碘标EGCG及其小鼠体内生物分布  

Radioiodine-labeling of EGCG and Its Biodistribution in Mice

作　　者：刁尧[1] 刘新宁[1,2] 兰振和 马婧 赵文瑾[1] 刘洁[1] 赵恂[1] 于成国[1] 崔泽实[1] 

机构地区：[1]中国医科大学实验技术中心,辽宁沈阳110001 [2]阜新市第二人民医院,辽宁阜新123000

出　　处：《同位素》2013年第2期86-90,共5页Journal of Isotopes

基　　金：辽宁省自然科学基金资助项目(20092118);辽宁省科学计划项目(2009415005);沈阳市科学技术项目(F11-241-00)

摘　　要：采用Iodogen法对表没食子儿茶素没食子酸酯(Epigallocatechin-3-Gallate,EGCG)进行125I标记,用Sephadex-G25层析柱分离纯化标记物,薄层层析法测定标记率和放化纯度,观察125I-EGCG在小鼠体内的生物分布。结果显示,125I-EGCG标记率达89.4%,放化纯度为96.4%;KM小鼠尾静脉注射后,125I-EGCG在小鼠体内广泛分布,胃、小肠、颌下腺的每克组织放射性摄取率(%ID.g-1)在注入后15min达峰值,分别为15.92、5.83、11.56%ID.g-1,4h时则分别下降为2.75、1.21、2.62;血液中放射性清除较快,注入后5min时血液放射性摄取率为11.95%ID.g-1,4h为1.25%ID.g-1。结果提示,EGCG在体内主要经胃、小肠、颌下腺、肝、肾代谢,可用于进一步的微量示踪研究。To establish the 125I-EGCG labeling method and investigate the biodistribution of 125I-EGCG in mice, 125I-EGCG was prepared by Iodogen solid labeling method, and were i- solated and purified by Sephadex-G25 agarose, The labeling yield and radiochemical purity of 125I-EGCG was analyzed by polymide TLC. The labeling yield of 125I-EGCG was 89.4 and its radiochemical purity（RCP） were 96.4%. The Biodistribution of 125I-EGCG in mice was measured at different times after caudal vein injection with 185 kBq for each mice. The biodistribution in mice demonstrated that 12si EGCG was distributed into broad organs and tissuuues, especially in the Stomach, Small intestine and Submaxillay gland, and the big gest uptake of 125I-EGCG in there organs was 15.92,5.83 and 11.56 %ID·g-1 respectivelyat 15 min post injection. In addition, 125I-EGCG was cleared out from blood guickly, and the uptake of 125I-EGCG in blood was 11.95 at 5 min, and decreased to 1.25 at 4 h post in- jection. Therefore, 125I-EGCG was stable and it was metabolized mainly in Stomach, Small intestine, Submaxillay gland, worthy of further investigation to trace the compound in vivo and in vitro.

关 键 词：表没食子儿茶素没食子酸酯 放射性碘标记 体内分布 

分 类 号：R324[医药卫生—人体解剖和组织胚胎学]