Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [131I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy
Document Type
Article
Publication Date
5-1-2023
Abstract
The high rate of incidence and mortality caused by breast cancer encourage urgent research to immediately develop new diagnostic and therapeutic agents for breast cancer. Alpha mangostin (AM) is a natural compound reported to have anti-breast cancer properties. Its electron-donating groups structure allows it to be labeled with an iodine-131 radioisotope to develop a candidate of a diagnostic and therapeutic agent for breast cancer. This study aims to prepare the (131I)]Iodine-a-mangostin (I-131]I-AM) and evaluate its stability, lipophilicity, and cellular uptake in breast cancer cell lines. The I-131]I-AM was prepared by direct radiosynthesis with Chloramine-T method in two conditions (A: AM dissolved in NaOH, B: AM dissolved in ethanol). Reaction time, pH, and mass of the oxidizing agent were optimized as crucial parameters that affected the radiosynthesis reaction. Further analysis was conducted using the radiosynthesis conditions with the highest radiochemical purity (RCP). Stability tests were carried out at three storage conditions, including -20, 2, and 25 degrees C. A cellular uptake study was performed in T47D (breast cancer cell line) and Vero cells (noncancerous cell line) at various incubation times. The results show that the RCP values of I-131]I-AM under conditions A and B were 90.63 +/- 0.44 and 95.17 +/- 0.80% (n = 3), respectively. In the stability test, I-131]I-AM has an RCP above 90% after three days of storage at -20 degrees C. A significant difference was obtained between I-131]I-AM uptake in T47D and Vero cells. Based on these results, I-131]I-AM has been prepared with high RCP, stable at -20 degrees C, and specifically uptaken by breast cancer cell lines. Biodistribution evaluations in animals are recommended as further research in developing I-131]I-AM as a diagnostic and therapeutic agent for breast cancer.
Keywords
I-131]I-alpha mangostin, radiosynthesis, evaluations
Divisions
InstituteofBiologicalSciences
Funders
Ministry of Research and Technology of the Republic of Indonesia (RISTEK) (2064/UN6.3.1/PT.00/2022)
Publication Title
International Journal of Molecular Sciences
Volume
24
Issue
10
Publisher
MDPI
Publisher Location
ST ALBAN-ANLAGE 66, CH-4052 BASEL, SWITZERLAND