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Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay

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...

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Autores principales: Daruwati, Isti, Gwiharto, Abednego Kristande, Kurniawan, Ahmad, Mahendra, Isa, Achmad, Tri Hanggono, Syaifudin, Mukh, Muchtaridi, Muchtaridi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8637476/
https://www.ncbi.nlm.nih.gov/pubmed/34901495
http://dx.doi.org/10.1016/j.heliyon.2021.e08438
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author Daruwati, Isti
Gwiharto, Abednego Kristande
Kurniawan, Ahmad
Mahendra, Isa
Achmad, Tri Hanggono
Syaifudin, Mukh
Muchtaridi, Muchtaridi
author_facet Daruwati, Isti
Gwiharto, Abednego Kristande
Kurniawan, Ahmad
Mahendra, Isa
Achmad, Tri Hanggono
Syaifudin, Mukh
Muchtaridi, Muchtaridi
author_sort Daruwati, Isti
collection PubMed
description 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 (131)I-estradiol was perfomed by direct method using chloramine T as an oxidizer and by indirect labeling using (131)I-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 (131)I-estradiol was succesfully obtained with radiochemical purity greater than 95% and more stable in the refrigerator until 21 days than freezer and room temperature. (131)I-estradiol and (131)I-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.
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spelling pubmed-86374762021-12-09 Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay Daruwati, Isti Gwiharto, Abednego Kristande Kurniawan, Ahmad Mahendra, Isa Achmad, Tri Hanggono Syaifudin, Mukh Muchtaridi, Muchtaridi Heliyon Research Article 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 (131)I-estradiol was perfomed by direct method using chloramine T as an oxidizer and by indirect labeling using (131)I-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 (131)I-estradiol was succesfully obtained with radiochemical purity greater than 95% and more stable in the refrigerator until 21 days than freezer and room temperature. (131)I-estradiol and (131)I-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. Elsevier 2021-11-18 /pmc/articles/PMC8637476/ /pubmed/34901495 http://dx.doi.org/10.1016/j.heliyon.2021.e08438 Text en © 2021 The Author(s) https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Research Article
Daruwati, Isti
Gwiharto, Abednego Kristande
Kurniawan, Ahmad
Mahendra, Isa
Achmad, Tri Hanggono
Syaifudin, Mukh
Muchtaridi, Muchtaridi
Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_full Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_fullStr Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_full_unstemmed Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_short Synthesis, stability, and cellular uptake of (131)I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_sort synthesis, stability, and cellular uptake of (131)i-estradiol against mcf7 and t-47d human cell lines as a radioligand for binding assay
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8637476/
https://www.ncbi.nlm.nih.gov/pubmed/34901495
http://dx.doi.org/10.1016/j.heliyon.2021.e08438
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