红景天苷的碘标记及其在小鼠体内的分布  

Radioiodine-labeling of salidroside and its biodistribution in mice

作　　者：林秀峰[1] 俞惠新[1] 谭成[1] 张莉[1] 陈波[1] 张荣军[1] 徐希杰[1] 曹国宪[1] 

机构地区：[1]江苏省原子医学研究所卫生部核医学重点实验室,无锡214063

出　　处：《核技术》2006年第12期913-916,共4页Nuclear Techniques

基　　金：江苏省无锡市自然基金(CK040004);江苏省自然基金(BK2006026)

摘　　要：通过131碘标记红景天苷以探索红景天苷在神经母细胞(SH-SY5Y)中的摄取及在小鼠体内的代谢分布。采用氯胺-T法对红景天苷进行131碘标记;以聚酰胺薄膜为支持介质、V三氯甲烷:V甲醇:V丙酮:V水=6:3:1:1的下层液为展开剂,测定标记率及标记物放化纯;分析神经母细胞SH-SY5Y及肿瘤细胞MCF-7对131I-红景天苷的摄取;KM小鼠尾静脉注射131I-红景天苷(1.85MBq/只,n=5),于5、10、30、60、120、240min分别取心、肝、肺、肾、脾、肌、骨、脑、肠、血,称重、计数,计算每克组织百分注射剂量率(%ID/g)。结果表明,131I-红景天苷标记率达98%,其放化纯在1、4、20d分别为98.5%、97.3%、97.1%;SH-SY5Y对131I-红景天苷基本无摄取,在0.5—4h内摄取维持在0.035%左右,而MCF-7则为0.1%;131I-红景天苷在体内主要通过肝代谢、肾排泄,其中肝和肾5min%ID/g组织分别为7.71%和11.32%,4h则分别下降为0.36%和0.3%;血液中清除也较快,5min时为6.41%,4h为0.35%;在脑中虽分布较少,但清除较慢,5min时为0.27%,4h为0.11%;在心、肺、脾、肌、骨及肠中分布不多。结论是,碘标红景天苷标记率高,标记物稳定;神经母细胞对131I-红景天苷基本无摄取。To investigate the preparation of radioiodinated salidroside and its cell uptake in SH-SY5Y and its biodistribution in mice, salidroside was labeled with ^131Ⅰ using the chloramine-T method and the radiolabeled compound was characterized by polyamide TLC, in which the substratum of Vtrichoromethane： Vmethanol： Vacetone： Vwater=6：3：1：1 was used as the developing agent. The uptake of ^131Ⅰ-salidroside in human neuroblast cells（SH-SYSY） and mammary cancer cells（MCF-7） was then measured and the biodistribution studies were carded out in KM mice. At different time（5, 10, 30, 60, 120, and 240 min） after radiopharmaceutical i.v. administration （1.85MBq ^131Ⅰ-salidroside/mouse）, the animals were sacrificed （n=5 animals for each time）. Blood and the interested tissues samples were collected, washed, weighted and counted. The percent injected dose per gram （%ID/g） was calculated for each sample. The labeling yield of ^131Ⅰ-salidroside was 98% and its RCPs were 98.5%, 97.3%, and 97.1% after 1, 4 and 20 days, respectively. In SH-SYSY, ^131Ⅰ-salidroside uptake kept at a low level of around 0.035% from 0.5 to 4h, while in MCF-7 a slightly higher uptake of 0.1% was reached. Biodistribution in mice demonstrated that ^131Ⅰ-salidroside was metabolized mainly in liver and rapid elimination through kidney, in which the % ID/g were 7.71% and 11.31% at 5 min, 0.36% and 0.3% at 4h, respectively. Rapid clearance was also found in blood, 6.43% at 5 min and decreased to 0.35% at 4h. A little distribution appeared in brain with slower clearance, the %ID/g were 0.27% at 5 rain and 0.11% at 4h. In heart, lung, spleen, muscle, bone, and intestines, there were little distributions. It is concluded that labeling yield of ^131Ⅰ-salidroside was high and the radioiodinated salidroside was stable, but its uptake in neuroblast was little.

关 键 词：红景天苷 放射性碘标记 体内分布 细胞摄取 

分 类 号：R817-33[医药卫生—影像医学与核医学] R285.5[医药卫生—放射医学]