碘标EGCG及其小鼠体内生物分布

Radioiodine-labeling of EGCG and Its Biodistribution in Mice

  • 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。

     

    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.

     

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