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Novel Tc-99m radiolabeled folate complexes with PEG linkers for FR-positive tumor imaging: synthesis and biological evaluation
Xie, F; Zhang, C; Yu, Q; Pang, Y; Chen, Y; Yang, WJ; Xue, JQ; Liu, Y; Lu, J;杨文江; Xue JQ(薛井泉); 刘宇(多)
2014
发表期刊RSC ADVANCES
卷号4期号:61页码:32197-32206
摘要In order to develop a novel Tc-99m-labeled folate based SPECT radiotracer with an optimized pharmacokinetic profile for the folate receptor (FR) positive tumor imaging, a folate conjugate, HYNIC-PEG2-FA, was designed, synthesized and radiolabeled with Tc-99m using tricine/diphenylphosphinobenzene-3-sulfonic acid sodium (TPPMS), tricine/trisodium triphenylphosphine-3,3',3 ''-trisulfonate (TPPTS), and ethylenediamine-N,N'-diacetic acid (EDDA) as coligands. Tc-99m(HYNIC-PEG2-FA)(tricine/TPPTS), 4, Tc-99m(HYNIC-PEG2-FA)(tricine/TPPMS), 5 and Tc-99m(HYNIC-PEG2-FA)(EDDA), 6, were obtained respectively. All of them were stable in saline and mouse plasma for 6 h, and displayed high specific binding in the FR-positive KB cell line in vitro. Among them, complex 4 exhibited a higher tumor uptake (11.35 +/- 0.67 ID% g(-1) at 2 h p.i.) and more rapid clearance from the liver, lungs, blood, muscle and other non-target organs than Tc-99m (HYNIC-NHHN-FA)(tricine/TPPTS), which we reported before. Small animal SPECT/CT imaging studies in FR-positive KB tumor models showed that the tumor could be clearly visualized at 120 min p.i., suggesting its potential as a promising folate receptor targeting agent for tumor imaging.
学科领域Chemistry
DOI10.1039/c4ra03564j
收录类别SCI
WOS记录号WOS:000340427600020
引用统计
被引频次:4[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.ihep.ac.cn/handle/311005/225349
专题核技术应用研究中心
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GB/T 7714
Xie, F,Zhang, C,Yu, Q,et al. Novel Tc-99m radiolabeled folate complexes with PEG linkers for FR-positive tumor imaging: synthesis and biological evaluation[J]. RSC ADVANCES,2014,4(61):32197-32206.
APA Xie, F.,Zhang, C.,Yu, Q.,Pang, Y.,Chen, Y.,...&刘宇.(2014).Novel Tc-99m radiolabeled folate complexes with PEG linkers for FR-positive tumor imaging: synthesis and biological evaluation.RSC ADVANCES,4(61),32197-32206.
MLA Xie, F,et al."Novel Tc-99m radiolabeled folate complexes with PEG linkers for FR-positive tumor imaging: synthesis and biological evaluation".RSC ADVANCES 4.61(2014):32197-32206.
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