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

Abstract

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 131 I-genestein which can be potential for application of breast cancer diagnosis. Methods: Synthesis of 131 I-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 131 I-Genistein compound was determined using thin layer chromatography TLC-SG F 254 , 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 131 I-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 AE 0.76%. Conclusion: Products labeled 131 I-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.

Effectiveness and Safety of Levothyroxine Tablets Combined with Iodine-131 in the Treatment of Thyroid Cancer

“…At present, surgery is the mainstay of treatment for thyroid cancer. Due to the slow progression of thyroid cancer and the low degree of malignancy, it has been reported that palliative treatment with thyroid hormones after tumor resection could achieve favorable results [ 16 ]. However, prior research has shown that most recurrence and metastasis occur within 5 years after surgery [ 17 , 18 ], which was similar to the results of the present study.…”

Targeted radioimmunotherapy with the iodine-131-labeled caerin 1.1 peptide for human anaplastic thyroid cancer in nude mice

“…The application of radioimmunoconjugates (RICs) in the brachytherapy of malignant tumors by vascular intervention or by direct implantation has achieved remarkable success, over the past 25 years, a wide variety of RICs labeled with radioisotopes (i.e., 111 In, 89 Zr and 131 I) have been explored and translated to the clinic [ 6 – 8 ]. Among the numerous radionuclides used in diagnosis and therapy, iodine-131 ( 131 I) is a rare radioisotope with both γ- and β-particle emission characteristics; it has a half-life of 8.1 days and is routinely commonly used in radionuclide labeling [ 9 ]. Moreover, free 131 I that dissociates from a RICs accumulates in the thyroid gland or is excreted, but is not excreted from the body but accumulates in the liver, spleen, and bone, which has almost no side effects [ 10 ].…”

“…RT has been considered an immunosuppressive treatment, and it has been extensively reported to have immunomodulatory effects in preclinical and clinical studies [ 2 , 20 ]. RT releases tumor-specific antigens and activates the immune signaling pathway [ 21 ], accelerates programmed cell death by immune mediation [ 22 ], modulates the TME, increases immunocyte infiltration in tumors [ 23 ], stimulates tumor-specific cytotoxic T cells, and enhances T cell homing, engraftment and function in tumors [ 9 , 24 ]. Therefore, the synergistic effect of RT and immunotherapy is well known.…”