CNMCHDG was significantly inhibited by pre-treatment with (D)-glucose and increased by pre-treatment with insulin. Preliminary cellular studies have demonstrated that the mechanism by which the complex enters into cells may be related to GLUTs. The results of biodistribution and SPECT imaging studies displayed high tumor uptake and good retention of [(99m)Tc]Tc-CNMCHDG in A549 tumor-bearing mice (4.42 ± 0.36%ID/g at 120 min post-injection). Moreover, [(99m)Tc]Tc-CNMCHDG exhibited excellent tumor-to-non-target ratios and a clean imaging background and is a potential candidate for clinical transformation. |
format | Online Article Text |
id | pubmed-10144323 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-101443232023-04-29 Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent Feng, Junhong Zhang, Xuran Jiang, Yuhao Ruan, Qing Wang, Qianna Zhang, Junbo Pharmaceuticals (Basel) Article To develop novel tumor imaging agents with high tumor uptake and excellent tumor/non-target ratios, a glucose derivative containing cyclohexane (CNMCHDG) was synthesized and labeled with Tc-99m. [(99m)Tc]Tc-CNMCHDG was prepared by a kit formulation that was straightforward to operate and fast. Without purification, [(99m)Tc]Tc-CNMCHDG had a high radiochemical purity of over 95% and great in vitro stability and hydrophilicity (log P = −3.65 ± 0.10). In vitro cellular uptake studies showed that the uptake of [(99m)Tc]Tc-CNMCHDG was significantly inhibited by pre-treatment with (D)-glucose and increased by pre-treatment with insulin. Preliminary cellular studies have demonstrated that the mechanism by which the complex enters into cells may be related to GLUTs. The results of biodistribution and SPECT imaging studies displayed high tumor uptake and good retention of [(99m)Tc]Tc-CNMCHDG in A549 tumor-bearing mice (4.42 ± 0.36%ID/g at 120 min post-injection). Moreover, [(99m)Tc]Tc-CNMCHDG exhibited excellent tumor-to-non-target ratios and a clean imaging background and is a potential candidate for clinical transformation. MDPI 2023-04-18 /pmc/articles/PMC10144323/ /pubmed/37111368 http://dx.doi.org/10.3390/ph16040612 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Feng, Junhong Zhang, Xuran Jiang, Yuhao Ruan, Qing Wang, Qianna Zhang, Junbo Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
title | Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
title_full | Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
title_fullStr | Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
title_full_unstemmed | Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
title_short | Preparation and Bioevaluation of a Novel (99m)Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
title_sort | preparation and bioevaluation of a novel (99m)tc-labeled glucose derivative containing cyclohexane as a promising tumor imaging agent |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10144323/ https://www.ncbi.nlm.nih.gov/pubmed/37111368 http://dx.doi.org/10.3390/ph16040612 |
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