• Bulletin of the Korean Chemical Society
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• 제35권5호
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• pp.1409-1412
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• 2014

Sex hormones are important metabolites in vertebrates' development and reproduction. For rapid screening sex hormones, matrix-assisted laser desorption/ionization (MALDI) mass spectrometry (MS) is one of the promising analytical platforms, but MALDI MS faces many challenges in detecting steroids such as low ionization efficiency and matrix background interference. One potential strategy to overcome matrix interference in the low m/z region is using a cyclodextrin (CD)-supported matrix for steroid analysis since CD-supported matrixes are known to effectively suppress matrix-related ion signals. In this study, we aimed to find the optimal CD-supported matrix for the analysis of the nonderivatized sex steroids. Our results showed that the ${\alpha}CD$-supported 2,5-dihydroxybenzoic acid (DHB) matrix efficiently ionized all three major classes of sex hormones, estrogens, androgens, and progestagens, with low or no matrix background and also with high sensitivity. In addition, the ${\alpha}CD$-supported DHB matrix mainly generated molecular ions or protonated ions of sex hormones, and this enabled us to obtain information-rich tandem mass spectra which potentially lead to unambiguous identification of steroid species from complex metabolite mixtures.

• Clinical and Experimental Reproductive Medicine
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• 제30권1호
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• pp.23-29
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• 2003

목 적: 본 연구의 목적은 내인성 성호르몬이 자궁근종의 성장에 미치는 영향을 알아보고자 연구를 시행하였다. 연구대상 및 방법: 폐경전 자궁근종 환자 27명과 같은 연령대의 정상여성 25명을 대상으로 하였다. 모든 대상군의 여성에서 24시간 소변을 모아서 소변내 estrogen, androgen의 대사체들을 GC-MS를 이용하여 측정하였으며 두 군에서의 차이를 비교분석 하였다. 결 과: 소변내 $17{\beta}$-estradiol, 5-androstene-$3{\beta}$, $16{\beta}$, $17{\beta}$-triol, 11-keto-ethiocholanolone, $11{\beta}$-hydroxy-androsterone, THS, THA, THE, a-cortolone, a-cortol 및 $\beta$-cortol가 환자군에서 의의있게 증가하였으며 $17{\beta}$estradiol/estrone 및 $11{\beta}$-hydroxy-ethiocholanolone/$11{\beta}$-hydroxy-androsterone도 환자군에서 의의있게 증가하였다. 결 론: 자궁근종의 성장은 요중 estrogen과 androgen의 농도와 밀접한 관련이 있으며 이는 환자의 스테로이드 호르몬 대사 감소에 기인한 것으로 사료된다.

• 한국물환경학회지
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• 제26권6호
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• pp.948-953
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• 2010

In this study, degradation of estrone (E1) and $17{\alpha}$-ethynylestradiol (EE2) by gamma-irradiation and subsequent reduction of estrogenic activity as a function of absorbed dose were conducted using the yeast two-hybrid assay. Relative potency of E1 and EE2 compared to estrogenic activity of $17{\beta}$-estradiol (E2) was found to be 0.0144 and 0.1605, respectively. More than 90% of E1 and EE2 (both $5.0{\times}10^{-6}M$) was removed at an absorbed dose of 5 kGy, but more than 40% of estrogenic activity still remained. The addition of $TiO_2$ catalyst appeared to improve the removal efficiency of E1 and decrease estrogenic activity while there was no significant effect for EE2. Additionally, the calculated estrogenic activity of E1 and EE2 based on a regression model was well correlated with the observed activity.

• 한국발생생물학회지:발생과생식
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• 제1권1호
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• pp.25-28
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• 1997

The present study was conducted to determine the effect of recombinant human follicle stimulating hormone (rhFSH) on the estrogen synthesis by human fetal ovarian tissues. Fetal ovaries were 18-19 weeks old (18 wks:n=1, 19 wks:n=2). One case of 19-week-old fetal ovaries were obtained from anencephalic fetus. Obtained ovarieswere cleaned and diced around $600\mu\textrm{m}$ pieces, and cultured in the sandwich agar bed system for 21-23 days. Estrone ($E_{1}$) and estradiol-17 $\beta$($E_{2}$) in the medium was measured by radioimmunoassay. Amount of $E_{2}$ synthesis was greater than $E_{1}$ in both normal cases. In contrast, fetal ovaries from anencephalic fetus did not produce neither $E_{1}$ nor $E_{2}$ in the presence or absence of rhFSH. Results suggest that the fetal ovaries have a capacity of estrogen production at 18-19 weeks of gestation Existence of FSH receptor is also supposed. Different results by anecephalic fetal ovaries suggest the difference in the development between normal and anencephalic fetal ovaries.

• Asian Pacific Journal of Cancer Prevention
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• 제16권6호
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• pp.2161-2166
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• 2015

Estrogen receptors (ERs) are steroid receptors located in the cytoplasm and on the nuclear membrane. The sequence similarities of human $ER{\alpha}$, mouse $ER{\alpha}$, rat $ER{\alpha}$, dog $ER{\alpha}$, and cat $ER{\alpha}$ are above 90%, but structures of $ER{\alpha}$ may different among species. Estrogen can be agonist and antagonist depending on its target organs. This hormone play roles in several diseases including breast cancer. There are variety of the relative binding affinity (RBA) of ER and estrogen species in comparison to $17{\beta}-estradiol$ (E2), which is a natural ligand of both $ER{\alpha}$ and $ER{\beta}$. The RBA of the estrogen species are as following: diethyl stilbestrol (DES) > hexestrol > dienestrol > $17{\beta}-estradiol$ (E2) > 17- estradiol > moxestrol > estriol (E3) >4-OH estradiol > estrone-3-sulfate. Estrogen mimetic drugs, selective estrogen receptor modulators (SERMs), have been used as hormonal therapy for ER positive breast cancer and postmenopausal osteoporosis. In the postgenomic era, in silico models have become effective tools for modern drug discovery. These provide three dimensional structures of many transmembrane receptors and enzymes, which are important targets of de novo drug development. The estimated inhibition constants (Ki) from computational model have been used as a screening procedure before in vitro and in vivo studies.

• Journal of Pharmaceutical Investigation
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• 제36권4호
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• pp.283-286
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• 2006

The present study aimed to investigate the interaction of nucleoside analogs with human organic anion transporter 1 and 3(hOAT1 and hOAT3) that play a primary role in the tubular uptake of endogenous and exogenous organic anions in the kidney. The interactions of ddC, ara-C, ara-A and ara-U with hOAT1 and hOAT3 were examined using MDCK cells stably overexpressing hOAT1 or hOAT3. Among the tested drugs, ddC showed the highest affinity to hOAT1 with $IC_{50}$ values of 5.2 mM, while ara-A, ara-C and ara-U weakly inhibited the cellular uptake of $[^3H]-PAH$ in MDCK-hOAT1 cells at 1 mM. In contrast, all the tested drugs did not have any inhibition effect on the cellular uptake of $[^3H]-estrone$ sulfate in MDCK-hOAT3 cells over the drug concentration of 0.01-2 mM, implying that they might not interact with hOAT3. Taken all together, the present study suggests that hOAT1 could weakly interact with nucleoside analogues such as ddC, ara-C, ara-A and ara-U but the interaction with hOAT3 during the urinary excretion of these nucleoside analogues may be negligible in the kidney.

• 한국수산과학회지
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• 제47권6호
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• pp.882-887
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• 2014

We studied oocyte steroidogenesis in blacktip grouper Epinephelus fasciatus ovarian follicles during vitellogenesis. Vitellogenic oocytes with average diameters of 0.45, 0.48 and 0.50 mm were incubated in vitro in the presence of $[^3H]17{\alpha}$-hydroxyprogesterone as a precursor. The steroid metabolites were analyzed using thin layer chromatography (TLC), high performance liquid chromatography (HPLC), and gas chromatography-mass spectrometry (GC/MS). The major metabolites in the vitellogenic oocytes were androstenedione ($A_4$), testosterone (T), estradiol-$17{\beta}$ ($E_2$), and estrone ($E_1$). The metabolites of androgen ($A_4$ and T) were higher in the 0.50-mm oocytes than in the 0.45- and 0.48-mm oocytes, while the estrogen metabolites (E2 and E1) were lower in the 0.50-mm oocytes. These results suggest that 0.50-mm oocytes are fully vitellogenic following initiation of the maturation process.

• 한국미생물·생명공학회지
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• 제35권2호
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• pp.81-97
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• 2007

Punica granatum, L. (Pomegranate) has 613 seeds which accidentally corresponds to the 613 commandments in the Bible. Accordingly, the fruit has been worshipped by the Jewish and other religious people from the ancient. Pomegranate's seed, peel and juice contain a variety of ethnomedical components so much as the sum of three kinds of other common fruits. The number of published papers related to the pomegranate in recent 7 years flourished 7 times more than before at the bases of Medline record. Since the containments of estrogen, as $17{\alpha}-estradiol,\;17{\beta}-estradiol$, estrone, and estradiol, etc., in pomegranate have been reported, public interests and commercial values of pomegranate arose considerably. The report was disproved later, however, merits of this fruit remained yet; clinical efficacy for preventing and remediating cancers including breast and prostate cancers by oral administration of the juice, seed oil, and peel extract is still believed to be true. In this review, target components of pomegranate such as antioxidants, anticancers, antiestrogens and ethnomedical components were analyzed and discussed along with examining its pharmaceutical efficacy and prescription to postmenopausal lesion, cardiosclerosis, cosmetic beautification, viral and allergic symptoms, and diabetes mellitus, etc.

• 생약학회지
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• 제24권4호
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• pp.282-288
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• 1993

Very little utilization of the fruits of Malus baccata(Rosaceae) has been employed for food and medicinal plants except for preparing fruit beverages. But, it was estimated as valuable to investigate the chemical components for the botanical resource of this plant. In this study, it was found that the fruits of this plant contained primary long chain alcohol, ${\beta}-sitosterol$, campesterol, ursolic acid and ${\beta}-_D-glucosides$ of ${\beta}-sitosterol$ and campesterol. However, phloretin(dihydrochalcone) and its 5-O-glucoside(phloridzin) known as plant growth regulators in many Rosaceae plants were not found in this plant material by co-TLC analysis with authentic specimens. Although plant sex hormone, estrone, was often contained in relates of M. baccata, e.g., Prunus spp., Crataegus spp. and Malus spp., this compound was not detected in this fruit by comparison with an authentic material. By RIC chromatography, it was suggested that the Soxhlet extraction by the solvent of ether was excellently useful to extract ursolic acid efficiently.

• 한국발생생물학회지:발생과생식
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• 제25권2호
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• pp.75-82
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• 2021

We studied steroid metabolites produced from red-spotted grouper ovarian follicles during maturation. Oocytes with 350-500 ㎛ diameter were in vitro incubated in the presence of [³H] 17α-hydroxyprogesterone as a precursor. Steroid metabolites were extracted from incubated media and oocytes. The extracts were separated and identified using thin layer chromatography, high performance liquid chromatography and gas chromatography-mass spectrometry. The identified metabolites were androstenedione (A₄), testosterone (T) and estrone (E₁). The metabolites of A₄ was dominant in all size of oocytes and it was the highest in 480 ㎛ diameter oocytes. The metabolites of two progestins, 17α,20β-dihydroxy-4-pregnen-3-one and 17α,20α-dihydroxy-4-pregnen-3-one were detected in the oocytes less than 480 ㎛ diameter although they were not identified definitely. In the oocytes of 480 ㎛ diameter, metabolite of progestin was the highest, and germinal vesicle (GV) was still in the middle of cytoplasm. In the oocytes of 500 ㎛ diameter, GV was began to migrate and the major metabolites were A₄ and E₁. The metabolite of E₁ was detected in all size of oocytes and it was higher than that of E₂. These results suggest that oocytes of 480 ㎛ diameter are the transitional stage involving steroidogenic shift to final oocyte maturation and potential function of E₁ during maturation process.