64Cu-DOTA-SPIONs-PEG-FA：靶向叶酸受体阳性肿瘤的PET/MRI双模态显像探针

报道了-种可用于叶酸受体阳性肿瘤显像的P E T /M R I双模态显像探针（ “ Cu-DOTA-SPIONs-PEG- FA）的合成、初步的生物学评价及 P E T /C T 和 MRI 显像结果.该探针由包覆了生物相容性的聚乙二醇（ poly ethyleneglycol,PEG）、超顺磁氧化铁纳米粒子（ superparamegnetic iron oxide nanoparticles,SPIONs）、叶酸（folic acid,FA）、 1, 4, 7 , 10-四乙酸- 1, 4 , 7 , 10-四氮杂环十二烧（ 1, 4 ,7 , 10-tetraazacyclodod...

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Bibliographic Details
Published in	核化学与放射化学 Vol. 39; no. 4; pp. 298 - 308
Main Author	孙钰林申一鸣梁积新陈玉清沈浪涛
Format	Journal Article
Language	Chinese
Published	原子高科股份有限公司,北京102413%中国原子能科学研究院国家同位素工程技术研究中心,北京,102413 2017 中国原子能科学研究院国家同位素工程技术研究中心,北京102413
Subjects	DOTA,64Cu PET/MRI双模态显像探针叶酸超顺磁性氧化铁纳米粒子 superparamagnetic iron oxide nanoparticles 叶酸 DOTA 64Cu folic acid PET/MRI双模态显像探针 PET/MRI dual-modal probe 超顺磁性氧化铁纳米粒子
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ISSN	0253-9950
DOI	10.7538/hhx.2017.39.04.0298

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Summary:	报道了-种可用于叶酸受体阳性肿瘤显像的P E T /M R I双模态显像探针（ “ Cu-DOTA-SPIONs-PEG- FA）的合成、初步的生物学评价及 P E T /C T 和 MRI 显像结果.该探针由包覆了生物相容性的聚乙二醇（ poly ethyleneglycol,PEG）、超顺磁氧化铁纳米粒子（ superparamegnetic iron oxide nanoparticles,SPIONs）、叶酸（folic acid,FA）、 1, 4, 7 , 10-四乙酸- 1, 4 , 7 , 10-四氮杂环十二烧（ 1, 4 ,7 , 10-tetraazacyclododecane-l, 4, 7, 10- tetraacetic acid,DOTA）和正电子放射性核素S4C u组成.经纯化后, 64Cu-DOTA-SPIONs-PEG-FA放化纯大于 98%.荷 KB裸鼠体内分布显示严Cu-DOTA-SPIONs-PEG-FA在肝脏、脾脏和肺中的放射性摄取较高,与非靶向标记物“Cu-DOTA-SPIONs-PEG-OH比较,其对 K B细胞瘤有明显的靶向作用.在 M R I和 PE T /C T 模式下, KB肿瘤能被较清晰地显像,Cu-DOTA-SPIONs-PEG-FA作为 K B细胞肿瘤的P E T /M R I双模态显像剂,有待于进一步深入研究以改善其标记率、稳定性和比活度等.
Bibliography:	11-2045/TL PET/MRI du al-mo d al probe; su p e rp a ram ag n e t ic iro n oxide n a n o p a r t ic le s; folic acid; DOTA ; 64Cu The synthesis , pre l iminary biological evaluation and PET/CT and MRI imaging results of a potential PET/MRI dual-modal imaging tumor probe, 64Cu-DOTA-SPIONs- PEG-FA, used for targeting folate receptor-positive cancer, have been reported in this inves-tigation. This probe was composed of a superparamagnetic iron oxide nanoparticles（SPIONs） coated with the biocompatible polymer poly（ethylene glycol）（PEG） , folic acid, 1, 4, 7, 10- tetraazacyclododecane-1,4 , 7 ,l 〇 - te t ra a c e t ic acid （D O T A ） and p o s i t ro n -em i t te r copper-64：. This radioactive probe has high radiochemical purity （greater than 98%） after purification.The bio-distribution in the nude mice bearing KB cells tumor shows that 64Cu-DOTA- SPIONs-PEG-FA has a higher uptake in liver, spleen and lung, respectively, and has an obvious effect of active targeting toward the KB tumor in contrast to 64 Cu-DOTA-SPIO
ISSN:	0253-9950
DOI:	10.7538/hhx.2017.39.04.0298