新型核素分子探针^(18)F-NT靶向前列腺癌的实验研究  

Experimental study of a novel radionuclide molecular probe ^(18)F-NT targeting prostate cancer

作　　者：邹开力 唐永祥[1] 周明[1] 李建[1] 胡硕[1] Kai-li Zou;Yong-xiang Tang;Ming Zhou;Jian Li;Shuo Hu(PET-CT Center, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China)

机构地区：[1]中南大学湘雅医院PE中心,湖南长沙410008

出　　处：《中国现代医学杂志》2018年第16期17-21,共5页China Journal of Modern Medicine

摘　　要：目的探讨新型核素分子探针^(18)F-NT在前列腺癌细胞及荷瘤小鼠的靶向性,为后续^(18)F-NT靶向前列腺癌的在体显像提供实验依据。方法制备^(18)F-NT,并完成质量控制检测。选取高表达神经降压素受体1(NTR1)的人前列腺癌细胞系PC3,分3组进行细胞结合实验,分别为实验组、阻断组和对照组(游离^(18)F离子)。对照组在细胞中加入游离^(18)F离子,实验组在细胞中加^(18)F-NT,阻断组细胞中加入^(18)F-NT前30 min加入神经降压素(NT)进行阻断。复制荷PC3前列腺癌裸鼠模型,分为实验组和阻断组,每组3只。阻断组单次尾静脉注射NT 0.2 ml(浓度为1 mg/ml);实验组注射0.2 ml生理盐水,30 min后两组裸鼠尾静脉分别注射37 MBq/ml的^(18)F-NT 0.2 ml,1 h后处死裸鼠,分离主要脏器及肿瘤组织,γ计数器测量各脏器组织的放射性计数。分析两组肿瘤细胞的放射性计数及肿瘤组织的放射性摄取值(%ID/g)。结果成功制备^(18)F-NT,其理化性质及各项质控指标均达标。细胞结合实验显示,PC3细胞实验组计数值(5 825.00±1 074.52)/min,高于阻断组(1 941.66±173.58)/min,两者比较,差异有统计学意义(t=7.227,P=0.003),而对照组计数值仅为(170.33±56.59)/min;两组荷瘤裸鼠体内生物学分布实验表明,^(18)F-NT血液清除较快,主要经肾脏代谢。实验组肿瘤摄取值最高,为(1.02±0.49)%ID/g,阻断组肿瘤摄取值降低,为(0.21±0.03)%ID/g,两者比较,差异有统计学意义(t=2.815,P=0.049)。结论^(18)F-NT标记率和放化纯高,体外稳定性好,前列腺癌细胞系PC3结合^(18)F-NT高,PC3荷瘤裸鼠的肿瘤摄取^(18)F-NT高,细胞和荷瘤均能被NT有效阻断,为后续^(18)F-NT靶向前列腺癌NTR1在体显像打下良好的实验基础。Objective To investigate the targeting of a novel radionuclide molecular probe ^18F-NT in prostate cancer cells and tumor bearing mice,and to provide experimental evidence for in vivo imaging of ^18F-NT targeted prostate cancer.Methods ^18F-NT was prepared,and quality control testing was completed.A human prostate cancer cell line PC3 with high expression of neurotensin receptor 1（NTR1）was selected.PC3 cells were divided into three groups.The control group received free ^18F ions into the cells.In the experimental group,^18F-NT was added to the cells.Neurotensin（NT）was added to the blocking group 30 min before addition of ^18F-NT.Nude mice were divided into two groups（experimental group and blocking group）,each group had 3 mice.In the blocking group,0.2 ml of1.0 mg/ml NT was injected into the tail vein of each nude mouse,and each mouse in the experimental group was injected with 0.2 ml of saline.After 30 min,each nude mouse in the two groups was injected with 0.2 ml ^18F-NT（the radioactive concentration was 37 MBq/ml）.After 1 h,the nude mice were sacrificed and the major organs and the tumor tissues were separated.γcounter was used to measure the radioactive count of the organs and the tissues.The radioactive count of PC3 cells and radioactive uptake values（%ID/g）of the tumor tissues were analyzed statistically.Results The ^18F-NT was successfully prepared,its physical and chemical properties and the quality control indicators reached standard.Cell-binding assay showed that the radioactive count of the experimental group[（5,825.00±1,074.52）/min]was significantly higher than that of the blocking group[（1,941.66±173.58）/min],the difference was statistically significant（t=7.227,P=0.003）,while that of the free ^18F control group was only（170.33±56.59）/min.The in vivo biological distribution experiment of the two groups of nude mice showed that blood removal rate of ^18F-NT was fast.The ^18F-NT was mainly metabolized by the kidneys.The radioactive uptake value of the tumor tissu

关 键 词：^18F-NT 前列腺癌 PC3 细胞结合实验 生物学分布实验 

分 类 号：R737.25[医药卫生—肿瘤] R-332[医药卫生—临床医学]