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Radiosynthesis of [131I]I-Hesperidin: Optimization, physicochemical profiling, and computational insights for targeted radiopharmaceuticals.

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Title: Radiosynthesis of [131I]I-Hesperidin: Optimization, physicochemical profiling, and computational insights for targeted radiopharmaceuticals.
Authors: Munir, Miftakul1,2 (AUTHOR), Forentin, Alfian Mahardika1 (AUTHOR), Febrian, Muhammad Basit1 (AUTHOR), Fakih, Taufik Muhammad3,4 (AUTHOR), Utomo, Rohmad Yudi5,6 (AUTHOR), Aries, Arni1,7 (AUTHOR), Lestari, Wening1 (AUTHOR), Meiyanto, Edy6,8 (AUTHOR), Muchtaridi, Muchtaridi3,7 (AUTHOR), Septisetyani, Endah Puji9 (AUTHOR), Astirin, Okid Parama10 (AUTHOR), Syaifudin, Mukh1,7 (AUTHOR) mukh002@brin.go.id
Source: Applied Radiation & Isotopes. Nov2025, Vol. 225, pN.PAG-N.PAG. 1p.
Subjects: Hesperidin, Radiopharmaceuticals, Radioactive tracers, HER2 protein, Epidermal growth factor receptors, Iodine, Radiolabeling, Absorption (Physiology)
Abstract: Hesperidin, a citrus flavonoid, has been investigated for its potential health benefits, including anticancer. However, the study of hesperidin as a theranostic agent and its cancer cellular uptake is still lacking. Therefore, in this research, we developed radiolabeling methods of hesperidin with Iodine-131 (131I) for radiotracing and investigating its potential theranostic application. Here, we showed that the radiochemical purity of [131I]I-hesperidin prepared with chloramine-T in methanol or DMSO, iodogen, and iodobeads as a catalyst were 97.75, 79.08, 78.13, and 49.91 %, respectively. The LogP and plasma protein-binding after 24 h of [131I]I-hesperidin prepared by chloramine-T in methanol were 0.54 ± 0.02 and 51.01 %, respectively. It was also stable in PBS for up to two days (RCP>90 %). The cellular uptake assay demonstrated the high and rapid uptake of [131I]I- hesperidin in A549 cells (92.03 % in 30 min), relatively low uptake in MCF-7 (21.30 % in 1 h), and deficient uptake in MDA-MB-231 (3.64 %). Interaction and binding energies of [131I]I-hesperidin-b toward EGFR, HER2, ERα, and ERβ, were −169.910; −131.574; −152.623, and −184.844 kJ/mol, respectively. Considering that the cellular uptake was the highest in A549 cells among the tested cells, the cellular uptake may be related to both EGFR and HER2 receptors. In addition, the interaction and binding energy of [131I]I-hesperidin-b toward AKT1 was −150.939 kJ/mol, indicating the potential [131I]I-hesperidin-b intervention in EGFR/HER2 signaling. Our data suggest that [131I]I-hesperidin-b is a potential radiopharmaceutical, especially for lung cancers with EGFR and HER2 expression. However, further studies are still needed to evaluate the uptake mechanism of [131I]I-hesperidin at the molecular level. Hopefully, [131I]I-hesperidin will provide an opportunity to investigate the biodistribution, pharmacokinetics, and its potential as a targeted therapeutic-diagnostic agent supported with beta decay for cancer cell eradication. • Hesperidin can be radiolabeled with 131I using chloramine-T in methanol as a catalyst. • [131I]I-hesperidin is predicted to pose good cellular membrane penetration, high bioavailability, and rapid renal clearance. • [131I]I-hesperidin poses a high cellular uptake in cells with EGFR and HER2 receptor expression. [ABSTRACT FROM AUTHOR]
Copyright of Applied Radiation & Isotopes is the property of Pergamon Press - An Imprint of Elsevier Science and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
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DbLabel: Engineering Source
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  Data: Radiosynthesis of [131I]I-Hesperidin: Optimization, physicochemical profiling, and computational insights for targeted radiopharmaceuticals.
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  Data: <searchLink fieldCode="AR" term="%22Munir%2C+Miftakul%22">Munir, Miftakul</searchLink><relatesTo>1,2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Forentin%2C+Alfian+Mahardika%22">Forentin, Alfian Mahardika</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Febrian%2C+Muhammad+Basit%22">Febrian, Muhammad Basit</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Fakih%2C+Taufik+Muhammad%22">Fakih, Taufik Muhammad</searchLink><relatesTo>3,4</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Utomo%2C+Rohmad+Yudi%22">Utomo, Rohmad Yudi</searchLink><relatesTo>5,6</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Aries%2C+Arni%22">Aries, Arni</searchLink><relatesTo>1,7</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Lestari%2C+Wening%22">Lestari, Wening</searchLink><relatesTo>1</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Meiyanto%2C+Edy%22">Meiyanto, Edy</searchLink><relatesTo>6,8</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Muchtaridi%2C+Muchtaridi%22">Muchtaridi, Muchtaridi</searchLink><relatesTo>3,7</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Septisetyani%2C+Endah+Puji%22">Septisetyani, Endah Puji</searchLink><relatesTo>9</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Astirin%2C+Okid+Parama%22">Astirin, Okid Parama</searchLink><relatesTo>10</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Syaifudin%2C+Mukh%22">Syaifudin, Mukh</searchLink><relatesTo>1,7</relatesTo> (AUTHOR)<i> mukh002@brin.go.id</i>
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  Data: <searchLink fieldCode="JN" term="%22Applied+Radiation+%26+Isotopes%22">Applied Radiation & Isotopes</searchLink>. Nov2025, Vol. 225, pN.PAG-N.PAG. 1p.
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  Data: <searchLink fieldCode="DE" term="%22Hesperidin%22">Hesperidin</searchLink><br /><searchLink fieldCode="DE" term="%22Radiopharmaceuticals%22">Radiopharmaceuticals</searchLink><br /><searchLink fieldCode="DE" term="%22Radioactive+tracers%22">Radioactive tracers</searchLink><br /><searchLink fieldCode="DE" term="%22HER2+protein%22">HER2 protein</searchLink><br /><searchLink fieldCode="DE" term="%22Epidermal+growth+factor+receptors%22">Epidermal growth factor receptors</searchLink><br /><searchLink fieldCode="DE" term="%22Iodine%22">Iodine</searchLink><br /><searchLink fieldCode="DE" term="%22Radiolabeling%22">Radiolabeling</searchLink><br /><searchLink fieldCode="DE" term="%22Absorption+%28Physiology%29%22">Absorption (Physiology)</searchLink>
– Name: Abstract
  Label: Abstract
  Group: Ab
  Data: Hesperidin, a citrus flavonoid, has been investigated for its potential health benefits, including anticancer. However, the study of hesperidin as a theranostic agent and its cancer cellular uptake is still lacking. Therefore, in this research, we developed radiolabeling methods of hesperidin with Iodine-131 (131I) for radiotracing and investigating its potential theranostic application. Here, we showed that the radiochemical purity of [131I]I-hesperidin prepared with chloramine-T in methanol or DMSO, iodogen, and iodobeads as a catalyst were 97.75, 79.08, 78.13, and 49.91 %, respectively. The LogP and plasma protein-binding after 24 h of [131I]I-hesperidin prepared by chloramine-T in methanol were 0.54 ± 0.02 and 51.01 %, respectively. It was also stable in PBS for up to two days (RCP>90 %). The cellular uptake assay demonstrated the high and rapid uptake of [131I]I- hesperidin in A549 cells (92.03 % in 30 min), relatively low uptake in MCF-7 (21.30 % in 1 h), and deficient uptake in MDA-MB-231 (3.64 %). Interaction and binding energies of [131I]I-hesperidin-b toward EGFR, HER2, ERα, and ERβ, were −169.910; −131.574; −152.623, and −184.844 kJ/mol, respectively. Considering that the cellular uptake was the highest in A549 cells among the tested cells, the cellular uptake may be related to both EGFR and HER2 receptors. In addition, the interaction and binding energy of [131I]I-hesperidin-b toward AKT1 was −150.939 kJ/mol, indicating the potential [131I]I-hesperidin-b intervention in EGFR/HER2 signaling. Our data suggest that [131I]I-hesperidin-b is a potential radiopharmaceutical, especially for lung cancers with EGFR and HER2 expression. However, further studies are still needed to evaluate the uptake mechanism of [131I]I-hesperidin at the molecular level. Hopefully, [131I]I-hesperidin will provide an opportunity to investigate the biodistribution, pharmacokinetics, and its potential as a targeted therapeutic-diagnostic agent supported with beta decay for cancer cell eradication. • Hesperidin can be radiolabeled with 131I using chloramine-T in methanol as a catalyst. • [131I]I-hesperidin is predicted to pose good cellular membrane penetration, high bioavailability, and rapid renal clearance. • [131I]I-hesperidin poses a high cellular uptake in cells with EGFR and HER2 receptor expression. [ABSTRACT FROM AUTHOR]
– Name: AbstractSuppliedCopyright
  Label:
  Group: Ab
  Data: <i>Copyright of Applied Radiation & Isotopes is the property of Pergamon Press - An Imprint of Elsevier Science and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
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      – Type: doi
        Value: 10.1016/j.apradiso.2025.111977
    Languages:
      – Code: eng
        Text: English
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      Pagination:
        PageCount: 1
        StartPage: N.PAG
    Subjects:
      – SubjectFull: Hesperidin
        Type: general
      – SubjectFull: Radiopharmaceuticals
        Type: general
      – SubjectFull: Radioactive tracers
        Type: general
      – SubjectFull: HER2 protein
        Type: general
      – SubjectFull: Epidermal growth factor receptors
        Type: general
      – SubjectFull: Iodine
        Type: general
      – SubjectFull: Radiolabeling
        Type: general
      – SubjectFull: Absorption (Physiology)
        Type: general
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      – TitleFull: Radiosynthesis of [131I]I-Hesperidin: Optimization, physicochemical profiling, and computational insights for targeted radiopharmaceuticals.
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            – D: 01
              M: 11
              Text: Nov2025
              Type: published
              Y: 2025
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