Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
Isti Daruwati,
Abednego Kristande Gwiharto,
Ahmad Kurniawan,
Isa Mahendra,
Tri Hanggono Achmad,
Mukh Syaifudin,
Muchtaridi Muchtaridi
Affiliations
Isti Daruwati
Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Indonesia; Center for Applied Nuclear Research and Technology, Nuclear Energy Research Organization, National Research and Innovation Agency (BRIN), Indonesia
Abednego Kristande Gwiharto
Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Indonesia
Ahmad Kurniawan
Center for Applied Nuclear Research and Technology, Nuclear Energy Research Organization, National Research and Innovation Agency (BRIN), Indonesia
Isa Mahendra
Center for Applied Nuclear Research and Technology, Nuclear Energy Research Organization, National Research and Innovation Agency (BRIN), Indonesia
Tri Hanggono Achmad
Department of Basic Medical Science, Faculty of Medicine, Universitas Padjadjaran, Indonesia
Mukh Syaifudin
Center for Research and Technology of Radiation Safety and Metrology, Nuclear Energy Research Organization, National Research and Innovation Agency (BRIN), Indonesia
Muchtaridi Muchtaridi
Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Indonesia; Functional Nano Powder University Center of Excellence (FiNder U CoE), Universitas Padjadjaran, Indonesia; Corresponding author.
Estradiol is a steroid hormone that works as an agonist estrogen receptor (ER). This compound is widely used as a ligand and bind specifically to the ERα. Radioligand binding assay is an in vitro method for drug development from natural products by synthesizing estradiol through radiolabeling using the radioiodination method. Synthesis of 131I-estradiol was perfomed by direct method using chloramine T as an oxidizer and by indirect labeling using 131I-histamine. The purity of chemical was determined by thin-layer chromatography and paper electrophoresis, as well as its stability for 30 days of storage in refrigerator, freezer and room temperature. The cellular uptake test of the radioligands from both methods was carried out with MCF7 and T-47D cell lines at 60 min. The results exhibited that 131I-estradiol was succesfully obtained with radiochemical purity greater than 95% and more stable in the refrigerator until 21 days than freezer and room temperature. 131I-estradiol and 131I-his-estradiol were internalized higher in T-47D cells than MCF7 cells (44.34 ± 5.93% vs. 17.27 ± 1.71% and 45.34 ± 6.42% vs. 4.92 ± 1.59%, respectively). Furthermore, the radioligands can be used to binding assay in determining the agonist or antagonist to ER of new drugs development.
