A novel 99m Tc-diester complex as tumor targeting agent: synthesis, radiolabeling and biological distribution study,Journal of Labelled Compounds and Radiopharmaceuticals

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A novel 99m Tc-diester complex as tumor targeting agent: synthesis, radiolabeling and biological distribution study
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-05-19 , DOI: 10.1002/jlcr.3841
Hesham A Shamsel-Din _{1,

2} , Mohamed A Gizawy _{1,

2} , Elsayed G Zaki ₃ , Amr Elgendy ₃

Affiliation

The target of this study is the synthesis of a new diester derivative and radiolabeling with one of the most effective diagnostic radioisotopes to be investigated as a novel targeting radiotracer for tumor imaging. 10-[2-(9-carboxynonanoyloxy)propoxy]-10-oxodecanoic acid was synthesized in excellent yield and characterized by FT-IR, mass, 1 HNMR and 13 C-NMR spectra. The diester was technetium-99m radiolabeled by direct technique using sodium dithionite as a reducing agent. The labeling parameters such as diester amount, reducing agent amount, pH of the medium and reaction time were optimized. High radiochemical yield of 95.10 ± 0.41% and in-vitro stability in serum up to 12h have been obtained on complexation of the synthesized diester with Tc-99m. Evaluation of the diester anticancer activity against breast cancer cell line (MCF-7) showed high percent of inhibition about 61.5 % at 100 μg/ml. The rhenium complex of the diester was synthesized and characterized by LC-MS (ESI) and elemental analysis depending on the strong chemical resemblance between Tc and Re. Biodistribution studies of 99m Tc-diester complex showed high target to non-target ratio (T/NT) equals 6.24 ± 0.09 in tumor bearing mice at 30 min post injection, suggesting this complex could be used as hopeful solid tumor imaging agent.

中文翻译：

一种新型 99m Tc-二酯复合物作为肿瘤靶向剂：合成、放射性标记和生物分布研究

本研究的目标是合成一种新的二酯衍生物，并用最有效的诊断放射性同位素之一进行放射性标记，作为肿瘤成像的新型靶向放射性示踪剂进行研究。以优异的收率合成了 10-[2-(9-羧基壬酰氧基)丙氧基]-10-氧代癸酸，并通过 FT-IR、质量、 1 HNMR 和 13 C-NMR 光谱进行了表征。使用连二亚硫酸钠作为还原剂，通过直接技术对二酯进行 99m 锝放射性标记。对二酯用量、还原剂用量、培养基pH值和反应时间等标记参数进行了优化。合成的二酯与 Tc-99m 络合，获得了 95.10 ± 0.41% 的高放射化学产率和长达 12 小时的血清体外稳定性。对乳腺癌细胞系 (MCF-7) 的二酯抗癌活性评估显示，在 100 μg/ml 浓度下，抑制率高达约 61.5%。根据 Tc 和 Re 之间强烈的化学相似性，合成了二酯的铼配合物，并通过 LC-MS (ESI) 和元素分析进行了表征。 99m Tc-二酯复合物的生物分布研究表明，注射后 30 分钟，荷瘤小鼠体内的靶点与非靶点比率 (T/NT) 高达 6.24 ± 0.09，表明该复合物有望用作实体瘤显像剂。

更新日期：2020-05-19

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