Preparation and Evaluation of Novel Folate Isonitrile (99m)Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors.
Preparation and Evaluation of Novel Folate Isonitrile (99m)Tc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors.
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新型叶酸异腈 99mTc 复合物作为靶向叶酸受体的潜在肿瘤显像剂的制备和评价
DOI:
10.3390/molecules26154552
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发表时间:
2021-07-28
期刊:
影响因子:
--
通讯作者:
Zhang J
中科院分区:
文献类型:
--
作者:
Feng J;Zhang X;Ruan Q;Jiang Y;Zhang J
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%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specific tumor uptake. Compared with [99mTc]Tc-CN5FA, the tumor/muscle ratios of [99mTc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two 99mTc complexes have potential as tumor imaging agents to target folate receptors.
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