^(99)Tc^m标记DPZM类右旋糖苷衍生物的淋巴结摄取  

Lymph Nodes Distribution and Imaging Study of ^(99)Tc^m Labeled DPZM Conjugates

作　　者：李洪玉[1,2] 梁积新[1] 杨春慧 罗洪义[1] 庄玲 陈阳 孙桂全 郑德强 

机构地区：[1]中国原子能科学研究院同位素研究所,北京102413 [2]原子高科股份有限公司,北京102413 [3]中国核工业北京401医院,北京102413

出　　处：《同位素》2014年第3期162-169,共8页Journal of Isotopes

基　　金：IAEA CRP项目(14513)

摘　　要：为探讨99 Tcm标记的甘露糖基右旋糖苷类衍生物DPZM(Dextran-Amine-Pyrazole-Manose)用于前哨淋巴结显像的可行性,采用羰基锝标记了DPZM-4和DPZM-8,制得99 Tcm-(CO)3-DPZM类配合物,考察标记物的体内分布及其在前哨淋巴结(Sentinel Lymph Node,SLN)与次级淋巴结的放射性摄取,研究不同注射剂量对正常鼠的SLN摄取及体内分布的影响,并进行显像。结果表明,99 Tcm-DPZM-4和99 Tcm-DPZM-8的标记率均>90%,配合物稳定性较好;在正常鼠体内,99 Tcm-(CO)3-DPZM类衍生物的前哨淋巴结摄取率较高,给药后1h最高可达6.31%ID,且持续浓集,给药后4h放射性摄取率为3.60%ID,而在其他主要器官的摄取较少;另外,适当减少标记物的注射剂量(包括注射化学量和注射体积)可以提高SLN的摄取率和显像效果。99 Tcm-(CO)3-DPZM的SLN摄取率和体内分布实验结果表明,该类化合物具有应用于SLN显像的潜在价值,值得进行进一步研究。In order to explore the potential application of ^99Tc^m labeled mannosylated dextran conjugates with amine-pyrazole group （Dextran-amine-pyrazole-mannose, DPZM） as senti-nel lymph node （SLN） imaging agent, 99Tcm labeled DPZM conjugates （DPZM-4 and DPZM-8） were prepared through [^99Te^m （CO）3]^＋ precursor synthesized from Isolink kit, and the in-vivo biological behaviors of ^99Tc^m-（co）3-DPZM conjugates were investigated. The labeling yields of ^99Tc^m-（CO）3-DPZM conjugates were above 90%, and the labeled conjugates were relatively stable in vitro and in vivo. The biodistribution results demonstrated that ^99Tc^m-（CO）3-DPZM conjugates were accumulated mainly at injection sites and SLNs, the highest uptake in SLN was found to be 6. 31%ID 1 h p.i. and no significant uptakes were found in major organs such as liver and spleen. The biodistribution of these conjugates was also sensitive to the injected dosage, the uptake of SLN and PE% increased while the injected dosage decreased. The results of SPECT imaging study corresponded to those of biodistribution study, SLN can be clearly visualized and better images could be obtained at lower dosages, the high SLN uptake and PE% along with low radioactivity background of %99Te^m labeled DPZM conjugates showed promise for SLN imaging and detection.

关 键 词：DPZM类右旋糖苷衍生物 ^99TC^M 标记 前哨淋巴结(SLN) 注射剂量 SPECT显像 

分 类 号：TL923[核科学技术—核燃料循环与材料]