Preparation and Bioevaluation of a Novel <sup>99m</sup>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. [<sup>99m</sup>Tc]Tc-CNMCHDG was prepared by a kit formulation that was straightforward to op...
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| Format: | Article |
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MDPI AG
2023-04-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/16/4/612 |
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| author | Junhong Feng Xuran Zhang Yuhao Jiang Qing Ruan Qianna Wang Junbo Zhang |
| author_facet | Junhong Feng Xuran Zhang Yuhao Jiang Qing Ruan Qianna Wang Junbo Zhang |
| author_sort | Junhong Feng |
| collection | DOAJ |
| 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. [<sup>99m</sup>Tc]Tc-CNMCHDG was prepared by a kit formulation that was straightforward to operate and fast. Without purification, [<sup>99m</sup>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 [<sup>99m</sup>Tc]Tc-CNMCHDG was significantly inhibited by pre-treatment with <i><sub>D</sub></i>-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 [<sup>99m</sup>Tc]Tc-CNMCHDG in A549 tumor-bearing mice (4.42 ± 0.36%ID/g at 120 min post-injection). Moreover, [<sup>99m</sup>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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| id | doaj.art-2d524420b8014a78a9e20bccce4f3cfc |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-11T04:38:03Z |
| publishDate | 2023-04-01 |
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| spelling | doaj.art-2d524420b8014a78a9e20bccce4f3cfc2023-11-17T20:51:22ZengMDPI AGPharmaceuticals1424-82472023-04-0116461210.3390/ph16040612Preparation and Bioevaluation of a Novel <sup>99m</sup>Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging AgentJunhong Feng0Xuran Zhang1Yuhao Jiang2Qing Ruan3Qianna Wang4Junbo Zhang5Key Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, ChinaTo 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. [<sup>99m</sup>Tc]Tc-CNMCHDG was prepared by a kit formulation that was straightforward to operate and fast. Without purification, [<sup>99m</sup>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 [<sup>99m</sup>Tc]Tc-CNMCHDG was significantly inhibited by pre-treatment with <i><sub>D</sub></i>-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 [<sup>99m</sup>Tc]Tc-CNMCHDG in A549 tumor-bearing mice (4.42 ± 0.36%ID/g at 120 min post-injection). Moreover, [<sup>99m</sup>Tc]Tc-CNMCHDG exhibited excellent tumor-to-non-target ratios and a clean imaging background and is a potential candidate for clinical transformation.https://www.mdpi.com/1424-8247/16/4/612glucose derivativecyclohexanetechnetium-99mSPECTtumor |
| spellingShingle | Junhong Feng Xuran Zhang Yuhao Jiang Qing Ruan Qianna Wang Junbo Zhang Preparation and Bioevaluation of a Novel <sup>99m</sup>Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent Pharmaceuticals glucose derivative cyclohexane technetium-99m SPECT tumor |
| title | Preparation and Bioevaluation of a Novel <sup>99m</sup>Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
| title_full | Preparation and Bioevaluation of a Novel <sup>99m</sup>Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
| title_fullStr | Preparation and Bioevaluation of a Novel <sup>99m</sup>Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
| title_full_unstemmed | Preparation and Bioevaluation of a Novel <sup>99m</sup>Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
| title_short | Preparation and Bioevaluation of a Novel <sup>99m</sup>Tc-Labeled Glucose Derivative Containing Cyclohexane as a Promising Tumor Imaging Agent |
| title_sort | preparation and bioevaluation of a novel sup 99m sup tc labeled glucose derivative containing cyclohexane as a promising tumor imaging agent |
| topic | glucose derivative cyclohexane technetium-99m SPECT tumor |
| url | https://www.mdpi.com/1424-8247/16/4/612 |
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