藤黄酸的标记及其小鼠体内分布实验  

Radioiodinated of Gambogic Acid and Its Biodistribution in Mice

作　　者：谭成[1] 俞惠新[1] 林秀峰[1] 杨勇[2] 张莉[1] 陈波[1] 宋翠翠 曹国宪[1] 王正武 

机构地区：[1]江苏省原子医学研究所,无锡214063 [2]中国药科大学,南京210009 [3]江南大学化工学院,无锡214036

出　　处：《核化学与放射化学》2008年第1期39-42,共4页Journal of Nuclear and Radiochemistry

基　　金：江苏省自然科学基金资助项目(BK2006026);国家自然科学基金资助项目(30470496)

摘　　要：通过131I标记藤黄酸以分析其在肿瘤细胞中的摄取及动物体内的分布。采用双氧水标记、氯仿萃取,以聚酰胺薄膜为支持介质、氯仿-甲醇(体积比为40∶1)为展开剂,测定标记率及放化纯;分析肿瘤细胞MCF-7对131I-藤黄酸的摄取;KM小鼠尾静脉注射131I-藤黄酸(每只185 kBq),于不同时间处死,取各脏器,称重、测量计数率,计算每克组织百分注射剂量率。131I-藤黄酸标记率达86%,放化纯在1,4,20 d分别为97.2%,95.4%,93.3%;MCF-7在30 min时对131I-藤黄酸摄取率达3.50%,显著高于对Na131I的摄取(P<0.01);131I-藤黄酸在体内分布广泛,以肝、肾和肠为最多,肝中5 min时放射性摄取达25.93%ID/g,4 h则为5.54%ID/g,而肾中5 min时为6.37%ID/g,4 h时为2.46%ID/g;甲状腺中的放射性摄取随时间的延长而增加1。31I-藤黄酸标记物稳定;肿瘤细胞MCF-7对131I-藤黄酸有显著摄取;体内主要通过肝肾代谢。The preparation of radioiodinated gambogic acid and its cell uptake in MCF-7 and bio distribution in mice were investigated. Gambogic acid was labeled with ^131I using hydrogen peroxide. The radiolabeled compound was characterized by polyamide TLC, in which the substratum of V（trichoromethane ） ： V（ methanol ） =40 ： 1 was used as developing agent. The uptake of ^131 I-gambogic acid in cancer ceils was measured. Biodistribution studies were carried out in KM mice. At different time after radiopharmaceutical i. v. administration （185 kBq ^131I-gambogic acid /mouse）, the animals were sacrificed. Blood samples and the tissues of interested were collected, weighted and counted. The percent injected dose per gram （%ID/g） was calculated for each sample. The labeling yield of ^131I-gambogic acid is 86% and its radiochemistry purity are 97. 2%, 95. 4%, and 93.3% at 1, 4, and 20 d, respectively. The uptake of ^131I- gambogic acid in MCF-7 shows markedly higher compared with Na^131 I（P〈0.01）. The in vivo biodistribution in mice indicates that ^131I-gambogic acid is mainly uptaked in liver, kidney, and intestines. The radioactivity in thyroid increases with time. ^131I-gambogic acid is stable and is markedly uptaked in cancer cells MCF-7. In mice, it is mainly metabolized by liver and excreted through kidney.

关 键 词：藤黄酸 放射性碘标记 细胞摄取 体内分布 

分 类 号：R817[医药卫生—影像医学与核医学]