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^99mTc标记蝶呤-赖氨酸衍生物的制备及生物性能评价

Preparation and Biological Evaluation of ^99mTc-labeled Pteroyl-lys Derivatives

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【Author】 YU Qian;HE Yingfang;CHEN Yuan;YANG Wenjiang;ZHANG Chun;LU Jie;Key Laboratory of Radiopharmaceuticals(Beijing Normal University) ,Ministry of Education,College of Chemistry,Beijing Normal University;Key Laboratory of Nuclear Radiation and Nuclear Energy Technology,Institute of High Energy Physics,China Academy of Sciences;Department of Nuclear Medicine,Beijing Chao-Yang Hospital,Capital Medical University;

【机构】北京师范大学化学学院放射性药物教育部重点实验室；中国科学院高能物理研究所核辐射与核能技术重点实验室；首都医科大学北京朝阳医院核医学科；

【摘要】基于蝶呤-赖氨酸分子结构,设计合成了2种^99mTc标记配合物^99mTc（HYNIC-penta-lys-Pteroyl）-（Tricine/TPPTS）和^99mTc（HYNIC-Gly-Gly-lys-Pteroyl）（Tricine/TPPTS）,并对其生物性能进行了初步评价.研究结果表明,2种配合物在叶酸受体高表达的人口腔表皮样癌（KB）细胞中均有很高的摄取和滞留.给药1 h后,^99mTc（HYNIC-penta-lys-Pteroyl）（Tricine/TPPTS）和^99mTc（HYNIC-Gly-Gly-lys-Pteroyl）（Tricine/TPPTS）在荷KB肿瘤裸鼠体内的肿瘤摄取率分别为（8.55±2.78）%ID/g和（9.77±1.54）%ID/g.荷KB肿瘤裸鼠的小动物SPECT/CT显像研究结果表明,上述2种标记配合物在给药2 h后,其肿瘤部位均清晰可见,有望作为新型的叶酸受体靶向肿瘤分子探针.更多还原

【Abstract】 Two ^99mTc labeled complexes,^99mTc（ HYNIC-penta-lys-Pteroyl）（ Tricine/TPPTS） and^99mTc-（ HYNIC-Gly-Gly-lys-Pteroyl）（ Tricine/TPPTS）,were prepared based on the structure of Pteroyl-lys.Both two complexes exhibited high receptor specific binding and extended retention in KB human epidermoid carcinoma cells. The tumor uptake values of^99mTc（ HYNIC-penta-lys-Pteroyl）（ Tricine/TPPTS） and^99mTc（ HYNIC-Gly-Gly-lys-Pteroyl）（ Tricine/TPPTS） were（ 8. 55 ± 2. 78） % ID/g and（ 9. 77 ± 1. 54） % ID/g at 1 h postinjection,respectively. Flank KB tumors were clearly visualized with^99mTc（ HYNIC-penta-lysPteroyl）（ Tricine/TPPTS） and^99mTc（ HYNIC-Gly-Gly-lys-Pteroyl）（ Tricine/TPPTS） by Micro-SPECT/CT images at 2 h postinjection. High receptor-specific tumor uptakes coupled with fast non-target tissues clearance demonstrated the feasibility of using^99mTc-labeled Pteroyl-lys derivatives as novel imaging probes for FR-positive tumors detection.更多还原