Erfani Mostafa, Shirmardi Seyed Pezhman, Shafiei Mohammad
Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
Iran J Pharm Res. 2017 Summer;16(3):999-1006.
Colchicine as a vascular disrupting agent creates microtubule destabilization which induces vessel blockage and consequently cell death. Accordingly, colchicines and its analogues radiolabeled with Tc may have potential for visualization of tumor. In this work, deacetylcolchicine a colchicine analogue was labeled with Tc via tricine as a coligand and characterized for its tumor targeting properties. The radiochemical stability and the biodistribution were studied in 4T1 breast tumor model bearing mice. Labeling yield of more than 90% was obtained corresponding to a specific activity of 46 MBq/µmol. biodistribution studies demonstrated that radiocomplex had high tumor to muscle and tumor to blood ratios at early time points. Planer gamma imaging of tumor bearing mice showed that this radioconjugate was able to clearly visualize tumors. According to high tumor uptake, presented radiocomplex may have a potential for targeted imaging studies.
秋水仙碱作为一种血管破坏剂会导致微管失稳，进而引起血管阻塞并最终导致细胞死亡。因此，用锝标记的秋水仙碱及其类似物可能具有肿瘤显像的潜力。在本研究中，将秋水仙碱类似物去乙酰秋水仙碱通过三羟甲基氨基甲烷作为共配体用锝进行标记，并对其肿瘤靶向特性进行了表征。在携带4T1乳腺肿瘤模型的小鼠中研究了其放射化学稳定性和生物分布。标记产率超过90%，比活度为46 MBq/µmol。生物分布研究表明，放射性复合物在早期时间点具有高的肿瘤与肌肉以及肿瘤与血液的比率。对荷瘤小鼠的平面γ显像显示，这种放射性缀合物能够清晰地显示肿瘤。基于高肿瘤摄取率，所呈现的放射性复合物可能具有靶向成像研究的潜力。
