Synthesis and Biological Evaluation of Bisphosphonate Compound Labeled with Tc-99m(CO)(3)(+)


SENOCAK K., TEKSÖZ S. , İÇHEDEF Ç. , UCAR E.

CHEMICAL BIOLOGY & DRUG DESIGN, cilt.85, ss.369-376, 2015 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 85 Konu: 3
  • Basım Tarihi: 2015
  • Doi Numarası: 10.1111/cbdd.12401
  • Dergi Adı: CHEMICAL BIOLOGY & DRUG DESIGN
  • Sayfa Sayıları: ss.369-376

Özet

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 H-1/C-13/P-31-NMR and HPLC. After then, the labeling with [Tc-99m(CO)(3)](+) core of synthesized compound was provided. Performing quality controls of newly synthesized [Tc-99m(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 24h in serum media. Biodistribution of the radiolabeled complex was performed on Wistar Albino rats to determine radiopharmaceutical potential of the [Tc-99m(CO)(3)-DTPA-Alendronate] complex. It is thought that the data gained from this study will contribute to the development of complexes with bisphosphonate.