^(131)I-组胺-吲哚美辛及其在荷Lewis肺癌小鼠体内分布、疗效观察的实验研究  

Therapeutic effect of ^(131)I-histamine-indomethacin in mice with Lewis pulmonary tumor

作　　者：罗佳文[1] 张彩霞[2] 刘侃峰[3] 

机构地区：[1]大连医科大学附属第二医院,大连116027 [2]中国医科大学附属盛京医院,沈阳110004 [3]浙江医科大学附属第一医院PET-CT中心,杭州310003

出　　处：《核技术》2012年第6期457-461,共5页Nuclear Techniques

基　　金：辽宁省教育厅重点课题基金资助(20060919)

摘　　要：用氯胺-T作氧化剂将合成的HIS-IN与Na131I室温下振荡反应1 min,加入Na2S2O3混匀终止反应。三氯甲烷和甲醇作展开剂,用支持介质为GF254的薄层层析法鉴定131I-HIS-IN的标记率、放化纯、标记稳定性。研究131I-HIS-IN在荷Lewis肺癌小鼠及正常小鼠体内生物分布实验、肿瘤组织病理观察。结果显示,131I-HIS-IN放化纯>98%;在荷瘤鼠体内生物分布:肿瘤组织在4 h时%ID.g–1达峰值4.73±0.07,8、12、16 h肿瘤/血比值分别为2.95±0.30、2.67±0.62、3.54±0.54,且随时间延长逐渐增加,正常小鼠体内分布实验结果相似。肿瘤组织坏死部分随给药后时间延长而增多。Histamine-indomethacin(HIS-IN) was labeled with 131I by chloramine-T method.Thin-layer chromatography(TLC) was performed to evaluate the labeling ratio,radiochemical purity and stability of 131I-HIS-IN,using silicagel GF254 coated on glass plates,with chloroform and methanol being the mobile phase.The biodistributions of 131I-HIS-IN in Lewis pulmonary tumor model mice and normal mice were examined,and therapeutic effect of 131I-HIS-IN on mice with Lewis pulmonary tumor was studied.The results showed that radiochemical purity of the 131I-HIS-IN was 98%,and the highest %ID.g–1 of tumor tissue was 4.73±0.07 at 4 h,while the tumor/blood ratios were 2.95±0.30 at 8 h,2.67±0.62 at 12 h and 3.54±0.54 at 16 h.The ratios,and the necrotic tissue cells,increased with the post-injection hours.Therefore,131I-HIS-IN can be a new radioactive drug for tumor therapy.

关 键 词：组胺-吲哚美辛 标记 LEWIS肺癌 生物学分布 

分 类 号：R817.1[医药卫生—影像医学与核医学]