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"One of the major health problems in elderly women is osteoporosis post menopause. Dentists must be aware of the disease since its involvement on the jaw. Nowadays, there are a lot of researches on correlation of osteoporosis and mandible but only few concentrate on hormonal substitution therapy and/or Calcium-vitamin D3 (Ca-vit D3). This research is to evaluate the effect of hormonal substitution therapy and/or Ca-vit D3 on mandibular height. Forty five rats are used in this research and divided into nine groups: one control group, two ovariectomized (OVX) groups, two OVX groups treated with estrogen, two OVX groups treated with Ca-vit D3, two OVX groups treated with estrogen and Ca-vit D3. All of the rats except the control groups were ovariectomized as model for pstmenopausal estrogen deficiency state. The treatment was done in two or four weeks. The animals were killed with cervical discoloration, the mandible were excised and soaked on Hydrogen Peroxide 10%. Then the mandible's heights on right buccal side were measured from the mandibular base to the alveolar crest. It is concluded that hormonal substitution therapy and combination of the hormonal substitution therapy and Ca-vit D3 can maintain the normal mandibular height. Mandibular height of groups with therapy using Ca-vit D3 have slightly lower means compared to control group but without significant difference statistically. The best therapy is combination of hormonal substitution therapy and Ca-vit D3."

"During three months ,August 1991 until November 1991, the randomized clinical trial study was conducted to elucidate the effect of calcium supplementation on calcium metabolism to prevent bone loss ip postmenopausal women. Thirty four postmeno- pausal women age 55 to 65 years old from RN. 01, Panjunan village, Astanaanyar subdistrict, Bandung regency West Java who had undergone menopause at least five years since last menses were recruited to the study. The subjects were randomly assigned to the treatment (1000 mg calcium/day) and the control groups in a double blind designs.Thirty one subjects who remained in the study consist of sixteen treatment subjects and fifteen control subjects were included in the final data analysis. Baseline data of the study showed no a significant difference for all variables, therefore baseline data were homogenous. Based on two x 24 hours dietary recall methods all subjects had low dietary calcium intake (291.5l mg/ day and 289.32 mg/day).After treatment, based on the laboratory tests show that the serum calcium concentration was significantly increased in the treatment group (p<0.001) and was not significant difference (p=O.596) in the control group. Serum calcium was a significant difference (p<0.001) between the treatment and the control group. Parathyroid hormone level was significantly decreased in the treatment group (p<0.05) and was significantly increased in the control group (p<0.01). There was significant difference (p<0.00l) between the treatment and the control group. Bone loss of radius and ulna were determined by z-ray standard measurement were significantly reduced (p<0.001 and p<0.01, respectively) after 1000 mg calcium supplementation. Alkaline phosphatase was significantly decreased (p<0.001) in the treatment group and was significantly increased in the control group. There was significant difference (p<0.001) between the treatment and the control group. Urinary ca}cium creatinine ratio was not significantly increased (pI0.764 and p=0.0BB) and was not significant difference (p=0.067) in all subjects after treatment. This study support the hypothesis that calcium supplementation can maintain calcium balance, even improved bone density in postmenopausal women."

"The need for women to use a dental prosthesis increases with age. Low estrogen level is characteristic in post menopausal women. In this case, it often related with reduction of density and mandibular alveolar bone height. This study aimed to investigate the differences in density and mandibular alveolar bone height in post-menopausal women wearing complete dentures with tissue conditioner. The clinical observations were conducted on seven persons who had received a new set of complete denture in the Prosthodontic Department of the Dental Hospital of the Dental Faculty in Jember University. Balanced occlusion was used in all dentures, fabricated according to the principles used in the department. Panoramic radiographs had been made for all subjects as the baseline, and two, four, and six months later using dentures with tissue conditioner. The data was analyzed by using one-way analysis of variance at the 0.05 level. The conclusion was that there is no significant difference in density and mandibular alveolar bone height of complete denture wearers with tissue conditioner in post-menopausal women."

"Ruang Lingkup dan Cara Penelitian: Usia lanjut berkaitan dengan peningkatan progresif risiko penyakit neurodegenerasi. 7% dari kelompok usia lanjut menunjukkan penurunan fungsi kognitif Dasar patologi penurunan fungsi kognitif antara lain disebabkan oleh berkurangnya sinap, neuron, neurotransmitter dan jejaring saraf. Proses regenerasi berkaitan dengan sinyal-sinyal penting seperti faktor neurotrofik, neurotransmitter dan barman. Proses neurodegenerasi dapat dihindari dengan memberikan rangsangan tertentu diantaranya estrogen sebagai hormon multiefek. Estrogen mempengaruhi jaringan saraf melalui mekanisme genom dan non genom diantaranya dengan menghasilkan BDNF (Brain derived neurotrophic factor). BDNF merupakan salah satu substansi dalam pengaturan neurogenesis. Penelitian ini merupakan studi ekperimental untuk meneliti kadar BDNF dan jumlah sel saraf pada kultur jaringan hipokampus tikus betina muda.Pengukuran kadar BDNF dengan spektrofotometer pada panjang gelombang 450 nm dengan kit BDNF dan Chemikon. Jumlah sel saraf dihitung perlapang pandang besar. Data dianalisis dengan uji t dependent, uji korelasi pm-son, dan sebelumnya diuji normalitas data dengan uji Shapiro Wilk.Hasil dan Kesimpulan: Dari penelitian ini diperoleh hasil (1) jumlah sel saraf lebih besar pada kultur jaringan hipokampus tikus betina muda yang diberi estrogen disbanding kontrol (p"

"Latar belakang: Prediabetes merupakan keadaan dengan kadar gula darah diantara normal dan diabetes. Salah satu komplikasi prediabetes adalah urolithiasis. Berbagai studi telah mengemukakan peran vitamin D dalam memodifikasi risiko prediabetes. Penelitian ini bertujuan untuk menganalisis pengaruh suplementasi vitamin D3 dalam mencegah urolithiasis pada kondisi prediabetes.Metode: Penelitian ini dilakukan pada 24 ekor tikus Wistar. Sebanyak 18 ekor tikus diberikan diet tinggi lemak dan tinggi glukosa (DTL-G) untuk menginduksi kondisi prediabetes dan 6 ekor tikus sehat diberikan diet standar selama tiga minggu. Pada akhir minggu ketiga, tikus prediabetes diinjeksi streptozotocin dan dibagi menjadi tiga kelompok yaitu: (1) kelompok prediabetes dengan DTL-G, (2) kelompok prediabetes dengan suplementasi vitamin D3 100 IU/kg/hari dan DTL-G, dan (3) kelompok prediabetes dengan suplementasi vitamin D3 1000 IU/kg/hari dan DTL-G selama 12 minggu. Tikus sehat diberikan diet normal selama 12 minggu. Pengumpulan urin 24 jam dilakukan untuk mengukur kadar kalsium dan pH urin.Hasil: Pemberian DTL-G tampak meningkatkan kadar kalsium urin tikus prediabetes. Pemberian vitamin D dosis 100 IU/kg/hari dan 1000 IU/kg/hari tampak meningkatkan kadar kalsium urin tikus prediabetes. pH urin pada kelompok prediabetes tampak meningkat dibandingkan kelompok sehat. Perbedaan kadar kalsium dan pH urin ditemukan tidak signifikan secara statistik.Kesimpulan: Suplementasi Vitamin D3 dosis 100 IU/kg/hari dan 1000 IU/kg/hari tidak memberikan perbedaan pada kadar kalsium dan derajat keasaman (pH) urin tikus prediabetes yang signifikan secara statistik.

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Introduction: Prediabetes is a condition with blood sugar levels between normal and diabetes. One of the complications of prediabetes is urolithiasis. Various studies have suggested the role of vitamin D in modifying the risk of prediabetes. This studi analyzes the effect of vitamin D3 supplementation in preventing urolithiasis caused by prediabetes.

Method: This experiment was conducted on 24 Wistar rats. A total of 18 rats were given a high-fat and high-glucose diet (HFD-G) to induce prediabetes and 6 healthy rats were given a normal diet. At the end of the third week, prediabetic rats were injected with streptozotocin and intervened in three groups: (1) HFD-G, (2) vitamin D 100 IU/kg/day and HFD-G, and (3) vitamin D 1000 IU/kg/day and HFD-G for 12 weeks. Healthy rats were given a normal diet for 12 weeks. 24-hour urine was collected to measure urinary calcium levels and pH.

Result: Administration of HFD-G increases urinary calcium levels in prediabetic rats. Administration of vitamin D 100 IU/kg/day and 1000 IU/kg/day increases urinary calcium levels in prediabetic rats. The urine pH of the prediabetic rats increases compared to the healthy rats. However, differences in urinary calcium levels and pH were not found to be statistically significant. Conclusion: Vitamin D3 100 IU/kg/day and 1000 IU/kg/day supplementation did not give a statistically significant difference in urinary calcium levels and pH of prediabetic rats."

"Pendahuluan: Jenis perawatan untuk memperbaiki deformitas dentokraniofasial pada pasien yang masih di dalam fase tumbuh kembang berbeda dengan pasien usia dewasa. Estimasi usia skeletal telah dikembangkan untuk mendapatkan estimasi status pertumbuhan seseorang, namun masih bersifat rerata dan subjektif sehingga menimbulkan ketertarikan terhadap biomarker molekuler. Estradiol (E2) merupakan hormon yang berperan dalam proses maturasi saat akhir pertumbuhan manusia dengan cara menginduksi osifikasi pada lempeng pertumbuhan. Kartilago kondil mandibula mencit sebagai salah satu titik pusat pertumbuhan dentokraniofasial diteliti untuk dilihat ekspresi E2 sebagai kandidat biomarker. Tujuan: Menganalisis ekspresi biomarker E2 melalui estrogen reseptor alfa (ERa) pada kondil mandibula di akhir masa pertumbuhan mencit jantan C57BL. Metode: Sampel penelitian merupakan spesimen kondil mencit C57BL jantan pada masa puncak pertumbuhan (usia 28 hari), awal dari akhir pertumbuhan (usia 56 hari), dan akhir pertumbuhan (usia 84 hari). Spesimen dilakukan dilakukan uji immunohistokimia untuk melihat ekspresi E2 melalui ERa pada kondil mencit C57BL. Ekspresi ERa kemudian dikuantifikasi menggunakan Image-J dan dilakukan uji statistik. Hasil: Tidak ditemukan ekspresi ERa pada kelompok usia 28 hari. Ditemukan ekspresi positif lemah ERa pada kelompok 56 hari dan 84 hari dengan ekspresinya semakin meningkat seiring bertambahnya usia. Terdapat perbedaan yang signifikan secara statistik mengenai ekspresi ERa diantara ketiga kelompok usia mencit. Kesimpulan: ERa dapat dijadikan kandidat biomarker untuk menilai periode puncak pertumbuhan kondil mandibula.

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Introduction: The type of treatment to correct dentocraniofacial deformities in patients who are still in the growth and development phase is different from adult patients. Skeletal age estimation has been developed to estimate a person's growth status, but is still average and subjective, giving rise to interest in molecular biomarkers. Estradiol (E2) is a hormone that plays a role in the maturation process at the end of human growth by inducing ossification in the growth plate. The mandibular condylar cartilage of mice as one of the central points of dentocraniofacial growth was studied to see the expression of E2 as a candidate biomarker. Objective: To analyze the expression of the E2 biomarker through estrogen receptor alpha (ERa) in the mandibular condyle at the end of the growth period of male C57BL mice. Methods: The research samples were condylar specimens of male C57BL mice at the peak growth period (28 days of age), the beginning of the end of growth (56 days of age), and the end of growth (84 days of age). Specimens were subjected to immunohistochemical testing to see the expression of E2 through ERa in the condyles of C57BL mice. ERa expression was then quantified using Image-J and statistical tests were carried out. Results: No ERa expression was found in the 28 day age group. There was a weak positive expression of ERa in the 56 day and 84 day groups with the expression increasing with age. It was found that there were statistically significant differences regarding ERa expression between the three age groups of mice. Conclusion: ERa can be used as a candidate biomarker to assess the peak period of mandibular condyle growth."

"Banyak penelitian di berbagai belahan dunia menunjukkan bahwa nilai asupan kalsium dan vitamin D ibu hamil masih jauh di bawah nilai rekomendasi. Padahal, kalsium memiliki peranan penting dalam proses pembentukan tulang janin selama kehamilan. Penelitian ini bertujuan untuk mengetahui kadar kalsium darah ibu hamil pada trimester I dan hubungannya dengan asupan kalsium dan vitamin D. Studi potong lintang dipilih terhadap 120 subjek data sekunder ibu hamil trimester pertama di RSIA Bunda dan RSIA Budi Kemuliaan tahun 2013-2014. Data asupan kalsium dan vitamin D diperoleh dengan bantuan food frequency questionnaire FFQ. Sementara itu, data kadar kalsium darah diperoleh dengan menggunakan pemeriksaan laboratorium standar. Pengolahan data secara deskriptif dan analitik dilakukan dengan menggunakan SPSS for windows versi 20. Hasil penelitian menunjukkan bahwa ibu hamil memiliki nilai tengah usia 28 19-35 tahun, berpendidikan tinggi 53,5, memiliki pekerjaan 58,3, dan memiliki pendapatan tinggi 86,7. Nilai tengah asupan kalsium, asupan vitamin D, dan kadar kalsium darah ibu hamil berturut-turut adalah 418,9 20,5-1820,6 mg/hari, 1,9 0,0-6,9 mcg/hari, dan 8,9 8,1-10,1 mg/dL. Hasil uji korelasi Spearman menunjukkan bahwa tidak ada korelasi bermakna baik antara asupan kalsium dengan kadar kalsium darah ibu hamil r=0,114; p=0,215, maupun antara asupan vitamin D dengan kadar kalsium darah ibu hamil r=0,103; p=0,265.

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Many studies show that maternal calcium and vitamin D intake are still below the recommendation value. Whereas, calcium has important role in skeletal formation during pregnancy. This study was held to know maternal blood calcium level among the first trimester and its relation with calcium and vitamin D intake.

Cross sectional study was chosen to examine 120 data subjects from secondary data of 1st trimester pregnant women in RSIA Bunda and RSIA Budi Kemuliaan year 2013 2014. Data of calcium and vitamin D intake was collected using food frequency questionnaire FFQ. Besides, data of blood calcium level was analyzed by standard laboratory equipment. SPSS for windows version 20 was used to analyze the data descriptively and analytically.

The results show that pregnant women have median of age 28 19 35 years, high educated 53.5, worker 58.3, and having high income 86.7. The median value of calcium intake, vitamin D intake, and blood calcium level are 418.9 20.5 182.6 mg day, 1.9 0.0 6.9 mcg day, and 8.9 8.1 10.1 mg dL respectively.

The result of Spearman correlation test shows unsignificant correlation between calcium intake and bloood calcium level r 0.114 p 0.215, as well as between vitamin D intake and blood calcium level r 0.103 p 0.265. "

"Senyawa dengan inti stilben yang dapat digunakan sebagai terapi hormon pada penderita osteoporosis pascamenopause diduga terdapat dalam akar kelembak (Rheum officinale Baill.). Tujuan penelitian ini adalah untuk membuktikan secara ilmiah efek pemberian ektrak etanol 70% akar kelembak terhadap peningkatan kadar kalsium tulang tikus melalui pengukuran menggunakan spektrofotometer serapan atom. Sejumlah 36 ekor tikus putih betina Sprague-Dawley dibagi menjadi 6 kelompok perlakuan yaitu sham, kontrol negatif, kontrol positif, dosis 1, dosis 2, dan dosis 3. Berturut-turut, ke-6 kelompok tersebut mendapatkan CMC Na 0,5% 3 ml/200 g bb tikus, CMC Na 0,5% 3 ml/200 g bb tikus, tamoksifen dengan dosis 0,4 mg/200 g bb tikus, ekstrak akar kelembak dengan dosis 7 mg/200 g bb tikus, ekstrak akar kelembak dengan dosis 35 mg/200 g bb tikus, dan ekstrak akar kelembak dengan dosis 175 mg/200 g bb tikus. Semua kelompok kecuali kelompok sham diovariektomi untuk mendapatkan kondisi osteoporosis pascamenopause. Setelah ovariektomi, semua tikus diistirahatkan selama 21 hari, kemudian dilanjutkan dengan pemberian bahan uji selama 28 hari secara peroral. Setelah 28 hari pemberian bahan uji, dilakukan pengukuran kadar kalsium tulang. Hasil yang didapatkan menunjukkan bahwa kadar kalsium tulang meningkat dengan bertambahnya dosis pemberian ekstrak. Selain itu, pemberian dosis 175 mg/200 g bb tikus/hari dapat meningkatkan kadar kalsium tulang secara bermakna (p<0,05).

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Stilbene compounds that can be used as a hormone therapy in patients with postmenopausal osteoporosis, allegedly found in rhubarb root ( Rheum officinale Baill.). The purpose of this study is to scientifically prove the effects of 70 % ethanol extract of rhubarb root on rat bone calcium levels through atomic absorption spectrophotometer measurements. A total of 36 female white rats of Sprague-Dawley were divided into 6 groups: sham, negative control, positive control, dose 1, dose 2, and dose 3. Successively, all 6 groups receive CMC Na 0.5 % 3 ml/200 g bw mice, CMC Na 0.5 % 3 ml/200 g bw mice, tamoxifen, rhubarb root extract at a dose of 7 mg/200 g bw mice, rhubarb root extract at a dose of 35 mg/200 g bw mice, and rhubarb root extract at a dose of 175 mg/200 g bw rat. All groups, except the sham, is ovariectomized to obtain the conditions of postmenopausal osteoporosis. After ovariectomy, all rats rested for 21 days, followed by administration of the test substance orally for 28 days. After 28 days of administration, measured levels of bone calcium. The results showed that the bone calcium levels increased with increasing doses of the extract. In addition, rhubarb root extract at dose 175 mg/200 g bw/day can increase the level of bone calcium significantly (p<0.05 )."

"Osteoporosis adalah penyakit yang ditandai dengan adanya penurunan massa tulang yang parah sehingga meningkatkan risiko terjadinya retak atau patah tulang. Penelitian sebelumnya menunjukkan bahwa pemberian aspirin dosis tinggi (300 mg) terbukti dapat menurunkan kadar Sphingosine-1-Phosphate (S1P) dalam plasma. Kadar rendah S1P dalam darah dapat mengaktifkan S1PR1 yang dapat mengarahkan prekursor osteoklas kembali ke darah sehingga proses osteoklastogenesis dapat terhambat. Penelitian ini dilakukan untuk mengevaluasi pengaruh pemberian aspirin dengan kombinasi kalsium secara in vivo. Penelitian ini menggunakan tikus putih betina Sprague-Dawley yang dibagi menjadi 8 kelompok, yaitu sham dan kontrol negatif yang diberikan 1ml CMC Na 0,5%, kontrol positif diberikan tamoksifen sitrat 3,6 mg/200 g BB/hari, kelompok aspirin diberikan aspirin 5,4 mg/200 g BB/hari, kelompok kalsium diberikan kalsium sitrat 15 mg/200 g BB/hari, serta 3 kelompok variasi dosis aspirin dalam kombinasi dengan kalsium sitrat yaitu D1 aspirin 1,8 mg/200 g BB/hari, D2 aspirin 5,4 mg/200 g BB/hari, D3 aspirin 16,2 mg/200 g BB/hari dimana ketiga variasi dosis tersebut dikombinasikan dengan dosis kalsium sitrat 15 mg/200 g BB/hari secara peroral. Semua tikus dilakukan ovariektomi, kecuali kelompok sham dilakukan pembedahan tanpa pengambilan ovarium. Tikus dipelihara 4 minggu pasca operasi, lalu diberi perlakuan selama 28 hari. Parameter pertama yang diukur adalah berat tulang tibia dengan rata-rata kelompok sham 321,90 ± 10,39 mg, kontrol negatif 272,300 ± 54,18 mg, kontrol positif 312,50 ± 40,86 mg, aspirin 336,67 mg, kalsium 335, 90 ± 60,66 mg, D1 346,27 ± 83,90 mg, D2 377,00 ± 36,10 mg, dan D3 336,67 ± 4,5 mg. Parameter kedua yang diukur adalah kadar kalsium dengan rata-rata kelompok kelompok sham 111,08 ± 4,74 mg, kontrol negatif 89,30 ± 23,94 mg, kontrol positif 109,69 ± 20,25 mg, aspirin 123,01 ± 17,98 mg, kalsium 124,53 ± 32,11 mg, D1 120,19 ± 3,63 mg, D2 149,22 ± 17,13 mg, dan D3 121,60 ± 5,21 mg. Berdasarkan penelitian, pengaruh pemberian dosis kombinasi aspirin 5,4 mg/200 g BB/hari dan dosis kalsium 15 mg/200 g BB/hari pada tikus dapat meningkatkan berat dan kadar kalsium tulang tibia secara efektif.

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Osteoporosis is a disease characterized by a severe decrease in bone mass that increases the risk of fractures. Previous studies have shown that high-dose aspirin (300 mg) has been shown to reduce plasma levels of Sphingosine-1-Phosphate (S1P). Low levels of S1P in the blood can activate S1PR1 which can direct osteoclast precursors back to the blood so that the process of osteoclastogenesis can be inhibited. This study was conducted to evaluate the effect of aspirin and calcium combination in vivo. This study used female Sprague-Dawley rats which were divided into 8 groups, namely sham and negative control which were given 1ml CMC Na 0.5%, positive control was given tamoxifen citrate 3.6 mg/200 g BW/day, aspirin group was given aspirin. 5.4 mg/200 g BW/day, the calcium group was given calcium citrate 15 mg/200 g BW/day, as well as 3 groups with variations in the dose of aspirin in combination with calcium citrate, namely D1 aspirin 1.8 mg/200 g BW/day, D2 aspirin 5.4 mg/200 g BW/day, D3 aspirin 16.2 mg/200 g BW/day where the three variations of the dose were combined with a dose of calcium citrate 15 mg/200 g BW/day. All rats were ovariectomized, except for the sham group which underwent surgery without removing the ovaries. After 4 weeks of ovariectomy, rats were treated for 28 days orally. The first parameter that was measured was the mass of the tibia bone with the average for bone mass in each group are 321.90 ± 10.39 mg for sham group, 272.300 ± 54.18 mg for negative control, 312.50 ± 40.86 mg for positive control, 336.67 mg for aspirin group, 335, 90 ± 60.66 mg for calcium group, 346.27 ± 83.90 mg for D1, 377.00 ± 36.10 mg for D2, and 336.67 ± 4.5 mg for D3. The second parameter measured was calcium levels with the average for calcium levels in each group are 111.08 ± 4.74 mg for sham group, 89.30 ± 23.94 mg for negative control, 109.69 ± 20.25 mg for positive control, 123.01 ± 17.98 mg for aspirin group, 124.53 ± 32.11 mg for calcium group, 120.19 ± 3.63 mg for D1, 149.22 ± 17.13 mg for D2, and 121.60 ± 5.21 mg for D3. Based on the research, the effect of a combination dose of aspirin 5.4 mg/200 g BW/day and calcium dose 15 mg/200 g BW/day in rats can increase the weight and calcium levels of the tibia bone effectively."

"ABSTRAKTelah dilakukan penelitian untuk mendapatkan ligan yang selektif dan berikatan kuat dengan reseptor estrogen melalui pengujian afinitas ikatan senyawa estradiol-17β-hemisuksinat. Untuk meningkatkan status senyawa tersebut menjadi kandidat senyawa aktif obat kanker payudara perlu diketahui selektifitasnya terhadap reseptor estrogen dengan metode Scintillation Proximity Assay (SPA). Reagen primer yang diperlukan dalam metode SPA adalah radioligan dan reseptor, dan dilakukan penandaan estradiol-17β-hemisuksinat dengan 125I sebagai radioligan. Studi ikatan radioligan dilakukan terhadap reseptor estrogen meggunakan sel MCF7. Penandaan dilakukan secara tidak langsung dengan dua tahap. Pertama dilakukan aktivasi estradiol-17β-hemisuksinat menggunakan isobutilkloroformat dan tributilamin sebagai katalis, dan penandaan histamin dengan 125I menggunakan metode kloramin-T. Tahap kedua adalah konjugasi histamin bertanda 125I dengan estradiol-17β-hemisuksinat yang sudah diaktivasi. Estradiol-17β-hemisuksinat bertanda 125I dilakukan ekstraksi menggunakan toluen dan fase organik dimurnikan dengan sistem KLT. Rendemen pemurnian yang diperoleh sebesar 79,8% untuk ekstraksi pelarut dan 84,4% untuk sistem KLT dengan kemurnian radiokimia 97,8%. Penentuan afinitas ikatan dilakukan dengan metode SPA menggunakan sel MCF7 yang mengekspresikan reseptor estrogen, dan diperoleh Kd sebesar 7,192 x 10-3 nM dan ikatan maksimum sebesar 336,1 nM. Afinitas ikatan estradiol-17β-hemisuksinat yang diperoleh tinggi, ditunjukkan dengan nilai Kd yang rendah.

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ABSTRACTResearch was carried out to get drugs that selective ligand and strongly bind estrogen receptors to determine the binding affinity to estradiol-17β-hemisuccinate. To improve the status of these compounds as a candidate for breast cancer active compound, selectivity of these compounds for estrogen receptor was studied using Scintillation Proximity Assay (SPA) method. Primary reagents required in the SPA method was radioligand and receptors, then performed with 125I labeling of estradiol-17β-hemisuccinate as a radioligand.

Radioligand binding studies were performed on MCF7 cell for estrogen receptor. The labeling process was performed by indirect method via two-stage reaction. First activation of estradiol-17β-hemisuccinate using isobutylchloroformate and tributylamine as a catalist, and labeling of histamine was carried out by 125I using Chloramin-T method. The second stage was conjugation of activated estradiol-17β-hemisuccinate with 125I-histamine. The estradiol-17β-hemisuccinate labeled with 125I was extracted using toluene and organic phase was purified by TLC system. The obtained purification yield for the extraction solvent was 79.8% and for the TLC system was 84,4% with a radiochemical purity was 97.8%. Determination of binding affinity by the SPA method using MCF7 cell lines which express estrogen receptors, were Kd of 7.192 x 10-3 nM and maximum binding of 336.1 nM. Having obtained binding affinity of estradiol-17β-hemisuccinate was obtained high, indicated by a low Kd values."