Synthesis, stability, and cellular uptake of 131I-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:	Isti Daruwati, Abednego Kristande Gwiharto, Ahmad Kurniawan, Isa Mahendra, Tri Hanggono Achmad, Mukh Syaifudin, Muchtaridi Muchtaridi
Formato:	article
Lenguaje:	EN
Publicado:	Elsevier 2021
Materias:	Estradiol Iodine-131 Estrogen receptor Chloramine T Cellular uptake Science (General) Q1-390 Social sciences (General) H1-99
Acceso en línea:	https://doaj.org/article/1ab9b020a26e4b4c88c84341edc3bca9
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spelling	oai:doaj.org-article:1ab9b020a26e4b4c88c84341edc3bca92021-12-02T05:03:13ZSynthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay2405-844010.1016/j.heliyon.2021.e08438https://doaj.org/article/1ab9b020a26e4b4c88c84341edc3bca92021-11-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S240584402102541Xhttps://doaj.org/toc/2405-8440Estradiol 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 131I-estradiol was perfomed by direct method using chloramine T as an oxidizer and by indirect labeling using 131I-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 131I-estradiol was succesfully obtained with radiochemical purity greater than 95% and more stable in the refrigerator until 21 days than freezer and room temperature. 131I-estradiol and 131I-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.Isti DaruwatiAbednego Kristande GwihartoAhmad KurniawanIsa MahendraTri Hanggono AchmadMukh SyaifudinMuchtaridi MuchtaridiElsevierarticleEstradiolIodine-131Estrogen receptorChloramine TCellular uptakeScience (General)Q1-390Social sciences (General)H1-99ENHeliyon, Vol 7, Iss 11, Pp e08438- (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Estradiol Iodine-131 Estrogen receptor Chloramine T Cellular uptake Science (General) Q1-390 Social sciences (General) H1-99
spellingShingle	Estradiol Iodine-131 Estrogen receptor Chloramine T Cellular uptake Science (General) Q1-390 Social sciences (General) H1-99 Isti Daruwati Abednego Kristande Gwiharto Ahmad Kurniawan Isa Mahendra Tri Hanggono Achmad Mukh Syaifudin Muchtaridi Muchtaridi Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
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 131I-estradiol was perfomed by direct method using chloramine T as an oxidizer and by indirect labeling using 131I-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 131I-estradiol was succesfully obtained with radiochemical purity greater than 95% and more stable in the refrigerator until 21 days than freezer and room temperature. 131I-estradiol and 131I-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	article
author	Isti Daruwati Abednego Kristande Gwiharto Ahmad Kurniawan Isa Mahendra Tri Hanggono Achmad Mukh Syaifudin Muchtaridi Muchtaridi
author_facet	Isti Daruwati Abednego Kristande Gwiharto Ahmad Kurniawan Isa Mahendra Tri Hanggono Achmad Mukh Syaifudin Muchtaridi Muchtaridi
author_sort	Isti Daruwati
title	Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_short	Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_full	Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_fullStr	Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_full_unstemmed	Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay
title_sort	synthesis, stability, and cellular uptake of 131i-estradiol against mcf7 and t-47d human cell lines as a radioligand for binding assay
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/1ab9b020a26e4b4c88c84341edc3bca9
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Synthesis, stability, and cellular uptake of 131I-estradiol against MCF7 and T-47D human cell lines as a radioligand for binding assay

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