^(188)Re-DTPA-DG的制备和荷瘤裸鼠实验研究  

^(188)Re-DTPA-DG preparation and its experimental imaging in MCF-7 tumor-bearing nude mice

作　　者：陈跃[1] 熊青峰[1] 何菱[2] 黄占文[1] 郑时龙[2] 李举联[2] 秦大莲[3] 

机构地区：[1]泸州医学院附属医院核医学科,646000 [2]四川大学华西药学院 [3]泸州医学院附属药学院

出　　处：《中华核医学杂志》2007年第2期107-108,共2页Chinese Journal of Nuclear Medicine

基　　金：国家自然科学基金(30670582);四川省教育厅自然科学研究基金(2004B005)

摘　　要：目的建立^(188)Re 标记 DTPA-脱氧葡萄糖(DG)的方法,观察其在荷瘤裸鼠体内分布和治疗效果。方法 DTPA-DG 的^(188)Re 标记体系有氯化亚锡、葡萄糖酸钠,pH 值5.5,反应体系温度为37℃,反应3 h,用纸层析法以生理盐水和丙酮作展开剂,测定标记物的放化纯及其在体外的稳定性。将标记物经荷乳腺癌 MCF-7裸鼠尾静脉注射,于注射后1,4,8,12,24 h 显像。经尾静脉注射0.1 ml 92.5 GBq/L 的^(188)Re-DTPA-DG,21 d 后观察疗效。结果 ^(188)Re-DTPA-DG 的放化纯可达到95.0%。^(188)Re-DTPA-DG 荷瘤裸鼠显像示肿瘤组织摄取高,病灶/健侧后肢对应部位放射性计数(T/NT)比值在12和24 h 分别为5.9和7.8。^(188)Re-DTPA-DG 组裸鼠治疗21 d 后肿瘤体积[(823.6±50.58)mm^3]明显比生理盐水组[(1162.7±73.08)mm^3]小,2组间差异有统计学意义(P<0.01),抑瘤率为29.2%。结论 ^(188)Re-DTPA-DG 经荷瘤裸鼠尾静脉注射后可被肿瘤组织高选择性摄取,其对肿瘤生长抑制作用明显,可能成为肿瘤内照射治疗药物。Objective With the similar physic property, ^188Re might replace 99Tem in labeling glu- cose analogues. ^188Re-DTPA-deoxyglueose （^188Re-DTPA-DG） was prepared, and was tried in MCF-7 breast cancer ceils bearing nude mice for imaging and therapeutic trials. Methods The labeling of DTPA-DG with ^188Re was conducted in the presence of stannous ion and sodium D-glueonate at pH 5.5, incubated for 3 h at 37℃. The radiolabeling yields of ^188Re-DTPA-DG were determined by using acetone and saline （0. 9% NaC1） developed paper chromatography. ^188Re-DTPA-DG of 0.1 ml 92.5 GBq/L was injected into the tail vein of tumor bearing nude mouse, then imaged at 2, 4, 8, 12 and 24 h. Tumor volumes were measured every 2 or 3 d for 21 d. Results The radiochemical purity of the ^188Re-DTPA-DG reached 95.0%. In imaging, the uptake ratios of tumor to background （T/B） at 12 and 24 h were 5.9 and 7.8, respectively. Tumors in ^188Re-DTPA-DG treated mice were smaller than that of control group. The volume was significantly different between treated group [ （ 823.6 ± 50.58 ） mm^3 ] and control group [ （ 1162.7± 73.08 ） mm^3 ] after 21 d （ P 〈 0.01 ）. Conclusion ^188Re-DTPA-DG showed excellent tumor targeting and tumor growth suppression effect, thereafter it could be a potential agent for the internal radiotherapy of tumor.

关 键 词：脱氧葡萄糖 DTPA 同位素标记 铼 鼠 裸 乳腺肿瘤 放射性核素显像 

分 类 号：R73-3[医药卫生—肿瘤]