Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)

Ünak P., Biber Müftüler F. Z., İÇHEDEF Ç., Medine E. I., Özmen K., Ünak T., ...Daha Fazla

Journal of Radioanalytical and Nuclear Chemistry, cilt.293, sa.1, ss.57-66, 2012 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 293 Sayı: 1
  • Basım Tarihi: 2012
  • Doi Numarası: 10.1007/s10967-012-1755-5
  • Dergi Adı: Journal of Radioanalytical and Nuclear Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.57-66
  • Anahtar Kelimeler: Diethylstilbestrol (DES), Tc-99m labeled diethylstilbestrol diphosphate (Tc-99m-DES-P), Tc-99m-DES-P for receptor saturated studies (Tc-99m-Rec-DES-P), Cancer imaging
  • Manisa Celal Bayar Üniversitesi Adresli: Evet

Özet

Diethylstilbestrol (DES) is a well known, nonsteroidal estrogen with high affinity for the estrogen receptor (ER). Today DES is used to treat breast and prostate cancers. A phosphate derivative of DES [Diethylstilbestrol diphosphate (DES-P)] which is specific to tumor cells consisting alkaline phosphatase enzyme was synthesized and labeled with 99mTc using tin chloride as reducing agent. In vivo biological activity of 99mTc labeled diethylstilbestrol phosphate compound ( 99mTc-DES-P) was examined by biodistribution studies on Wistar Albino rats. Statistical evaluation was performed using SPSS 13 program. The percentage (%) radiolabeling yield of 99mTc-DES-P and quality control studies were done by Thin Layer Radio Chromatography (TLRC). Results showed that, 99mTc-DES-P may be proposed as an imaging agent for ER enriched tumors such as uterus and prostate and their metastases in bones. © 2012 Akadémiai Kiadó.