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藤黄酸的标记及其小鼠体内分布实验

期刊名称：核化学与放射化学 2008,1:39-42
时间：0
分类：R817[医药卫生—影像医学与核医学;医药卫生—放射医学;医药卫生—临床医学]
作者机构：[1]江苏省原子医学研究所,无锡214063, [2]江南大学化工学院,无锡214036, [3]中国药科大学,南京210009
相关基金：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）
相关项目：泛函数理论精确研究带电胶体粒子双电层间的相互作用

关键词：藤黄酸, 放射性碘标记, 细胞摄取, 体内分布, gambogic acid, radioiodinate, cellular uptake, biodistribution

中文摘要：

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Na^131I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.^131I-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。

英文摘要：

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.

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