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Synthesis of 125I Labeled Estradiol-17β-Hemisuccinate and Its Binding Study to Estrogen Receptors Using Scintillation Proximity Assay Method

Atom Indonesia · Vol. 38 No. 3 (2013) · hlm. 112–117

DOI
10.17146/aij.2012.175
ISSN
2356-5322, 0126-1568
Terbit
2013-02-12
Penerbit
National Research and Innovation Agency
Bahasa
eng
Lisensi
creativecommons.org/licenses/by-nc-sa/4.0

Abstrak

Research was carried out to obtain a selective ligand which strongly bind to estrogen receptors through determination of binding affinity of estradiol-17β-hemisuccinate. Selectivity of these compounds for estrogen receptor was studied using Scintillation Proximity Assay (SPA) method. Primary reagents required in the SPA method including radioligand and receptor, the former was obtained by labeling of estradiol-17β-hemisuccinate with 125I, while MCF7 was used as the receptor. The labeling process was performed by indirect method via two-stage reaction. In this procedure, first step was activation of estradiol-17β-hemisuccinate using isobutylchloroformate and tributylamine as a catalist, while labeling of histamine with 125I was carried out using chloramin-T method to produce 125I-histamine. The second stage was conjugation of activated estradiol-17β-hemisuccinate with 125I-histamine. The product of estradiol-17β-hemisuccinate labeled 125I was extracted using toluene. Furtherly, the organic layer was purified by TLC system. Characterization of estradiol-17β-hemisuccinate labeled 125I from this solvent extraction was carried out by determining its radiochemical purity and the result was obtained using paper electrophoresis and TLC were 79.8% and 84.4% respectively. Radiochemical purity could be increased when purification step was repeated using TLC system, the result showed up to 97.8%. Determination of binding affinity by the SPA method was carried out using MCF7 cell lines which express estrogen receptors showed the value of Kd at 7.192 x 10-3 nM and maximum binding at 336.1 nM. This low value of Kd indicated that binding affinity of estradiol-17β-hemisuccinate was high or strongly binds to estrogen receptor.Received: 04 December 2012; Revised: 19 December 2012; Accepted: 21 December 2012

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  • National Nuclear Energy Agency of Indonesia
  • University of Indonesia
  • Padjadjaran University
  • Universitas Halu Oleo
  • Universitas Muhammadiyah Prof Dr Hamka
  • Indonesian Institute of Sciences
  • Indonesia Defense University
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Rekan penulisOrganisasiArtikel bersama
Veronika Yulianti SusiloNational Nuclear Energy Agency of Indonesia8
Triningsih TriningsihNational Nuclear Energy Agency of Indonesia8
Martalena RamliNational Nuclear Energy Agency of Indonesia6
Ratna Dini HaryuniNational Nuclear Energy Agency of Indonesia3
Abdul MutalibPadjadjaran University3
Rien RitawidyaNational Nuclear Energy Agency of Indonesia3
Setiawan SetiawanAfiliasi tidak diketahui2
Dede KurniasihNational Nuclear Energy Agency of Indonesia2
Anung PujiyantoNational Nuclear Energy Agency of Indonesia2
Mujinah MujinahNational Nuclear Energy Agency of Indonesia2
Witarti WitartiNational Nuclear Energy Agency of Indonesia2
Sandra HermantoSyarif Hidayatullah State Islamic University Jakarta1
Yahdiana HarahapIndonesia Defense University1
Sunarhadijoso SoenarjoNational Nuclear Energy Agency of Indonesia1
Anton BahtiarUniversity of Indonesia1
D. HaffidNational Nuclear Energy Agency of Indonesia1
Aisyah ElliyantiAndalas University1
Johan S. MasjhurPadjadjaran University1
Tri Hanggono AchmadPadjadjaran University1
Fadlina Chany SaputriUniversity of Indonesia1
Ni Putu Ermi HikmawantiUniversitas Muhammadiyah Prof Dr Hamka1
Ratih Asmana NingrumNational Research and Innovation Agency1
Abdul Mun’imUniversity of Indonesia1
Hayati HayatiUniversitas Muhammadiyah Prof Dr Hamka1
Titis Sekar HumaniNational Nuclear Energy Agency of Indonesia1
Muhammad ArbaUniversitas Halu Oleo1
Sanang Nur SafitriUniversitas Halu Oleo1
Andry Nur HidayatUniversitas Halu Oleo1

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Sumber metadata: OAI-PMH (metadata jurnal) https://atomindonesia.brin.go.id/index.php/aij/oai, pertama di-harvest 8 Nov 2026, terakhir terlihat 8 Nov 2026.
Metadata asli (oai_dc) 
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	<dc:title xml:lang="en-US">Synthesis of 125I Labeled Estradiol-17β-Hemisuccinate and Its Binding Study to Estrogen Receptors Using Scintillation Proximity  Assay Method</dc:title>
	<dc:creator>Susilo, Y.</dc:creator>
	<dc:creator>Mondrida, G.</dc:creator>
	<dc:creator>Setiyowati, S.</dc:creator>
	<dc:creator>Sutari, Sutari</dc:creator>
	<dc:creator>Triningsih, Triningsih</dc:creator>
	<dc:creator>Lestari, W.</dc:creator>
	<dc:creator>Widayati, P.</dc:creator>
	<dc:creator>Ardiyatno, C.N.</dc:creator>
	<dc:creator>Ariyanto, A.</dc:creator>
	<dc:creator>Darwati, S.</dc:creator>
	<dc:creator>Kardono, L.B.S.</dc:creator>
	<dc:creator>Yanuar, A.</dc:creator>
	<dc:subject xml:lang="en-US">Indirect labeling, Estrogen receptor, Estradiol, Scintillation proximity assay, Binding affinity, MCF7</dc:subject>
	<dc:description xml:lang="en-US">Research was carried out to obtain a selective ligand which strongly bind to estrogen receptors through determination of binding affinity of estradiol-17β-hemisuccinate. Selectivity of these compounds for estrogen receptor was studied using Scintillation Proximity Assay (SPA) method. Primary reagents required in the SPA method including radioligand and receptor, the former was obtained by labeling of estradiol-17β-hemisuccinate with 125I, while MCF7 was used as the receptor. The labeling process was performed by indirect method via two-stage reaction. In this procedure, first step was activation of estradiol-17β-hemisuccinate using isobutylchloroformate and tributylamine as a catalist, while labeling of histamine with 125I was carried out using chloramin-T method to produce 125I-histamine. The second stage was conjugation of activated estradiol-17β-hemisuccinate with 125I-histamine. The product of estradiol-17β-hemisuccinate labeled 125I was extracted using toluene. Furtherly, the organic layer was purified by TLC system. Characterization of estradiol-17β-hemisuccinate labeled 125I from this solvent extraction was carried out by determining its radiochemical purity and the result was obtained using paper electrophoresis and TLC were 79.8% and 84.4% respectively. Radiochemical purity could be increased when purification step was repeated using TLC system, the result showed up to 97.8%. Determination of binding affinity by the SPA method was carried out using MCF7 cell lines which express estrogen receptors showed the value of Kd at 7.192 x 10-3 nM and maximum binding at 336.1 nM. This low value of Kd indicated that binding affinity of estradiol-17β-hemisuccinate was high or strongly binds to estrogen receptor.Received: 04 December 2012; Revised: 19 December 2012; Accepted: 21 December 2012</dc:description>
	<dc:publisher xml:lang="en-US">National Research and Innovation Agency</dc:publisher>
	<dc:contributor xml:lang="en-US">National Nuclear Energy Agency of Indonesia</dc:contributor>
	<dc:date>2013-02-12</dc:date>
	<dc:type>info:eu-repo/semantics/article</dc:type>
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	<dc:format>application/pdf</dc:format>
	<dc:identifier>https://atomindonesia.brin.go.id/index.php/aij/article/view/175</dc:identifier>
	<dc:identifier>10.17146/aij.2012.175</dc:identifier>
	<dc:source xml:lang="en-US">Atom Indonesia; Vol 38, No 3 (2012): December 2012; 112-117</dc:source>
	<dc:source>2356-5322</dc:source>
	<dc:source>0126-1568</dc:source>
	<dc:source>10.17146/aij.2012.%x</dc:source>
	<dc:language>eng</dc:language>
	<dc:relation>https://atomindonesia.brin.go.id/index.php/aij/article/view/175/127</dc:relation>
	<dc:rights xml:lang="en-US">Copyright (c) 2016 Atom Indonesia</dc:rights>
	<dc:rights xml:lang="en-US">http://creativecommons.org/licenses/by-nc-sa/4.0</dc:rights>
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