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

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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.

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Acknowledgments

The authors thank the financial support from Ege University Scientific Research Fund with the Project Number 2009NBE001. Authors thank to Dr. Memduh Bülbül for providing ALP.

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Authors and Affiliations

  1. Department of Nuclear Applications, Institute of Nuclear Science, Ege University, Bornova, Izmir, Turkey

    Perihan Ünak, F. Zümrüt Biber Müftüler, Çiğdem İçhedef, E. İlker Medine, Kübra Özmen & Ayfer Yurt Kilçar

  2. Department of Chemistry, Faculty of Science, Ege University, Bornova, Izmir, Turkey

    Turan Ünak

  3. Department of Nuclear Medicine, School of Medicine, Celal Bayar University, Manisa, Turkey

    F. Gül Gümüşer, Yasemin Parlak & Elvan Sayıt Bilgin

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  1. Perihan Ünak
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  2. F. Zümrüt Biber Müftüler
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  4. E. İlker Medine
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  6. Turan Ünak
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Correspondence to F. Zümrüt Biber Müftüler.

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Ünak, P., Biber Müftüler, F.Z., İçhedef, Ç. et al. Synthesis, radiolabeling and in vivo biodistribution of diethylstilbestrol phosphate derivative (DES-P). J Radioanal Nucl Chem 293, 57–66 (2012). https://doi.org/10.1007/s10967-012-1755-5

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  • DOI: https://doi.org/10.1007/s10967-012-1755-5

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