Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P)
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Date
2012
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Abstract
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.
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Keywords
alkaline phosphatase , diethylstilbestrol phosphate , diethylstilbestrol phosphate derivative , technetium 99m , tin chloride , unclassified drug , animal experiment , animal tissue , article , carbon nuclear magnetic resonance , controlled study , distillation , drug distribution , drug structure , drug synthesis , female , imaging , in vivo study , isotope labeling , male , nonhuman , population distribution , purification , quality control , radioactivity , radiochromatography , rat , tandem mass spectrometry , thin layer chromatography , tissue distribution