Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)
Makaleler > Tam Makale · 2012
Yazarlar: Perihan ÜNAK, Fazilet Zümrüt BİBER MÜFTÜLER, Çiğdem İÇHEDEF, Emin İlker MEDİNE, Kubra OZMEN, Turan UNAK, Ayfer YURT KILÇAR, F. Gul Gumuser, Yasemin Parlak, Elvan Sayit Bilgin
Journal of Radioanalytical and Nuclear Chemistry, SCI Expanded İndekslerine Giren Dergi, Uluslararası, Wos, 2012, cilt 293, ss 57-66
DOI: 10.1007/s10967-012-1755-5
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 Tc-99m using tin chloride as reducing agent. In vivo biological activity of Tc-99m labeled diethylstilbestrol phosphate compound (Tc-99m-DES-P) was examined by biodistribution studies on Wistar Albino rats. Statistical evaluation was performed using SPSS 13 program. The percentage (%) radiolabeling yield of Tc-99m-DES-P and quality control studies were done by Thin Layer Radio Chromatography (TLRC). Results showed that, Tc-99m-DES-P may be proposed as an imaging agent for ER enriched tumors such as uterus and prostate and their metastases in bones.