对二羟基硼酰苯丙氨酸的^(99)Tcm标记及其生物分布  

Labelling of 4-Dihydroxyborylphenylalanine(BPA) With ^(99)Tc^m and Biodistribution of ^(99)Tc^m-DMG-BPA

作　　者：肖艳[1] 屠荆[1] 唐凌天[2] 唐秀欢[1] 王祥云[2] 

机构地区：[1]西北核技术研究所,陕西西安710024 [2]北京大学化学与分子工程学院,北京100871

出　　处：《核化学与放射化学》2005年第1期35-42,共8页Journal of Nuclear and Radiochemistry

摘　　要：对 二羟基硼酰苯丙氨酸(BPA)由于具有在肿瘤处富集的性质而用于硼中子俘获治疗(BNCT)。按文献方法合成了BPA,并用99Tcm 对其标记,生成一种新的锝包合型螯合物BATO(Boronic acid adducts of techne tium dioxime)配合物,并进行了99Tcm DMG BPA配合物在小鼠体内的生物分布研究。实验结果表明,99Tcm DMG BPA可以选择性富集在肿瘤处,并且清除较慢,在肿瘤中的放射性活度明显高于肌肉和心、肺、血液等组织。随着时间的延长,肿瘤/正常组织的摄入比在不断增加。最大值出现在摄入后 4 h,这时的 R(肿瘤/肌肉)为6 0,R(肿瘤/血液)为4 5,R(肿瘤/心)为 6 0,R(肿瘤/肺)为 3 0,R(肿瘤/肝)为 0 41,R(肿瘤/肾)为0 134。通过分子轨道理论计算推测了99Tcm DMG BPA配合物可能的结构。BPA(4-dihydroxyborylphenylalanine) has being used in clinical trials for treatment of cancer with boron neutron capture therapy (BNCT) technology for its selective accumulation in tumors. BPA is prepared according to the published synthetic procedure. A new BATO complex is synthesized with dimethylglyoxime, BPA, and ^(99)Tc^mO^-_4 as the starting materials via a template reaction. The biodistribution of ^(99)Tc^m-DMG-BPA is studied. The results demonstrate that the complex is selectively accumulated in tumor and slowly cleared from it, the uptake in tumor is higher than in blood, heart, muscle and most of the other organs. The uptake ratio of tumor-to-tissue increased along with time. At 4 hour after injection, the uptake ratio of tumor to muscle reached 6.0, tumor/blood 4.5, tumor/heart 6.0, tumor/lung 3.0, tumor/liver 0.41, and tumor/kidney 0.134. The possible molecular structure of ^(99)Tc^m-DMG-BPA complex is predicted by ab inito MO calculation.

关 键 词：^99TC^M 苯丙氨酸 二羟基 生物分布 标记 硼中子俘获治疗 选择性富集 放射性活度 配合物 acid 分布研究 理论计算 分子轨道 肿瘤 BPA 螯合物 最大值 肌肉 组织 血液 摄入 包合 

分 类 号：TQ463[化学工程—制药化工] TQ246.37