Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors

In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA complexes, which exhibited high radiochemical purity (>95%...

Full description

Bibliographic Details
Main Authors:	Junhong Feng, Xuran Zhang, Qing Ruan, Yuhao Jiang, Junbo Zhang
Format:	Article
Language:	English
Published:	MDPI AG 2021-07-01
Series:	Molecules
Subjects:	<sup>99m</sup>Tc isonitrile folate receptor SPECT/CT imaging
Online Access:	https://www.mdpi.com/1420-3049/26/15/4552

id	doaj-965657a67cec4b0d8b73d56183076cc1
record_format	Article
spelling	doaj-965657a67cec4b0d8b73d56183076cc12021-08-06T15:29:07ZengMDPI AGMolecules1420-30492021-07-01264552455210.3390/molecules26154552Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate ReceptorsJunhong Feng0Xuran Zhang1Qing Ruan2Yuhao Jiang3Junbo Zhang4Key Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, ChinaKey Laboratory of Radiopharmaceuticals of Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, ChinaIn order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA complexes, which exhibited high radiochemical purity (>95%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA had specific tumor uptake. Compared with [<sup>99m</sup>Tc]Tc-CN5FA, the tumor/muscle ratios of [<sup>99m</sup>Tc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two <sup>99m</sup>Tc complexes have potential as tumor imaging agents to target folate receptors.https://www.mdpi.com/1420-3049/26/15/4552<sup>99m</sup>Tcisonitrilefolate receptorSPECT/CT imaging
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Junhong Feng Xuran Zhang Qing Ruan Yuhao Jiang Junbo Zhang
spellingShingle	Junhong Feng Xuran Zhang Qing Ruan Yuhao Jiang Junbo Zhang Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors Molecules <sup>99m</sup>Tc isonitrile folate receptor SPECT/CT imaging
author_facet	Junhong Feng Xuran Zhang Qing Ruan Yuhao Jiang Junbo Zhang
author_sort	Junhong Feng
title	Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors
title_short	Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors
title_full	Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors
title_fullStr	Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors
title_full_unstemmed	Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors
title_sort	preparation and evaluation of novel folate isonitrile <sup>99m</sup>tc complexes as potential tumor imaging agents to target folate receptors
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2021-07-01
description	In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA complexes, which exhibited high radiochemical purity (>95%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [<sup>99m</sup>Tc]Tc-CN5FA and [<sup>99m</sup>Tc]Tc-CNPFA had specific tumor uptake. Compared with [<sup>99m</sup>Tc]Tc-CN5FA, the tumor/muscle ratios of [<sup>99m</sup>Tc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two <sup>99m</sup>Tc complexes have potential as tumor imaging agents to target folate receptors.
topic	<sup>99m</sup>Tc isonitrile folate receptor SPECT/CT imaging
url	https://www.mdpi.com/1420-3049/26/15/4552
work_keys_str_mv	AT junhongfeng preparationandevaluationofnovelfolateisonitrilesup99msuptccomplexesaspotentialtumorimagingagentstotargetfolatereceptors AT xuranzhang preparationandevaluationofnovelfolateisonitrilesup99msuptccomplexesaspotentialtumorimagingagentstotargetfolatereceptors AT qingruan preparationandevaluationofnovelfolateisonitrilesup99msuptccomplexesaspotentialtumorimagingagentstotargetfolatereceptors AT yuhaojiang preparationandevaluationofnovelfolateisonitrilesup99msuptccomplexesaspotentialtumorimagingagentstotargetfolatereceptors AT junbozhang preparationandevaluationofnovelfolateisonitrilesup99msuptccomplexesaspotentialtumorimagingagentstotargetfolatereceptors
_version_	1721217823799246848

Preparation and Evaluation of Novel Folate Isonitrile <sup>99m</sup>Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors

Similar Items