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

Heliyon

Maula Eka Sriyani¹  Eva Maria Widyasari²  Hiroshi Watabe³  Quinzheilla Putri Arnanda³  Danni Ramdhani⁴ 

[1] Corresponding author.;Division of Radiation Protection and Safety Control, Cyclotron and Radioisotope Center, Tohoku University, Sendai, Japan;Applied Nuclear Science and Technology Center (PSTNT), National Nuclear Energy Agency of Indonesia (BATAN), Bandung, West Java 40116, Indonesia;Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Padjadjaran University, Sumedang, West Java 45363, Indonesia;

关键词: Pharmaceutical chemistry;    Iodine-131;    Genestein;    Breast cancer;    Radiotracer;    Estrogen receptors beta;   

DOI  :  

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown