• Title/Summary/Keyword: estrone

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Microbial synthesis of sex hormones

  • Lee, Sang-Sup;Kang, Young-Ui;Kim, Young-Bae;Han, Jung-Rip
    • YAKHAK HOEJI
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    • v.16 no.3
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    • pp.137-147
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    • 1972
  • Estrone, which is obtainable from 19-hydroxycholesterol acetate through microbial oxidation, was chemically transformed to orally active estrogens, ethynylestradiol and methylestradiol. For progestin synthesis, $5{\alpha}$-bromo-619-oxidoisoandrosterone, was harvested from the culture broth(ATCC:19170), in which $5{\alpha}$-bromo-619-oxidocholestanol, acetate was added as a carbon source. Methylestrenolone, a potent orally active progestin, was synthesized from the harvested product via several reactions. Norethindrone, a popular progestin, was also prepared from 19-norandrostenedione. 19-Norandrostenedione is also available through microbial oxidation and chemical modification of $5{\alpha}$-chlor-619-oxidocholestanol, acetate.

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Estrogenic activity of Pomegranate extract in MCF7-ERE cells

  • Cho minjungo;An Jinyoung;Lansky Ephraim
    • Proceedings of the Korea Society of Environmental Toocicology Conference
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    • 2003.05a
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    • pp.192-192
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    • 2003
  • Pomegranate, a small tree originating in Orient, belongs to Punicaceae family. The seeds contain an oil of which about 80% is rare trans 18 carbon fatty acid (punicic acid), and have highest botanical concentration of a sex steroid, estrone. Pharmacological properties of pomegranate extract have been studied, with anti-microbial, anti-parasitic, ant-viral, and anti-cancer effects. We have examined the estrogenic activity of the pomegranate extracts using MCP-7-ERE cells. MCF-7-ERE cells, stably transfected with pERE-Luc were treated various amount of pomegranate extract and after overnight treatments, luciferase activity were measured. Estradiol(E2) dose dependently induced luciferase activity in this cell and maximal response is obtained at 100pM E2.

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돼지 Cytochrome P450 Aromatase의 새로운 기능

  • 최인호
    • Proceedings of the KSAR Conference
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    • 2003.06a
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    • pp.3-5
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    • 2003
  • 여성호르몬으로 잘 알려진 estrogen은 난소의 granulosa 세포와 정소의 Sertoli 세포에서 주로 생성되는 것으로 알려져 있으며 최근엔 사람의 지방, 근육, 뇌, 뼈세포 등에서의 합성 가능성과 각 조직에서 생성되는 estrogen 의 생리학적인 기능에 관해 많은 관심이 모여져 왔다. 다른 steroid처럼 지방친화적인 (lipophilic) estrogen은 세포막과 핵막을 쉽게 통과하여 목표세포 (target cell)의 핵에 존재하는 estrogen receptor (ER)에 결합하여 특정 유전자를 발현에 관여하는 것으로 알려져 있다. Cytochrome P450 Aromatase (간략히, aromatase)는 steroid hormone을 합성하는 마지막 단계에서 androgens을 estrogens으로 전환시키는데 관여하는 효소이다. Aromatase의 substrate (기질)로 사용되는 androgen에는 androstenedione과 testosterone 등이 있으며, 최종 산물로써 estrone(E1)이나 17$\beta$-estradiol(E2) 등의 estrogen이 생성된다. Aromatase는 steroidogenic tissues의 세포내 골지체에 존재하는 것으로 알려져 있으며, NADPH-cytochrome P450 reductase와 함께 복합체로써 존재한다. NADPH-cytochrome P450 reductase는 다른 steroid hormone에 관여하는 효소들과도 복합체를 형성하여 다른 steroid hormone을 합성할 수 있으므로, 어떤 조직에서 여성호르몬이 만들어질 수 있느냐 하는 것은 그 조직에서 aromatase 단백질이 만들어지느냐에 따라서 결정된다.

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Improved Calibration for the Analysis of Emerging Contaminants in Wastewater Using Ultra High Performance Liquid Chromatography and Time-of-Flight Mass Spectrometry

  • Pellinen, Jukka;Lepisto, Riikka-Juulia;Savolainen, Santeri
    • Mass Spectrometry Letters
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    • v.9 no.3
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    • pp.77-80
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    • 2018
  • The focus of this paper is to present techniques to overcome certain difficulties in quantitative analysis with a time-of-flight mass spectrometer (TOF-MS). The method is based on conventional solid-phase extraction, followed by reversed-phase ultra high performance liquid chromatography of the extract, and mass spectrometric analysis. The target compounds included atenolol, atrazine, caffeine, carbamazepine, diclofenac, estrone, ibuprofen, naproxen, simazine, sucralose, sulfamethoxazole, and triclosan. The matrix effects caused by high concentrations of organic compounds in wastewater are especially significant in electrospray ionization mass spectroscopy. Internal-standard calibration with isotopically labeled standards corrects the results for many matrix effects, but some peculiarities were observed. The problems encountered in quantitation of carbamazepine and triclosan, due to nonlinear calibration were solved by changing the internal standard and using a narrower mass window. With simazine, the use of a quadratic calibration curve was the best solution.

Ovarian response and surgical collection of embryos after induction of estrus in the bitch (발정유기견(發情誘起犬)의 난소반응(卵巢反應)과 수정란(受精卵)의 외과적(外科的) 회수(回收))

  • Kang, Byong-kyu;Choi, Han-sun;Na, Jin-su;Oh, Ki-seok;Son, Chang-ho;Lee, Cha-bum
    • Korean Journal of Veterinary Research
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    • v.29 no.3
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    • pp.373-381
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    • 1989
  • The aim of the present study was to test the efficiency of estrous induction in the premature, metestrous and anestrous bitches. The estrus was induced with prostaglandin $F_{2{\alpha}}$, estradiol-$17{\beta}$, pregnant mare serum gonadotropin (PMSG) and human chorionic gonadotropin(HCG) in the treatment A, and with PMSG and HCG in the treatment B. Day 0 was the first day of estrone injection in the treatment A and the day of PMSG injection in the treatment B. Twenty three of the twenty six bitches were laparotomized under general anesthesia between 11 and 18 days after onset of behavioral estrus, whereas three bitches were not laparotomized and remained until parturition. Ovarian responses were evaluated with the total number of corpora lutea or ovulation sites. The uterine horns were flushed with phosphate-buffered saline added heat treated canine serum(10%), the flushing media was collected into watch glass and the ova were examined under stereomicroscope. The results obtained were as follows: 1. Standing estrus was observed on the day $17.7{\pm}1.5$ after injection of estrone in the treament A, but ovarian responses were not detectable. 2. Standing estrus was observed on the day $12.2{\pm}0.2$ after injection of PMSG in the treament Band 14 of 17 bitches showed ovarian responses. Ova were recovered in 9 of the 14 bitches. 3. Ovarian responses were observed in one of the three premature bitches. two of the three metestrous bitches and all of the 11 anestrous bitches. The average number of the ova collected from 9 bitchs were $12.2{\pm}1.4$. 4. Three bitches in the treament B exhibited behavioural estrus and all of them were mated with fertile male dog, resulting the pregnancy in only one bitch. The pregnant bitch gave the birth of two pups.

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Removal of Organic Matter and Pharmaceuticals in Wastewater Effluent through Managed Aquifer Recharge (하수처리수를 이용한 대수층 함양관리 기술(Managed Aquifer Recharge)에서 유기물과 의약화합물 제거)

  • Im, Huncheol;Yeo, Inseol;Maeng, Sung-Kyu;Choi, Heechul
    • Journal of Korean Society of Environmental Engineers
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    • v.37 no.3
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    • pp.182-190
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    • 2015
  • This study was conducted to evaluate the removal efficiencies of organic matter and pharmaceuticals and to identify the removal mechanism of pharmaceuticals using sand obtained from Hwangryong River in Jangsung. Batch and column studies were used to simulate managed aquifer recharge (MAR) systems. All experiments were performed using field effluent containing pharmaceuticals from Damyang Wastewater Treatment Plant as an influent. Based on the removal results of organic matter and pharmaceuticals from the batch and column experiments, soil organic matter (SOM) and microbial activity were found to effectively remove target contaminants. The removal of organic matter was found to increase under biotic conditions. Neutral and cation pharmaceuticals (iopromide, estrone, and trimethoprim) exhibited removal efficiencies higher than 70% from natural sand and baked sand media in batch and column studies. Carbamazepine persisted in the sand batch and column studies. Anion pharmaceuticals (ketoprofen, ibuprofen, and diclofenac) can be removed under conditions featuring high SOM and adenosine triphosphate (ATP) concentrations in the sand surface. Based on the experimental Batch and column results, biodegradation and sorption were found to be important mechanisms for the removal of pharmaceuticals within the simulated MAR systems.

Studies on resveratrol and its metabolite in human urine by GC/MS (GC/MS를 이용한 요 중 resveratrol과 그 대사체에 관한 연구)

  • Jung, Hyun-Joo;Paeng, Ki-Jung;Kim, Yun-Je
    • Analytical Science and Technology
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    • v.24 no.2
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    • pp.142-149
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    • 2011
  • This study was conducted to define metabolite of the resveratrol by gas chromatography- time-offlight mass spectrometric detection. From these results, we suppose that the structure of metabolite is the result of reduction of double-bond attached by two-phenyl groups. Also, validity of method for determining metabolite of resveratrol and endogenous steroids was tested. The recoveries ranged from 96.47 to 114.74%, and intraand inter-day precision ranged 11.40 - 10.87% and 1.10 - 10.93%, accuracy ranged 80.03 - 119.92% and 80.02 - 119.56%, respectively. Resveratrol and endogenous steroids had correlation coefficients above or equal to 0.996. The method was successfully validated for the determination of resveratrol and endogenous steroids. Urinary samples from volunteers dosed resveratrol were analyzed to confirm a correlation resveratrol and its metabolite. From these results, the highest level of resveratrol and its metabolite was excreted in 10 - 15 hr more slowly than common drug, and conversion rate of metabolite was higher in woman than that in man. In addition, endogenous steroids were shown same the highest level of 10 - 15 hr. For estrone and estradiol, sensitivity was relatively higher in female than in man. And there were no significant changes of excretion patterns in the other endogenous steroids. Thus, we assumed that activation of resveratrol has impact on woman than man.

A Study on Relationship to Risk Factors according to Menopausal Status in Breast Cancer (유방암 환자에 있어서 폐경상태에 따른 위험인자의 상관성 연구)

  • Yoon, Han-Sik
    • Journal of radiological science and technology
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    • v.23 no.1
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    • pp.49-54
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    • 2000
  • It is important to identify modifiable risk factors for breast cancer, because the breast cancer is one of the major causs of mortality among women. Some reported that obesity is a risk factor for breast cancer, but the results are not constant. Many risk factors are related to the duration of estrogenic stimulation of the breast. In general, early menarche and late menopause are positive risk factors. Human breast cancer has different characteristics according to the status of menopause(premenopause and postmenopause). In premenopausal women, about 60% of circulating estrogen is from the ovaries in the form of estradiol, and the remaining 40% is estrogen formed primarily in the adipose(fat) tissue via aromatization of androstenedion from the adrenal glands. After menopause this adipose cell production of estrone is the main source of estrogens and the level of estrone is maintained approximately at premenopausal levels. This study was undertaken to determine the role of body size and body mass index by status of menopause in development of breast cancer using retrospective case/control study. From March 1991 to February 1997 at the Wonkwang University Hospital, the breast cancer cases(n=72) and controls(n=86) were selected. By statistical analysis method, regression analysis, paired T-test and multiple logistic regression were done to estimate the influenced factors same as height, weight, BMI, age at menarche and age at menopause. The following results were obtained : 1. In premenopausal women, age at menarche was showed comparatively high correlation coefficients and BMI was described prominently highly in postmenopause. 2. At the results of multiple regression analysis, age at monarch, BMI and weight were showed as significant variables. In this method, critical factor ($R^2$) was 0.054. 3. Paired samples T-test was undertaken to test mean difference between two groups of cases and controls. The result of test performance showed a significant difference. 4. In comparison with women whose weight less than 50 kg, the ORs for the upper 5th group was 1.82(95% confidence interval). The heaviest women had a higher risk(OR=1.14, 95% confidence interval $1.12{\sim}1.31$, p=0.005). Higher body mass index was significantly associated with increased risk of premenopausal breast cancer (OR=1.01, 95% confidence interval $1.08{\sim}l.18$, p=0.05).

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THE HORMONAL LEVELS OF THE SHORT LUTEAL PHASE IN KOREAN W0MEN (III);CHANGE OF STEROID GLUCURONIDES (황체기 단축현상을 가진 한국여성의 호르몬 양(Ⅲ);뇨내 Steroid Glucuronides의 변동)

  • Yoon, Yong-Dal
    • Clinical and Experimental Reproductive Medicine
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    • v.12 no.1
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    • pp.31-40
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    • 1985
  • 월경주기 중 황체기가 짧은 여성 즉 황체기 단축현상을 가진 한국여성(SLP) 의 특성을 조사하고 진단하는 방법을 개발하기 위하여 본 실험을 행하였다. 재료는 정상 월경주기를 가진 12명의 여성에서 26주기와 8명의 황체기 단축현상을 가진 여성에서 17주기를 선택하였다. 기상후 첫 오줌에서 steroid glucuronides의 농도를 측정하여 비교한 결과는 다음과 같았다. SLP 의 estrone -3 -glucuronide ($E_1G)의 농도는 초기 여포기와 황체기 동안 정상인에 비하여 현저히 낮았다. 또한 SLP 의 전 월경기 중 pregnanediol-$3{\alpha}$-glucuronide($P_2G$)의 농도 역시 유의성있게 낮았다. 그러나 $E_1G/P_2G$의 비율은 여포기가 황체기에 비하여 현저히 높았고, SLP 여성의 비율이 정상인 보다 각 월경주기 중 유의성있게 높았다. 위의 결과로 보아 $E_1G$, $P_2G$$E_1G/P_2G$의 농도차로 황체기 단축현상을 가진 여성을 진단 하고 또 치료시 난소의 기능조절에 이욜될 수 있을 것으로 사려된다.

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Inhibitory Effects of Curcuminoids on $17{\beta}$-hydroxysteroid Dehydrogenase Type 1 Activity in Animal Livers

  • Lee, Sung-Eun;Park, Byeoung-Soo;Kim, Hye Jin;Lee, Eun-Woo;Yum, Jong Hwa
    • Biomedical Science Letters
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    • v.19 no.2
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    • pp.147-152
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    • 2013
  • 17-${\beta}$-hydroxysteroid dehydrogenase type 1 ($17{\beta}$-HSD type 1) mediates the reaction of $17{\beta}$-estradiol (E2) production from estrone (E1). Inhibitory effects of curcuminoids on $17{\beta}$-HSD type 1 activity were investigated to find a lead compound for treating estrogen-dependent diseases including breast cancer. Among curcuminoids, demethoxycurcumin showed potent inhibitory effect ($IC_{50}=2.7{\mu}M$) on mouse $17{\beta}$-HSD type 1. Curcuminoids also displayed their inhibitory effects on the production of $17{\alpha}$-estradiol which is a carcinogenic metabolite produced by the enzyme. Bisdemethoxycurcumin ($IC_{50}=1.3{\mu}M$) showed potent inhibitory effect on the $17{\alpha}$-estradiol production by chicken $17{\beta}$-HSD type 1. Curcuminoids did not inhibit ERE transcriptional activity with and without E2. Taken together, curcuminoids can be used for treating and preventing E2-dependent diseases via inhibition on $17{\beta}$-HSD type 1 activity.