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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...

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Detalles Bibliográficos
Autores principales: Feng, Junhong, Zhang, Xuran, Jiang, Yuhao, Ruan, Qing, Wang, Qianna, Zhang, Junbo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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.
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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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