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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...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2021
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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. |
format | Online Article Text |
id | pubmed-8637476 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
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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