Preprint Article Version 1 This version is not peer-reviewed

I-124 Labeled Anthraquinone-Derivative-Coating Gold Nanoparticles for Targeted Breast Cancer Diagnosis and Therapy

Version 1 : Received: 7 November 2024 / Approved: 7 November 2024 / Online: 7 November 2024 (15:43:02 CET)

How to cite: Lee, J. Y.; Park, J. H. I-124 Labeled Anthraquinone-Derivative-Coating Gold Nanoparticles for Targeted Breast Cancer Diagnosis and Therapy. Preprints 2024, 2024110557. https://doi.org/10.20944/preprints202411.0557.v1 Lee, J. Y.; Park, J. H. I-124 Labeled Anthraquinone-Derivative-Coating Gold Nanoparticles for Targeted Breast Cancer Diagnosis and Therapy. Preprints 2024, 2024110557. https://doi.org/10.20944/preprints202411.0557.v1

Abstract

Background: Rhein, an anthraquinone derivative, and gold nanoparticles have demonstrated significant potential in facilitating the theranostics of breast cancer. Rhein inhibits breast cancer by exhibiting a strong binding affinity to the estrogen receptor. In addition, gold nanoparticles, when used as nanocarriers, may enhance the therapeutic effects against breast cancer. This study out-lines the preparation of [124I]rhein-gold for position emission tomography (PET) imaging in a breast cancer mouse model. Method: Gold nanoparticles (30 nm) were prepared using the citrate reduction method. Second, the anthraquinone derivative rhein-cysteine complex was synthesized using the carbodiimide coupling method. Third, the radiosynthesis of [124I]rhein-Cys-gold nanocomposites (RCGs) was performed using the chloramine T method. Specifically, 1 mg of RCGs in dimethylformamide was mixed with Na124I (37 MBq) at pH 12 along with chloramine T (5 mg). The reaction was allowed to proceed for 15 min at room temperature. To remove free 124I, the mixture was purified via centrifugation for 10 min at 10,000 rpm. Results: The radiochemical yield of [124I]RCGs was 65% ± 8.2%, with a radiochemical purity of > 98%. In vivo [124I]RCGs targeted MCF-7 cells in a hormone-dependent manner, with cellular uptake values of 25.4 ± 1.59% at 15 min, 27.1 ± 1.27% at 30 min, 28.6 ± 0.38% at 60 min, and 15.97 ± 0.66% at 120 min. In vivo small-animal PET images of [124I]RCGs showed significant uptake in human breast cancer and MCF-7 tumors. Conclusion: This study demonstrated the synthesis and biological evaluation of [124I]RCGs. [124I]RCGs showed high cellular uptake in a time-dependent manner. PET images of [124I]RCGs confirmed their high affinity for MCF-7 tumors in mice from 1 h to 24 h. These results suggest that [124I]RCGs are promising radiopharmaceuticals, demonstrating potential both as an imaging agent and therapeutic option for estrogen-receptor-targeted breast cancer treatment.

Keywords

breast cancer; anthraquinone; Iodine-124; gold nanoparticle

Subject

Chemistry and Materials Science, Inorganic and Nuclear Chemistry

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