• YAKHAK HOEJI
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• v.51 no.6
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• pp.495-499
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• 2007

Seven epoxy- and hydroxyandrostane derivatives ($DH-1{\sim}DH-7$) and nine epoxy- and hydroxycholestane derivatives ($CH-1{\sim}CH-9$) with unsaturation in ring A and ring B were synthesized from DHEA and cholesterol, respectively. The antinociceptive effects of all synthesized compounds were measured by hot plate method. Most of androstane derivatives except $1{\alpha},2{\alpha}$-epoxy-4,6-androstadiene-3,17-dione (DH-3), and CH-6, CH-7 and CH-9 exhibited antinociceptive effect. 1,4-Androstadiene-$3{\beta},17{\beta}$-diol (DH-5, 100 mg/kg, $35.8{\pm}7.39$), $6{\alpha},7{\alpha}$-epoxy-1,4-androstadiene-3,17-dione (DH-4, 100 mg/kg, $32.6{\pm}5.50$) and $5{\alpha},6{\alpha}$-epoxy-17-oxo-androstan-$3{\beta}$-ol (DH-1, 100 mg/kg, $32.5{\pm}2.98$) were more effective than morphine (10 mg/kg, $30.6{\pm}0.5$). The analgesic effects of androstane derivatives on acetic acid writhing in mice were lower than aspirin. The androstane derivatives were less effective than ibuprofen at inhibiting effects on the carrageenin induced paw oedema. 4,6-Cholestadien-$3{\beta}$-ol (CH-5), $1{\alpha},2{\alpha}$-epoxy-4,6-cholestadien-$3{\beta}$-ol (CH-7) and $7{\alpha}$-hydroxy4-cholesten-3-one (CH-9) showed the decrease of serum triglyceride and total cholesterol levels in poloxamer P-407 injected rat.

• Bulletin of the Korean Chemical Society
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• v.35 no.11
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• pp.3224-3226
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• 2014

A new androstane derivative, $4{\beta}$-methyl-15-oxa-$14{\beta}$-androstane-7-ene-$4{\alpha}$-carboxylic acid (1) and a known one $4{\beta}$-methyl-15-oxa-$14{\beta}$-androstane-7-ene-$4{\alpha}$-hydroxyl (2) were isolated from the EtOAc extract of the cultures of the fungus Marasmiellus ramealis (Bull.) Singer. Their structures were elucidated on the basis of 1D and 2D NMR as well as MS spectroscopic data analysis. The inhibitory activity of two isolates against acetylcholinesterase (AChE) revealed that compound 1 exhibited definitely inhibitory activity.

• Journal of Life Science
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• v.21 no.4
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• pp.481-485
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• 2011

T0901317 is a potent synthetic ligand for liver X receptor (LXR, NR1H2/3), a member of the nuclear receptor superfamily that functions as a transcription factor. However, T0901317 has been also reported to modulate the activity at least four other nuclear receptors (NRs), acting as agonists for farnesoid X receptor (FXR, NR1H4) and pregnane X receptor (PXR, NR1I2) and as antagonists for androgen receptor (AR, NR3C4) and retinoid-related orphan receptor-${\alpha}$ (ROR-${\alpha}$, NR1F1). We report here that T0901317 can also function as an inhibitor for constitutive androstane receptor (CAR, NR1I3). Since CAR is a major player of xenobiotic and cholesterol metabolism in the liver, along with PXR, FXR and LXR, which are reported to be regulated by T0901317, this further complicates the interpretation of potential results with T0901317 in liver cells.

• Analytical Science and Technology
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• v.12 no.3
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• pp.190-195
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• 1999

The metabolism of testosterone ($17{\beta}$-hydroxy-androst-4-en-3-one) was confirmed in horse after a single intramuscular administration of testosterone cypionate (750 mg). Solvent extracts of urine obtained with enzymatic hydrolysis and methanolysis were analyzed by GC/MS after oxime t-butyldimethylsilyl (oxime-TBDMS) derivatization. The structures of four urinary metabolite after testosterone administration in horse were determined based on EI mass spectra and $5{\alpha}$-androstane-$3{\beta}$, $17{\alpha}$-diol and $5{\alpha}$-androstane-$3{\beta}$-ol-17-one as major was confirmed with authentic standard. Also the concentrations of $5{\alpha}$-androstane-$3{\beta}$, $17{\alpha}$-diol, $5{\alpha}$-androstane-$3{\beta}$, $17{\beta}$-diol, dehydroepiandrosterone (DHEA), $5{\alpha}$-androstane-$3{\beta}$-ol-17-one and testosterone were determined in the urine of normal subjects and the urine after administration. The recovery and detection limit in the most drugs were 86.3~94.7% and 1~3 ppb, respectively. Correlation coefficients for calibration were in the range of 0.984~0.999. Excretion profile of testosterone presents the rapid and large increasement up to maximum values at days 5 after administration and the slow regression. The relative ratios of testosterone, its metabolites over DHEA were determined for indication of testosterone administration in horse doping.

• Proceedings of the Korean Society of Life Science Conference
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• 2003.05a
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• pp.125-126
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• 2003

• Proceedings of the Korean Society of Developmental Biology Conference
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• 2005.10a
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• pp.133-133
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• 2005

• Proceedings of the Korean Society of Embryo Transfer Conference
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• 2005.10a
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• pp.133-133
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• 2005

• Journal of Life Science
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• v.13 no.3
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• pp.324-332
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• 2003

The objective of this study was to examine if transient transfection of CAR can transactivate CYP2B1 PBRU reporter gene in COS cells in which the endogenous CYP2B1 gene is not induced by PB. In non-transfeced cells of both Hep G2 and COS, the endogeneous expression of CAR was not detected by antibody against CAR. When cultured cells were transfected with CAR expression plasmid, mCAR1-GFP, both cell types expressed high levels of CAR protein and could allow to examine the effect of CAR in PBRU transactivation. Both cell types expressed endogenous RXR and transfection of RXR expression plasmid dramatically increased its protein expression. Whereas CAR transactivated PBRU2C1Luciferase about 12 fold as compared to 2C1Luciferase in Hep G2 cells, it did not stimulate the luciferase activity of the PBRU reporter gene in COS cells. These results indicate that Hep G2 cells can respond to CAR differently from COS cells, and suggest that factors other than CAR and RXR may be required in inducing PBRU activation and the expression of these factors may be different between liver and kidney.

• Proceedings of the Korean Society of Life Science Conference
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• 2006.09a
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• pp.71.1-71.1
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• 2006

• Proceedings of the Korean Society of Life Science Conference
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• 2007.10a
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• pp.80.2-80.2
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• 2007

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