Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy
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...
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| Format: | Article |
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MDPI AG
2023-05-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/24/10/8678 |
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| author | Wiwit Nurhidayah Eva Maria Widyasari Isti Daruwati Isa Mahendra Toto Subroto Nur Kusaira Khairul Ikram Muchtaridi Muchtaridi |
| author_facet | Wiwit Nurhidayah Eva Maria Widyasari Isti Daruwati Isa Mahendra Toto Subroto Nur Kusaira Khairul Ikram Muchtaridi Muchtaridi |
| author_sort | Wiwit Nurhidayah |
| collection | DOAJ |
| description | 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 [<sup>131I</sup>]Iodine-α-mangostin ([<sup>131</sup>I]I-AM) and evaluate its stability, lipophilicity, and cellular uptake in breast cancer cell lines. The [<sup>131</sup>I]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 °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 [<sup>131</sup>I]I-AM under conditions A and B were 90.63 ± 0.44 and 95.17 ± 0.80% (n = 3), respectively. In the stability test, [<sup>131</sup>I]I-AM has an RCP above 90% after three days of storage at −20 °C. A significant difference was obtained between [<sup>131</sup>I]I-AM uptake in T47D and Vero cells. Based on these results, [<sup>131</sup>I]I-AM has been prepared with high RCP, stable at −20 °C, and specifically uptaken by breast cancer cell lines. Biodistribution evaluations in animals are recommended as further research in developing [<sup>131</sup>I]I-AM as a diagnostic and therapeutic agent for breast cancer. |
| first_indexed | 2024-03-11T03:40:46Z |
| format | Article |
| id | doaj.art-9b7bce9fb81e4adcaceefbc8d888193b |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-11T03:40:46Z |
| publishDate | 2023-05-01 |
| publisher | MDPI AG |
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| series | International Journal of Molecular Sciences |
| spelling | doaj.art-9b7bce9fb81e4adcaceefbc8d888193b2023-11-18T01:39:57ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-05-012410867810.3390/ijms24108678Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and TherapyWiwit Nurhidayah0Eva Maria Widyasari1Isti Daruwati2Isa Mahendra3Toto Subroto4Nur Kusaira Khairul Ikram5Muchtaridi Muchtaridi6Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Padjadjaran, Sumedang 45363, IndonesiaResearch Center for Radioisotope, Radiopharmaceutical, and Biodosimetry Technology, Research Organization for Nuclear Energy, National Research and Innovation Agency, South Tangerang 15310, IndonesiaResearch Collaboration Center for Theranostic Radiopharmaceuticals, Sumedang 45363, IndonesiaResearch Collaboration Center for Theranostic Radiopharmaceuticals, Sumedang 45363, IndonesiaResearch Centre of Molecular Biotechnology and Bioinformatics, Universitas Padjadjaran, Sumedang 45363, IndonesiaInstitute of Biological Sciences, Faculty of Science, Universiti Malaya, Kuala Lumpur 50603, MalaysiaResearch Collaboration Center for Theranostic Radiopharmaceuticals, Sumedang 45363, IndonesiaThe 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 [<sup>131I</sup>]Iodine-α-mangostin ([<sup>131</sup>I]I-AM) and evaluate its stability, lipophilicity, and cellular uptake in breast cancer cell lines. The [<sup>131</sup>I]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 °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 [<sup>131</sup>I]I-AM under conditions A and B were 90.63 ± 0.44 and 95.17 ± 0.80% (n = 3), respectively. In the stability test, [<sup>131</sup>I]I-AM has an RCP above 90% after three days of storage at −20 °C. A significant difference was obtained between [<sup>131</sup>I]I-AM uptake in T47D and Vero cells. Based on these results, [<sup>131</sup>I]I-AM has been prepared with high RCP, stable at −20 °C, and specifically uptaken by breast cancer cell lines. Biodistribution evaluations in animals are recommended as further research in developing [<sup>131</sup>I]I-AM as a diagnostic and therapeutic agent for breast cancer.https://www.mdpi.com/1422-0067/24/10/8678[<sup>131</sup>I]I-alpha mangostinradiosynthesisevaluations |
| spellingShingle | Wiwit Nurhidayah Eva Maria Widyasari Isti Daruwati Isa Mahendra Toto Subroto Nur Kusaira Khairul Ikram Muchtaridi Muchtaridi Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy International Journal of Molecular Sciences [<sup>131</sup>I]I-alpha mangostin radiosynthesis evaluations |
| title | Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy |
| title_full | Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy |
| title_fullStr | Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy |
| title_full_unstemmed | Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy |
| title_short | Radiosynthesis, Stability, Lipophilicity, and Cellular Uptake Evaluations of [<sup>131</sup>I]Iodine-α-Mangostin for Breast Cancer Diagnosis and Therapy |
| title_sort | radiosynthesis stability lipophilicity and cellular uptake evaluations of sup 131 sup i iodine α mangostin for breast cancer diagnosis and therapy |
| topic | [<sup>131</sup>I]I-alpha mangostin radiosynthesis evaluations |
| url | https://www.mdpi.com/1422-0067/24/10/8678 |
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