• 제목/요약/키워드: dehydrogenase(3{\alpha}-HSD)$

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Progesterone의 이화(異化)효소, 20α-hydroxysteroid dehydrogenase의 활성 및 활용에 관한 연구 1. 20α-hydroxysteroid dehydrogenase의 활성 및 혈청 progesterone 농도의 변화 (Activity and application of 20α-hydroxysteroid dehydrogenase in rat 1. Changes in activities of 20α-hydroxysteroid dehydrogenase and serum progesterone concentration)

  • 강정부;곽수동
    • 대한수의학회지
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    • 제34권4호
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    • pp.867-872
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    • 1994
  • Progesterone catabolizing enzyme, the enzyme $20{\alpha}$-hydroxysteroid dehydrgenase($20{\alpha}$-HSD) is pivotal in the regulation of ovarian function in rodents, which catabolizes progesterone into biologically inactive $20{\alpha}$-hydroxypregn-4-en-3-one($20{\alpha}$-OHP). In this study was carried out the influence of $20{\alpha}$-HSD activity of ovarian function, we investigated changes in ovarian cytosol $20{\alpha}$-HSD activity and serume progesterone concentration during the estrous cycles and pregnancy in rat. During the estrous cycles, the $20{\alpha}$-HSD activities were highest on the progestrous, but serum progesterone concentration was lowest on this phase. During the pregnancy, the $20{\alpha}$-HSD activities were relatively higher early pregnancy(day-1-3 gestation) and late pregnancy(day 21 to parturition), serum progesterone concentration was maintained significantly high to day 19 of gestation. The $20{\alpha}$-HSD activities were lower during the middle pregnancy. From these results, ovarian $20{\alpha}$-HSD activities may possibly act as physiologically very important in the control and maintenance of estrous cycles in rat.

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계혈등(Mucuna birdwoodiana)의 $3{\alpha}-Hydroxysteroid\;dehydrogenase$억제 성분 (Inhibitory Activities of Three Compounds from Mucuna birdwoodiana on $3{\alpha}-Hydroxysteroid\;dehydrogenase$)

  • 권용수;이진훈;김창민
    • 생약학회지
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    • 제30권2호
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    • pp.216-221
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    • 1999
  • The NAD(P)-linked $3{\alpha}-Hydroxysteroid$ $dehydrogenase(3{\alpha}-HSD)$ of rat liver cytosol is powerfully inhibited by the non-steroidal anti-inflammatory drugs in rank-order of their therapeutic potency, and this observation has now been developed into a rapid screen for predicting the potency of products that show anti-inflammatory effect. Five-plants were screened by using this method. Among them, BuOH-fraction of Mucuna birdwoodiana showed strong inhibitory effect on $3{\alpha}-HSD$, and three isoflavone compounds were isolated. Inhibitory activates of isolated compounds were compared.

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한방청열제의 $3{\alpha}-Hydroxysteroid$ dehydrogenase에 대한 억제효과 (Inhibitory Activities of Chinese Herbs that Clear Heat on $3{\alpha}-Hydroxysteroid$ dehydrogenase)

  • 안중수;최승연;권용수;김창민
    • 생약학회지
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    • 제29권1호
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    • pp.8-12
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    • 1998
  • $3{\alpha}-Hydroxysteroid$ dehydrogenase $(3{\alpha}-HSD)$ is one of the main enzymes involved in the metabolism of the active androgen, dihydrotestosterone. The NAD(P)-linked $3{\alpha}-HSD$ of rat liver cytosol is powerfully inhibited by the non-steroidal anti-inflammatory drugs in rank-order of their therapeutic potency. This observation has now been developed into a rapid screen for predicting the potency of products that show anti-inflammatory effect. 52-Chinese Herbs that clear heat were screened by using this method.

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Changes in Ovarian and Placental 20α-hydroxysteroid Dehydrogenase Activity during the Pregnancy in the Rat

  • Seong, H.H.;Min, K.S.;Kang, M.H.;Yoon, J.T.;Jin, H.J.;Chung, H.J.;Chang, W.K.;Yun, S.G.;Shiota, Kunio
    • Asian-Australasian Journal of Animal Sciences
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    • 제16권3호
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    • pp.342-347
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    • 2003
  • The enzyme $20{\alpha}$-hydroxysteroid dehydrogenase ($20{\alpha}$-HSD) catabolizes progesterone to $20{\alpha}$-dihydroprogesterone ($20{\alpha}$-OHP), and is appeared in rat corpora luteal and placenta. A polled samples of 10-15 placental and ovarian tissues collected from each individual rat were subjected to measurement of $20{\alpha}$-HSD activity. A $20{\alpha}$-HSD activity in the cytosol fraction was based on the generation of NADPH. In this study, it is designed to study cytosolic $20{\alpha}$-HSD activity in rat ovarian and placenta during pregnancy, and its relationship to embryonic mortality. It was found that from days 5 to 18 of pregnancy the $20{\alpha}$-HSD activities steady by decreased but at parturition time rapidly increased in ovary. On the other hand, placental cytosolic $20{\alpha}$-HSD activities were high detected from days 8 to 10 of pregnancy, not detectable from days 11 to 20 of pregnancy, but again very high at the time of parturition. Analysis of DEAE column chromatography revealed that two different types of $20{\alpha}$-HSD (HSD-1 and HSD-2) were found with similar activity in the placental cytosol on day 10 of pregnancy. The number of fetuses on day 10 of pregnancy was 15.4 and decreased significantly to 12.9 on day 12. The results suggested that expression of $20{\alpha}$-HSD in the placental tissues seems to be related the number of fetal survived in the specific time (days 11 and 12) which spontaneous fetal loss occurs.

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
    • 대한의생명과학회지
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    • 제19권2호
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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.

권삼의 소염활성성분(I) (Anti-inflammatory Constituents of Polygonum bistorta)

  • 안중수;권용수;김창민
    • 생약학회지
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    • 제30권3호
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    • pp.345-349
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    • 1999
  • Five compounds were isolated from the BuOH fraction of Polygonum bistorta (Polygonaceae). On the basis of spectral data, these compounds were established as caffeic acid, quercimeritrin, avicularin, gallic acid and protocatechuic acid. The inhibitory activies on $3{\alpha}-hydroxysteroid$ dehydrogenase $(3\;{\alpha}-HSD)$ of isolated compounds were compared. $IC_{50}$ value of isolated compounds were $133.57\;{\mu}g/ml\;(caffeic\;acid)$, $89.1\;{\mu}g/ml\;(quercimeritrin)$, $189.85\;{\mu}g/ml\;(avicularin)$, $140.69\;{\mu}g/ml\;(gallic\;acid)$ and $165.27\;{\mu}g/ml\;(protocatechuic\;acid)$ respectively. Although all compounds showed lower inhibition activities than BuOH fraction $(IC_{50}<50\;{\mu}g/ml)$ of Polygonum bistorta, it showed higher inhibition activities than aspirin $(IC_{50}\;246.81\;{\mu}g/ml)$.

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무지개송어 (Oncorhynchus mykiss)의 난소내 협막층(theca layers)에서의 Pregnenolone 대사: cyanoketone과 trilostane의 저해 효과 (Pregnenolone Metabolism in the Ovarian Thecal Layers of the Rainbow Trout, Oncorhynchus mykiss: in vitro Inhibitory Effects of Cyanoketone and Trilostane)

  • BAEK Hea-Ja;FOSTIER Alex
    • 한국수산과학회지
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    • 제28권4호
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    • pp.469-474
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    • 1995
  • [ $3\beta-$ ]히드록시-$\Delta^5$-스테로이드 탈수소효소 ($3\betaβ-HSD,$ $3\beta-hydroxy-\Delta^5-steroid\;dehydrogenase$ $\Delta^5$-스테로이드$\rightarrow\Delta^4$-스테로이드로의 대사경로에 관여하는 효소)에 대하여 특이적 저해제인 cyanoketone과 trilostane의 저해 효과가 $^3H-pregnenolone$ 전구체를 이용하여 무지개송어 난소에서 분리한 여포층, 협막층(theca layers)을 대상으로 비교 관찰되었다. Pregnenolone으로부터 $17\alpha-hydroxyprogesterone$으로의 대사과정에서 주요 효소인 $(3\beta-HSD$ 활성은cyanoketone $10^{-6}$$10^{-5}\;M$, 그리고 trilostane $10^{-5}$$10^{-4}\;M$의 농도에서 억제되었으며, trilostane이 cyanoketone보다 더 효과적인 억제반응을 보이는 것으로 나타났다. Pregnenolone으로부터 $\Delta^4$-스테로이드 대사물 축적에 대한 trilostane의 저해작용은 사용한 농도 즉, $10^{-8}, 10^{-7}, 10^{-6}$ 그리고 $10^{-5}\;M$에 비례하여 나타났으나 완전한 저해효과는 보이지 않았다.

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황체기능의 내분비 제어 (The Endocrine Control of Corpus Luteum Function)

  • 성환후
    • 한국가축번식학회지
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    • 제19권4호
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    • pp.307-322
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    • 1996
  • The corpus luteum (CL) is formed by the action of a surge of luteinizing hormone (LH) on the pre-ovulatory follicle. Luteal cells derived from granulosa and theca interna cells continue to secrete progesterone for about two weeks. LH in domestic animals is essential for the normal secretion of progesterone at all stages of the luteal phase. For this process in the rodents, 20$\alpha$-hydroxysteroid dehydrogenase (20$\alpha$-HSD) is indispensable. 20$\alpha$-HSD is an enzyme to be a biologically inactive steroid. This enzyme plays a critical role in the regulation of the rat luteal function and reported to be present in steroid-producing tissues such as the testis and adrenal gland. We have purified 20$\alpha$-HSD and found two distinct 20$\alpha$-HSD molecules (HSD-1 and HSD-2). Their molecular weights are both estimated to be 33kd.The amino acid compositions of HSD-1 and HSD-2 are mostly similar, but there is a slight difference in the content of lysine. We demonstrated that 1) CL of previous generations contribute more to whole ovarian 20$\alpha$-HSD activity, 2) newly formed corpora lutea contain only 20$\alpha$-HSD-1 activity, and 3) old CL express activities of each HSD isozyme as shown in the luteal tissue of cycling rats on the day of diestrus where only degenerating old CL exist. The increase in 20$\alpha$-HSD activity identified seems to be related to the increase in the numbers of 20$\alpha$-HSD-positive cells. Interestingly, 20$\alpha$-HSD-1 activities were strongly found in the follicle fluids and theca interna cells by immunohistochemical study. Thus, the activity of 20$\alpha$-HSD may be related to a survival mechanism of those luteal cells and follicles remaining in the ovaries. Luteal cells arise from two sources. The small luteal cells are all of theca cell origin, while the large luteal cells are mainly of granulosa cell origin. CL of Korean Native Cattle, as those of other animal species, contains two morphologycally and functionally distinct luteal cell populations, such as small and large luteal cells as well as nonluteal cells. In all reproductive states except in the late luteal phase, the bovine CL also contained more small luteal cells than large luteal cells. Luteal tissue secretes a variety of growth factors (proteins) and the pattern of secretion changes during all stages of the luteal phase. These growth factors could be important in regulating the function of the bovine corpus luteum and may act in a potential endocrine autocrine and paracrine mechanisms. Therefore, further work has to be done to elucidate the role of growth factors in the ovary, especially in the corpus luterum. Interest should be focussed on interaction of these growth factors in the regulation of luteal cell and the localization of cytokine synthesis in differnet luteal cells.

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TM-3 cell에서 eritadenine 함유 신령버섯균사체 액체배양물의 testosterone 생성 촉진효과 (Enhancement of Testosterone in TM3 Leydig Cells by an Eritadenine-containing Agaricus blazei Mycelial Liquid Culture Extract)

  • 김영숙;정재은;정희정;문연규;김정옥;하영래
    • 생명과학회지
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    • 제28권6호
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    • pp.648-655
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    • 2018
  • 신령버섯 액체배양추출물(Agaricus blazei mycelial liquid culture extract: ABMLCE)과 eritadenine (EA)의 mouse 정소 Leydig TM3 세포에서 testosterone (TS) 생성에 관한 연구를 정상 조건과 산화스트레스 조건에서 수행하였다. 정상 조건에서는 TM3 세포를 DMEM 배지에 배양하면서 EA (0~100 ppm)와 EA (0~50 ppm) + ABMLCE (10 ppm)를 24 hr처리하였다. 산화스트레스 조건에서는 TM3 세포를 $H_2O_2$ ($50{\mu}M$)를 4 hr 처리하고 정상 조건과 동일하게 처리하였다. DMEM 배양물에 함유된 TS 함량, HSD3B2 효소 활성, $5{\alpha}-R2$ 효소 활성과 NO 함량을 assay kit를 사용하여 측정하였다. EA는 정상 조건이나 산화스트레스 조건에서 TS 함량을 유의성 있게 증가시켰고, ABMLCE와 ABMLCE + EA도 TS의 함량을 증가시켰다. TS 전구체 생성에 관여하는 HSD3B2 효소 활성은 두 조건에서 모두 EA, ABMLCE, ABMLCE + EA에 의해서 증가되었다. 또한 TS를 DTH로 전환시켜 TS함량을 감소시키는 역할을 하는 $5{\alpha}-R2$ 효소활성은 정상 조건 및 산화스트레스 조건에서 ABMLCE에 의해서만 감소되었다. Free radical로 작용하는 NO의 함량은 두 조건 모두 EA, ABMLCE, ABMLCE + EA에 의해 감소되었다. 이 결과는 EA, ABMLCE, ABMLCE + EA 처리가 TM3 세포의 HSD3B2 효소 활성을 증가시키고, NO 생성을 억제하여 TS 함량을 증가시켰음을 의미하며 EA + ABMLCE 혼합물이 남성 성기능개선 물질로 사용될 수 있음을 의미한다.