Kong Fan-Lin, Ali Mohammad S, Zhang Yinhan, Oh Chang-Sok, Yu Dong-Fang, Chanda Mithu, Yang David J
Department of Experimental Diagnostic Imaging, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA.
J Biomed Biotechnol. 2011;2011:276907. doi: 10.1155/2011/276907. Epub 2011 Apr 7.
This study was to develop an efficient synthesis of (99m)Tc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-α-methyl tyrosine ((99m)Tc-N4-AMT) and evaluate its potential in cancer imaging.
N4-AMT was synthesized by reacting N4-oxalate and 3-bromopropyl AMT (N-BOC, ethyl ester). In vitro cellular uptake kinetics of (99m)Tc-N4-AMT was assessed in rat mammary tumor cells. Tissue distribution of the radiotracer was determined in normal rats at 0.5-4 h, while planar imaging was performed in mammary tumor-bearing rats at 30-120 min.
The total synthesis yield of N4-AMT was 14%. Cellular uptake of (99m)Tc-N4-AMT was significantly higher than that of (99m)Tc-N4. Planar imaging revealed that (99m)Tc-N4-AMT rendered greater tumor/muscle ratios than (99m)Tc-N4.
N4-AMT could be synthesized with a considerably high yield. Our in vitro and in vivo data suggest that (99m)Tc-N4-AMT, a novel amino acid-based radiotracer, efficiently enters breast cancer cells, effectively distinguishes mammary tumors from normal tissues, and thus holds the promise for breast cancer imaging.
本研究旨在开发一种高效合成（99m）锝 - O - [3 - （1,4,8,11 - 四氮杂双环十六烷） - 丙基] - α - 甲基酪氨酸（（99m）Tc - N4 - AMT）的方法，并评估其在癌症成像中的潜力。
通过使N4 - 草酸盐与3 - 溴丙基AMT（N - BOC，乙酯）反应合成N4 - AMT。在大鼠乳腺肿瘤细胞中评估（99m）Tc - N4 - AMT的体外细胞摄取动力学。在0.5 - 4小时测定正常大鼠中放射性示踪剂的组织分布，同时在荷乳腺肿瘤大鼠中于30 - 120分钟进行平面成像。
N4 - AMT的总合成产率为14%。（99m）Tc - N4 - AMT的细胞摄取明显高于（99m）Tc - N4。平面成像显示，（99m）Tc - N4 - AMT的肿瘤/肌肉比值高于（99m）Tc - N4。
N4 - AMT可以以相当高的产率合成。我们的体外和体内数据表明，（99m）Tc - N4 - AMT作为一种新型的基于氨基酸的放射性示踪剂，能有效进入乳腺癌细胞，有效区分乳腺肿瘤与正常组织，因此有望用于乳腺癌成像。
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