Synthesis and Biological Evaluation of Bisphosphonate Compound Labeled with 99mTc(CO)3+
Synthesis and Biological Evaluation of Bisphosphonate Compound Labeled with 99mTc(CO)3+
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DOI：
10.1111/cbdd.12401
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发表时间：
2015-03
影响因子：
3
通讯作者：
Kamile Şenocak;S. Teksöz;C. Ichedef;E. Uçar
中科院分区：
文献类型：
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作者：
Kamile Şenocak;S. Teksöz;C. Ichedef;E. Uçar
在这项研究中，放射性标记的双磷酸盐，阿仑膦酸盐（阿仑膦酸钠），是在双功能螯合剂的帮助下进行的。为此，用DTPA和NHS之间的酯化反应合成了DTPA - NHS（二乙烯三胺五乙酸二酐- N -羟基琥珀酰亚胺）。将DTPA - NHS酯与阿仑膦酸结合，得到DTPA -阿仑膦酸化合物。用1H/13C/31P‐NMR和HPLC对合成的化合物进行了结构分析。然后对合成的化合物进行[99mTc(CO)3]+核标记。用薄层放射色谱（TLRC）和高效液相放射色谱（HPLRC）对新合成的[99mTc(CO)3 - DTPA -阿仑膦酸]配合物进行质量控制，标记率为99%。结果表明，该化合物在血清培养基中可保持24 h的稳定性。在Wistar白化大鼠身上进行放射性标记复合物的生物分布，以确定[99mTc(CO)3 - DTPA -阿仑膦酸盐]复合物的放射性药物潜力。据认为，从这项研究中获得的数据将有助于开发与二膦酸盐配合物。
In this study, radiolabeling of a bisphosphonate, alendronate (Alendronate sodium), was performed with the help of a bifunctional chelating agent. For that purpose, DTPA‐NHS (Diethylenetriaminepentaacetic acid dianhydride‐N‐hydroxysuccinimide) was synthesized with an esterification between DTPA and NHS. Combining the DTPA‐NHS ester with alendronate yields the DTPA‐Alendronate compound. The structure of synthesized compound was analyzed by 1H/13C/31P‐NMR and HPLC. After then, the labeling with [99mTc(CO)3]+ core of synthesized compound was provided. Performing quality controls of newly synthesized [99mTc(CO)3‐DTPA‐Alendronate] complex with thin layer radiochromatography (TLRC) and high‐performance liquid radiochromatography (HPLRC), the labeling yield was found as 99%. It was observed that the compound conserves its stability for 24 h in serum media. Biodistribution of the radiolabeled complex was performed on Wistar Albino rats to determine radiopharmaceutical potential of the [99mTc(CO)3‐DTPA‐Alendronate] complex. It is thought that the data gained from this study will contribute to the development of complexes with bisphosphonate.