^(99m)TcO(DGDTC)_2肺腺癌Spca-1荷瘤裸鼠实验研究  

Biodistribution of ^(99m)TcO(DGDTC)_2 in nude mice bearing Spca-1

作　　者：霍宗伟[1] 王晓慧[1] 陈鸣陆[1] 方永存[1] 李国梁[1] 张鹏[1] 杨国仁[1] 

机构地区：[1]山东省肿瘤医院核医学科,山东济南250117

出　　处：《肿瘤影像学》2013年第3期237-240,244,共5页Oncoradiology

基　　金：山东省自然科学基金(No:ZR2009CL023)

摘　　要：目的用99mTcO核标记D-葡萄糖氨基酸盐配合物99mTcO(DGDTC)2观察其在肺腺癌(Spca-1)荷瘤裸鼠体内的摄取情况,并与18F-2-氟-2-脱氧-D-葡萄糖(18F-FDG)的分布情况进行比较,分析99mTcO(DGDTC)2作为肿瘤代谢显像剂的可行性。方法配体交换法制备99mTcO(DGDTC)2,将Spca-1荷瘤裸鼠模型50只分为99mTcO(DGDTC)2组和18F-FDG组,检测血液、肝、肾、肌肉、肿瘤中的单位放射性计数比值(%ID/g)及肿瘤与非肿瘤(T/NT)放射性比值。结果高效液相层析(HPLC)分析法测定99mTcO(DGDTC)2放射性化学纯度≥95%。荷瘤裸鼠体内分布实验结果显示,99mTcO(DGDTC)2组注射显像剂后30 min时血液、肾内%ID/g最高,1 h时显著降低。注射显像剂后30 min、1 h、2 h、3h和4 h时肿瘤组织的%ID/g分别为5.16±0.96、3.18±0.73、1.94±0.39、0.86±0.15和0.34±0.09;T/NT分别为1.7、3.2、3.8、1.9和1.4。18F-FDG组注射显像剂后10 min时血液、肾内%ID/g最高,以后逐渐下降,肿瘤%ID/g最高值出现在10min时。T/NT比值在60 min时达最高值2.5,以后逐渐下降。结论 99mTcO(DGDTC)2放射稳定性较好,荷瘤裸鼠体内分布显示具有较好的肿瘤靶向性,类似于18F-FDG,是一种很有发展前景的肿瘤代谢显像剂。Objective To observe the biodistribution of 99mTc-labelled deoxyglucose dithiocarbamate compound[99mTcO(DGDTC)2] in the nude mice bearing pulmonary adenocarcinoma cell line Spca-1. Methods 99mTcO(DGDTC)2was prepared using ligand exchange reaction. The radioactive uptake of 99mTcO(DGDTC)2in pulmonary adenocarcinoma cell line Spca-1 and its biodistribution in nude mice with transplanted Spca-1 were measured. A total of 50 nude mice with transplanted Spca-1 were divided equally into 99mTcO(DGDTC)2group(injected99mTcO(DGDTC)23.7 MBq intravenously, and then the mice were killed at 30 min,1 h,2 h,3 h and 4 h, respectively) and18F-FDG group(injected18F-FDG 3.7 MBq intravenously, and then the mice were killed at 10 min, 20 min, 40 min, 60 min and 120 min, respectively). The radioactive distribution(%ID/g) and tumor/non-tumor tissue(T/NT) radioactive ratio in tumor, blood, liver, kidneys and muscles were measured. Results99mTcO(DGDTC)2was successfully prepared and the radiochemical purity(RCP) was ≥95% determinated by high-performance liquid chromatography(HPLC). In99mTcO(DGDTC)2group, the %ID/g in blood and kidneys reached the maximum 30 min after injection, and then gradually decreased. The %ID/g in the tumor at 30 min, 1 h, 2 h, 3 h and 4 h was 5.16±0.96, 3.18±0.73, 1.94±0.39, 0.86±0.15 and 0.34±0.09, respectively. The corresponding T/NT was 1.7, 3.2, 3.8, 1.9 and1.4, respectively. At each time point, the %ID/g in the kidneys was significantly higher than that in the liver, with a peak at 30min, and then decrease after 3 h. In18F-FDG group,the %ID/g in blood and kidneys reached the maximum 10 min after injection, then then gradually decreased. The maximum %ID/g in the tumor was detected at 10 min and the maximum T/NT was detected at 1 h after injection. Both %ID/g and T/NT significantly decreased 2 h after injection. Conclusion The new tracer,99mTcO(DGDTC)2, can be prepared with good quality. The in vivo study demonstrated the high uptake of99mTcO(DGDTC)2in transplanted tumor, implicating the potential applicati

关 键 词：99mTc标记葡萄糖 放射性药物 细胞系 单光子发射计算机断层扫描 正电子发射计算机断层扫描 

分 类 号：R817.4[医药卫生—影像医学与核医学] R734.2[医药卫生—放射医学]