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Iodine-131 labeled genistein as a potential radiotracer for breast cancer
Danni Ramdhani1,2, Eva Maria Widyasari3, Maula Eka Sriyani3
1Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Padjadjaran University, Sumedang, West Java 45363, Indonesia.
Objective:
Genistein is an isoflavone compound that has been proven to have anticancer activity and is capable of binding to estrogen β receptors with Selective Estrogen Receptor Modulators (SERMs) properties, and has a strong affinity to inhibit the development of cancer cells. This study is to determine the optimum conditions of the reaction in the synthesis process of compounds labeled 131I-genestein which can be potential for application of breast cancer diagnosis.
Methods:
Synthesis of 131I-Genistein compound labeling using the Chloramine-T iodination method. This method uses several parameter optimizations, including: pH conditions, the amount of chloramine-T oxidizer and sodium metabisulfite reducing agent. The radiochemical purity of the 131I-Genistein compound was determined using thin layer chromatography TLC-SG F254, and measured by SCA (Single Channel Analyzer). The radiochemical purity of labeled compounds must fulfill the requirements of the United States of Pharmacopeia.
Results:
Optimization of the synthesis conditions of the 131I-Genistein compound was obtained at pH 8, the amount of chloramine-T 0.225 mg, and the amount of Na-Metabisulfite 0.342 mg, with 30 min reaction time. This optimum condition produces radiochemical purity of 95.02 ± 0.76%.
Conclusion:
Products labeled 131I-Genistein meet radiochemical purity requirements according to USP requirements. The labeled compound is expected to be able to be used to detect breast cancer through a binding mechanism with estrogen receptors β.
Insights
Optimized synthesis of 131I-genistein achieved 95.02% radiochemical purity, meeting USP standards. This labeled compound shows promise for breast cancer diagnosis via estrogen receptor β binding.
Area of Science:
- Radiochemistry
- Nuclear Medicine
- Organic Synthesis
Background:
- Genistein, an isoflavone, exhibits anticancer properties and Selective Estrogen Receptor Modulator (SERM) activity.
- Genistein's affinity for estrogen β receptors suggests potential in cancer therapy and diagnosis.
- 131I-genistein is a potential radiotracer for breast cancer detection.
Purpose of the Study:
- To determine optimal reaction conditions for synthesizing 131I-genistein.
- To achieve high radiochemical purity for diagnostic applications.
- To evaluate the feasibility of 131I-genistein for breast cancer diagnosis.
Main Methods:
- Radiolabeling of genistein using the Chloramine-T iodination method.
- Optimization of synthesis parameters: pH, Chloramine-T concentration, and sodium metabisulfite concentration.
- Radiochemical purity assessment via Thin Layer Chromatography (TLC-SG F254) and Single Channel Analyzer (SCA).
Main Results:
- Optimal synthesis conditions identified at pH 8, 0.225 mg Chloramine-T, and 0.342 mg Na-Metabisulfite.
- Achieved a radiochemical purity of 95.02 ± 0.76% under optimized conditions.
- The synthesized 131I-genistein met United States Pharmacopeia (USP) purity requirements.
Conclusions:
- The optimized synthesis yields 131I-genistein of high radiochemical purity meeting USP standards.
- 131I-genistein is a promising radiolabeled compound for breast cancer detection.
- Its diagnostic potential relies on specific binding to estrogen receptors β.
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