Synthesis of &lt;sup&gt;125&lt;/sup&gt;I Labeled Estradiol-17β-Hemisuccinate and Its Binding Study to Estrogen Receptors Using Scintillation Proximity Assay Method

Susilo, Yarianto Sugeng Budi; Mondrida, Gina; Setiyowati, Sri; Sutari,; Triningsih,; Lestari, Wening; Widayati, Puji; Ardiyatno, C. N.; Ariyanto, Agus; Darwati, S.; Kardono, L.B.S.; Yanuar, Arry

doi:10.17146/aij.2012.175

Cited by 2 publications

(3 citation statements)

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“…[ 31 ] showed that ER level in T47-D was higher than ER level in MCF7 cell line. The cellular uptake of 125 I-his-estradiol has also been carried out by Susilo et al [ 18 ] with the SPA method and showed a significant binding to MCF7. In agreement with their study, this results confirmed that the higher the ER expression, the higher accumulation of 131 I-estradiol and 131 I-his-estradiol.…”

Section: Discussionmentioning

confidence: 96%

“…Indirect labeling of β-estradiol-17β-hemisuccinate using histamine with 125 I conducted by Susilo et al. resulted in a radiochemical purity of 97.8% [ 18 ]. On the other hand, Kumar et.…”

Section: Introductionmentioning

confidence: 99%

“…This synthesis was chosen because it is a relatively simple and easy for radiolabeling, but it is necessary to determine its stability after radiolabeling, due to the relatively short half-life of iodine-131 (8 days). As a comparison, the radiolabeling was also carried out by indirect method following the procedure of Susilo et al [ 18 ]. This radioligand was tested for its binding ability with two types of cancer cells to determine the ability of the radioligand to the estrogen receptor in these cells to prove that the radioligand had the same binding ability as the original estradiol.…”

Section: Introductionmentioning

confidence: 99%

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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

Daruwati

Gwiharto

Kurniawan

et al. 2021

Heliyon

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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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Section: Discussionmentioning

confidence: 96%

“…Indirect labeling of β-estradiol-17β-hemisuccinate using histamine with 125 I conducted by Susilo et al. resulted in a radiochemical purity of 97.8% [ 18 ]. On the other hand, Kumar et.…”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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