Department of Biomedical Engineering, School of Life Science and Technology, China Pharmaceutical University, Nanjing, People's Republic of China.
Mol Imaging Biol. 2010 Dec;12(6):595-607. doi: 10.1007/s11307-010-0305-1.
The purpose of this study is to synthesize a folate-polyethylene glycol (PEG) conjugated near-infrared fluorescence probe (fPI-01) for diagnosis of folate receptor (FR)-overexpressed tumors with high sensitivity and specificity.
fPI-01 was synthesized, purified, and characterized. Its cytotoxicity and affinity to tumor cells were determined in vitro. The dynamics and biodistribution of the probe was monitored in normal nude mice. And the tumor-targeting capability was investigated in nude mice bearing different tumor xenograft.
fPI-01 was successfully synthesized with strengthened optical properties. Cells experiments showed the probe had high FR affinity and without apparent cytotoxicity. Animal experiments indicated the probe excreted through urine by kidney. And its tumor-targeting ability was demonstrated on different tumor-bearing mice, with high sensitivity and tumor-to-normal tissue contrast ratio (10:1).
fPI-01 is a promising optical agent for diagnosis of FR-positive tumors, especially in their early stage.
本研究旨在合成一种叶酸-聚乙二醇（PEG）偶联近红外荧光探针（fPI-01），用于高灵敏度和特异性诊断叶酸受体（FR）过表达的肿瘤。
合成、纯化和表征 fPI-01。在体外测定其细胞毒性和对肿瘤细胞的亲和力。监测探针在正常裸鼠体内的动力学和生物分布。并在携带不同肿瘤异种移植物的裸鼠中研究其肿瘤靶向能力。
成功合成了具有增强光学性质的 fPI-01。细胞实验表明，该探针具有高 FR 亲和力，且无明显细胞毒性。动物实验表明，探针通过肾脏经尿液排泄。并且在不同的荷瘤小鼠中证明了其肿瘤靶向能力，具有高灵敏度和肿瘤与正常组织的对比率（10:1）。
fPI-01 是一种很有前途的 FR 阳性肿瘤诊断光学试剂，特别是在早期阶段。
