Abstract
ObjectiveGenistein 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. MethodsSynthesis 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. ResultsOptimization 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%. ConclusionProducts 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.
Highlights
Breast cancer arises due to abnormal cell growth that duplicates uncontrollably and becomes malignant in the breast
In the US in 2019, there will be an estimated 268,600 new cases of invasive breast cancer diagnosed in women; 2,670 cases diagnosed in men; and an additional 62,930 cases of in situ breast lesions ductal carcinoma in situ [DCIS] or lobular carcinoma in situ [LCIS] diagnosed in women, and invasive female breast cancer incidence rates increased slightly, by 0.4% per year [1]
Expression approaches of estrogen receptors (ER), progesterone receptors (PgR), and HER2 receptors, and evaluation of clinical variables, such as nodal involvement, tumor size, histological type, tumor grade, and surgical margins, are widely used to determine treatment and a prediction of effective breast cancer prognosis [3, 4]
Summary
Breast cancer arises due to abnormal cell growth that duplicates uncontrollably and becomes malignant in the breast. There are many types of breast cancer, in general, ductal carcinoma in situ (DCIS) and invasive carcinoma. Other types, such as phyllodes and angiosarcoma tumors are very rare [1]. In Indonesia, the highest incidence of cancer in women is occupied by breast cancer, which is 42.1 per 100,000 population with an average death rate of 1.7 per 1000 population in 2018 [2]. Expression approaches of estrogen receptors (ER), progesterone receptors (PgR), and HER2 receptors, and evaluation of clinical variables, such as nodal involvement, tumor size, histological type, tumor grade, and surgical margins, are widely used to determine treatment and a prediction of effective breast cancer prognosis [3, 4]
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