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99Tcm(CO)3-CNRGD的制备及生物学评价

Preparation of 99Tcm(CO)3-CNRGD and Its Biologic Evaluation

    摘要
  • 摘要: 合成了含异腈基团的多肽偶联物（CNRGD），并用99Tcm(CO)3(H2O)3+标记，得到具有与整合素αvβ3受体多结合位点的99Tcm(CO)3-CNRGD，并对其进行了体内外生物学评价。结果表明，在优化的标记条件下，99Tcm(CO)3-CNRGD的标记率达到77%，纯化后，标记物放射化学纯度大于96%。体外稳定性实验显示其具有很高的稳定性；脂水分配系数显示其具有较好的脂溶性。正常小鼠体内分布显示，99Tcm(CO)3-CNRGD在血液中清除较快，主要通过肝肾代谢。荷MCF-7人乳腺癌裸鼠体内分布显示，注射1、4 h后，标记物在肿瘤部位的摄取值达(2.38±0.37) %ID/g和(1.57±0.21) %ID/g，瘤/血比分别达0.71±0.09、1.15±0.15，表明该标记物在肿瘤细胞中有一定的摄取和较长的滞留时间。

     

    Abstract: A new radioconjugate with three cyclic RGD was prepared, and in vitro and in vivo evaluation of this conjugate was studied. The results show that the radiolabeled yield of 99Tcm(CO)3-CNRGD reaches to 77% under optimum conditions and the radiochemical purity is more than 96% after purification with a C-18 Sep-Pak Cartridge. The in vitro stability of 99Tcm(CO)3-CNRGD is satisfactory. The partition coefficients of 99Tcm(CO)3-CNRGD indicate that it is a lipophilic compound. The in vivo biodistribution of the radioconjugate in normal mice shows rapid clearance from blood and excretion mainly through hepatobiliary and renal systems. The results in nude mice bearing MCF-7 breast tumor xenografts show that the radioconjugate has moderately tumor uptake and long tumor retention time.

     

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