碘标EGCG及其小鼠体内生物分布

doi:10.7538/tws.2013.26.02.0086

摘要/Abstract

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15 min达峰值，分别为15.92、5.83、11.56%ID·g^-1，4 h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5 min时血液放射性摄取率为11.95%ID·g^-1，4 h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。

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

Abstract:

To establish the ¹²⁵I-EGCGlabeling method and investigate the biodistribution of ¹²⁵I-EGCG inmice, ¹²⁵I-EGCG was prepared by Iodogen solid labeling method, andwere isolated and purified by Sephadex-G25 agarose, The labeling yield andradiochemical purity of ¹²⁵I-EGCG was analyzed by polymide TLC. Thelabeling yield of ¹²⁵I-EGCG was 89.4% and its radiochemicalpurity(RCP) were 96.4%. The Biodistribution of ¹²⁵I-EGCG in mice wasmeasured at different times after caudal vein injection with 185 kBq for eachmice. The biodistribution in mice demonstrated that ¹²⁵I-EGCG wasdistributed into broad organs and tissuuues, especially in the Stomach, Smallintestine and Submaxillay gland, and the biggest uptake of ¹²⁵I-EGCGin there organs was 15.92、5.83and 11.56 %ID·g^-1respectively at 15 min post injection. In addition, ¹²⁵I-EGCG wascleared out from blood guickly, and the uptake of ¹³¹I-EGCG in blood was 11.95 at 5 min, anddecreased to 1.25 at 4 h post injection. Therefore, ¹²⁵I-EGCG wasstable and it was metabolized mainly in Stomach, Small intestine, Submaxillaygland, worthy of further investigation to trace the compound in vivo and invitro.

Key words: Epigallocatechin-3-Gallate, radioiodinate, biodistribution

刁尧;刘新宁;兰振和;马婧;赵文瑾;刘洁;赵恂;于成国;崔泽实. 碘标EGCG及其小鼠体内生物分布[J]. 同位素, 2013, 26(2): 86-90.

DIAO Yao;LIU Xin-ning;LAN Zhen-he;MA Jing;ZHAO Wen-jin;LIU Jie;ZHAO Xun;YU Cheng-guo;CUI Ze-shi. Radioiodine-labeling of EGCG and Its Biodistribution in Mice[J]. Journal of Isotopes, 2013, 26(2): 86-90.

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