Iodine-131 labeled genistein as a potential radiotracer for breast cancer

Danni Ramdhani, Eva Maria Widyasari, Maula Eka Sriyani, Quinzheilla Putri Arnanda, Hiroshi Watabe

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Article numbere04780
JournalHeliyon
Volume6
Issue number9
DOIs
Publication statusPublished - 2020 Sep

Keywords

  • Breast cancer
  • Estrogen receptors beta
  • Genestein
  • Iodine-131
  • Pharmaceutical chemistry
  • Radiotracer

ASJC Scopus subject areas

  • General

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