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叶酸受体肿瘤显像剂99 Tcm-(HYNIC-NHHN-FA)(EDDA)的制备及生物性能评价

Preparation and biological evaluation of radiolabeled folate receptor-positive tumor agent 99 Tcm-(HYNIC-NHHN-FA) (EDDA)

摘要:

目的制备99 Tcm 标记的FR靶向肿瘤分子探针99 Tcm?( HYNIC?NHHN?FA)( EDDA),并评价其生物性能。方法合成FA衍生物配体FA?NHHN?HYNIC,以EDDA作为共配体进行99 Tcm标记,经HPLC纯化后,测定其放化纯、脂水分配系数和体外稳定性,选用FR高表达的人口腔表皮样癌KB细胞进行体外细胞结合实验,研究其在正常小鼠体内的生物分布及荷KB肿瘤裸鼠SPECT/CT显像。结果标记配合物经HPLC纯化后放化纯大于95%,在生理盐水和小鼠血清中稳定性良好,可与FR高表达的KB细胞特异性结合,温育1 h后细胞总结合率可达(6.76±0.60)%,加入过量FA后摄取率降低至(0.24±0.02)%;正常小鼠体内生物分布显示其仅在FR高表达的肾脏有高放射性浓聚,给药后0.5 h肾脏摄取达(21.79±9.79)%ID/g。小动物SPECT/CT显像肿瘤部位清晰可见,且能被过量FA明显抑制。结论标记物99 Tcm?( HYNIC?NHHN?FA)( EDDA)是一种性能良好的FR靶向肿瘤分子探针。

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abstracts:

Objective To prepare a novel radiolabeled FR?positive tumor targeting agent 99 Tcm?( HYNIC?NHHN?FA) ( EDDA) and evaluate its biological properties. Methods FA derivative FA?NHHN?HYNIC was synthesized and radiolabeled with 99 Tcm using EDDA as a coligand. The radiochemical purity, octanal/water partition coefficient and in vitro stabilities of the complex were studied after purified by HPLC. In vitro cellular uptakes were performed on FR?positive KB cells ( human oral epidermoid carcinoma cells) . Biodistribution and microSPECT/CT imaging were investigated on normal Kunming mice and nude mice bearing KB tumors, respectively. Results The radiochemical purity of the complex was over 95% after pu?rified by HPLC. It displayed high stability both in saline and in serum. It also exhibited high specific FR binding in FR?positive KB cells in vitro. The binding ratio was (6.76±0.60)%1 h after incubation, and de?creased to (0.24±0.02)% after adding excessive FA. The results of biodistribution showed high kidney up?take in normal mice, and the uptake reached (21.79±9.79) %ID/g 0.5 h after injection. Flank KB tumors were clearly visualized with 99 Tcm?( HYNIC?NHHN?FA ) ( EDDA ) by microSPECT/CT imaging at 2 h postinjection, and the uptake could be inhibited by excessive FA. Conclusions 99 Tcm?( HYNIC?NHHN?FA) ( EDDA) exhibits good pharmacokinetic properties, suggesting its potential as a promising FA targeting agent for tumor imaging.

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