99Tcm-MAG3-isoDGR-2C分子探针的制备与体内分布的实验研究

Labeling MAG3-isoDGR-2C with 99Tcm and its biodistribution in mice

    摘要
  • 摘要:
    目的 摸索99Tcm-MAG3-isoDGR-2C分子探针的标记条件并研究其在正常昆明小鼠体内的生物学分布。
    方法 利用葡庚糖酸盐（GH）转换络合法进行标记，即首先用99Tcm标记GH形成99TcmO-GH中间体，再进行99Tcm-MAG3-isoDGR-2C的标记；考察pH值和温度等因素对标记率的影响，采用高效液相色谱法鉴定标记物的放射化学纯度；取30只昆明小鼠随机分成6组，分别于注射99Tcm-MAG3-isoDGR-2C 15、30、60、120、240和360 min后测定其在小鼠体内的分布情况。
    结果 pH值为4.6、反应温度为100℃时的标记率最高（94.2%）。体内分布研究显示该标记物能够较快地从血液中清除，且心、肺、脾、胃、骨等组织的放射性摄取均很少。
    结论 99Tcm-MAG3-isoDGR-2C标记率高、血液清除快，具备一定的成为SPECT显像剂的条件。

     

    Abstract:
    Objective To analyze the feasibility of labeling MAG3-isoDGR-2C with 99Tcm and investigate the biodistribution of the tracer in normal mice.
    Methods Glucoheptonate was initially labeled with 99Tcm as the intermediate, followed by MAG3-isoDGR-2C. High-performance liquid chromatography was employed to determine the radiochemical purity. The biodistribution of 99Tcm-MAG3-isoDGR-2C was studied at 15, 30, 60, 120, 240 and 360 min after caudal vein injection in normal mice.
    Results MAG3-isoDGR-2C was successfully labeled with 99Tcm, and the radiochemical purity was 94.2%. The biodistribution revealed that the tracer was rapidly cleared out from the blood with mild activity in the heart, lung, spleen, stomach, and bone.
    Conclusions MAG3-isoDGR-2C was labeled with 99Tcm with high radiochemical purity, and the tracer could be cleared out quickly. Therefore, MAG3-isoDGR-2C is a potential molecular tracer in the study of early cancer diagnosis.

     

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