基于受体的肿瘤成像剂的合成与生物学评价：(99m)Tc-叶酸-葡萄糖醛酸。
Synthesis and biological evaluation of receptor-based tumor imaging agent: (99m)Tc-folate-glucaric acid.
机构信息
Department of Nuclear Applications, Ege University, Bornova 35100 Izmir, Turkey.
出版信息
Int J Pharm. 2011 Sep 15;416(1):288-92. doi: 10.1016/j.ijpharm.2011.07.010. Epub 2011 Jul 18.
The aim of the present study was to prepare (99m)Tc-folate-glucaric acid and investigate the radiopharmaceutical potential for tumors imaging that over express folate receptor. Folate-glucaric acid was synthesized and the synthesized folate conjugate was confirmed with (1)H NMR and LC-MS/MS methods. Folate-glucaric acid was labeled with (99m)Tc, and its radiolabelling efficiency was found as 96 ± 2.0%. Biodistribution study of (99m)Tc-folate-glucaric acid was carried out in vivo using two groups of female Albino Wistar rats: folate receptor (FR) saturated and unsaturated. Biodistribution study showed that (99m)Tc-folate-glucaric acid indicated high uptake in folate receptor rich tissues such as breast, ovary and uterus. Therefore, (99m)Tc-folate-glucaric acid shows good radiolabeling and biodistribution in FR organs, the radiolabeled conjugate is a reason potentially useful radiopharmaceutical for detection of FR-positive tumors.
本研究旨在制备（99m）Tc-叶酸-葡萄糖酸，并研究其用于成像过度表达叶酸受体的肿瘤的放射性药物潜力。叶酸-葡萄糖酸被合成，并用（1）H NMR 和 LC-MS/MS 方法确认合成的叶酸缀合物。叶酸-葡萄糖酸被（99m）Tc 标记，其放射性标记效率为 96±2.0%。使用两组雌性白化 Wistar 大鼠进行（99m）Tc-叶酸-葡萄糖酸的体内分布研究：叶酸受体（FR）饱和和不饱和。分布研究表明，（99m）Tc-叶酸-葡萄糖酸在富含叶酸受体的组织（如乳房、卵巢和子宫）中具有高摄取率。因此，（99m）Tc-叶酸-葡萄糖酸在 FR 器官中表现出良好的放射性标记和分布，放射性标记的缀合物是一种潜在有用的用于检测 FR 阳性肿瘤的放射性药物。
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