• 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.

• 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.

• 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.

• 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 $(IC_{50}\;246.81\;{\mu}g/ml)$.

• 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.

• 대한수의학회지
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• 제34권4호
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• pp.873-880
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• 1994

Progesterone catabolizing enzyme, the enzyme $20{\alpha}$-hydroxysteroid deltydrgenase($20{\alpha}$-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 to ovarian function and regulation such as ovulation, formation of corpus luteum, maintenance of estrous cycles and pregnancy, we investigated changes in activities of the splenic macrophages and ovarian histological findings in rat. During the estrous cycles, the ratious of phagocytotic macrophage in splenic adherent cells were highest on the proestrous, but they were lowest on metestrous. During the pregnancy, the ratious of phagocytotic macrophages in splenic adhrent cells were lowest by 1 day and then significantly increased toward the pregnancy, which were highest pregnancy on day 12. On histological findings in rat ovary, the mean number of growing, antral and mature follicles were 15.9(72.9%), 3.4(15.9%), and 2.4(11.2%), respectively. Growing follicles reached to lowest number at diestrus and mature follicle reached to lowest number at metestrus. The numbers of corpus luteums per tissue section of the ovary were 14.4 and the number of normal and atretic follicles were 11.0(76.4%) and 3.4(23.6%), respectively. The number of corpus luteum with vacolated cell were 1.7(11.8%). In this study suggests splenic macrophages are as a source of the substance which maintainer progesterone secretion from luteal cells, and are recognized pass the vessels and reside in the fresh corpora lutea soon after ovulation via inflammatory reactions, and these macrophages are felt to have a stimulatory effect on the formation of cropora lutea. In view of the results include previous report, ovarian $20{\alpha}$-hydroxysteroid dehydrogenase enzyme and splenic macrophages consider play central role in the control and maintenance of estrous cycles and pregnancy, and also applicable to both clinical and research in a wide variety such as control of reproductive system.

• 한국식물학회:학술대회논문집
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• 한국식물학회 2001년도 춘계학술발표대회:발표눈문요지록
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• pp.26-26
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• 2001

• 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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2007년도 Proceedings of The Convention
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• pp.57-64
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• 2007

Metabolic interactions of the three major cannabinoids, ${\Delta}^9$-tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol (CBN) with steroid hormones were investigated. These cannabioids concentration-dependently inhibited $3{\beta}$-hydroxysteroid dehydrogenase and $17{\alpha}$-hydroxylase in rat adrenal and testis microsomes. CBD and CBN were the most potent inhibitors of $3{\beta}$-phydroxysteroid dehydrogenase and progesterone $17{\alpha}$-hydroxylase, respectively, in rat testis microsomes. Three cannabinoids highly attenuated hCG-stimulated testosterone production in rat testicular interstitial cells. These cannabinoids also decreased in levels of mRNA and protein of StAR in the rat testis cells. These results indicate that the cannabinoids could interact with steroid hormones, and exert their modulatory effects on endocrine and testicular functions. Metabolic interaction of a THC metabolite, $7{\beta}$-hydroxy-${\Delta}^8$-THC with steroids is also investigated. Monkey liver microsomes catalyzed the stereoselective oxidation of $7{\beta}$-hydroxy-${\Delta}^8$-THC to 7-oxo-${\Delta}^8$-THC, so-called microsomal alcohol oxygenase (MALCO). The reaction is catalyzed by CYP3A8 in the monkey liver microsomes, and required NADH as well as NADPH as an efficient cofactor, and its activity is stimulated by some steroids such as testosterone and progesterone. Kinetic analyses revealed that MALCO-catalyze reaction showed positive cooperativity. In order to explain the metabolic interaction between the cannabinoid metabolite and testosterone, we propose a novel kinetic model involving at least three binding sites for mechanism of the metabolic interactions.

• Journal of Pharmaceutical Investigation
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• 제21권2호
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• pp.67-71
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• 1991

A simple and sensitive method was developed for the quantification of free and conjugated bile acids in bezoar without prior hydrolysis. $3{\alpha}-Hydroxy$ bile acids are first oxidized to 3-keto bile acids in the reaction catalyzed by $3{\alpha}-hydroxysteroid$ $dehydrogenase(3{\alpha}-HSD)$. During this oxidative reaction, an equimolar quantity of nicotinamide adenine dinucleotide(NAD) is reduced to NADH and subsequently oxidized to NAD with concomitant reduction of nitrotetrazolium blue(NTB) to diformazan by the catalytic action of diaphorase. The diformazan has an absorbance maximum at 540 nm. The intensity of the color produced is directly proportional to bile acids concentration in the bezoar extracts. The optimum conditions for the enzymatic reaction such as effects of reaction time, reaction temperature and pH, and stability were investigated. Calibration plots for the sodium chelate observed to be linear and intra-, inter-assay analytical recovery of bile acids averaged $97.65{\pm}3.4%(S.D.)$. Therefore, it is considered that the quality control of total bile acids from bezoar or bezoar-containing liquid preparation using this simple and sensitive assay system will be acceptable. Also current bezoars and bezoar-containing liauid preparations were examined their total bile acids from this method.