• Title/Summary/Keyword: Methyl testosterone

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Microbial $9{\alpha}$-Hydroxylase:Epoxidation of 9(11)-dehydro-$17{\alpha}$-methyl-testosterone

  • Kang, Hee-Kyoung;Lee, Sang-Sup
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.525-528
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    • 1997
  • Steroid $9{\alpha}$.-hydroxylase is a key enzyme system in steroid nucleus degradation in company with ${\Delta}$-dehydrogenase. To examine $9{\alpha}$-hydroxylase activity during microbial transformation of steroids, 9(11)-dehydro-$17{\alpha}$-methyl-testosterone was adopted as a stable substrate for preventing the rupture of steroid nucleus. Using Nocardia restrictus ATCC 14887 capable of introducing a $9{\alpha}$-hydroxyl group into steroids, $9{\alpha}$,$11{\alpha}$-oxido-$17{\beta}$-hydroxy-$17{\alpha}$-methyl-4-androstene-3-one and $9{\alpha}$-hydroxyl group into steroids,$9{\alpha}$,$11{\alpha}$-oxido-$17{\beta}$-hydroxy-$17{\alpha}$-methyl-1,4-androstadiene-3- one were obtained. These microbiologically transformed products could be used as reference compounds in the enzyme assay.

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Effects of Testosterone, 17β-estradiol, and Progesterone on the Differentiation of Bovine Intramuscular Adipocytes

  • Oh, Young Sook;Cho, Sang Bum;Baek, Kyung Hoon;Choi, Chang Bon
    • Asian-Australasian Journal of Animal Sciences
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    • v.18 no.11
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    • pp.1589-1593
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    • 2005
  • The aim of this study was to investigate the effects of testosterone, 17$\beta$-estradiol, and progesterone on the differentiation of bovine intramuscular adipocytes (BIA). Stromal-vascular (SV) cells were obtained from M. longissimus dorsi of 20 months old Korean (Hanwoo) steers, and were cultured in DMEM containing 5% FBS. The proliferated BIA were induced to differentiate with 0.25 $\mu$M dexamethasone, 0.5 mM 1-methyl-3-isobutyl-xanthine and 10 $\mu$g/ml insulin. During differentiation, the cells were treated with testosterone, 17$\beta$-estradiol, and progesterone at concentrations of $10^{-10}$, $10^{-9}$, and $10^{-8}$ M, respectively, for 12 days. Regardless of its concentration, testosterone remarkably reduced lipid droplets in the cytosol of BIA. On the other hand, 17$\beta$-estradiol and progesterone increased the accumulation of lipid droplets in BIA. Testosterone significantly (p<0.05) decreased GPDH activities with a dose-dependent pattern. 17$\beta$-Estradiol treatment onto BIA during differentiation, however, increased GPDH activity showing the highest activity (11.3 nmol/mg protein/min) at $10^{-10}$ M. Treatment of BIA with progesterone also increased (p<0.05) GPDH activity with the highest activity (13.8 nmol/mg protein/min) at $10^{-9}$ M. In conclusion, the results in the current study suggest that testosterone inhibits differentiation of BIA by suppressing GPDH activity while 17$\beta$-estradiol and progesterone have adverse effects.

Immersion in sea cucumber's steroid extract to increase male production of juvenile freshwater crayfish

  • Gregorius Nugroho Susanto;Endang Linirin Widiastuti;Tri Rustanti;Sutopo Hadi
    • Fisheries and Aquatic Sciences
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    • v.26 no.1
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    • pp.48-57
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    • 2023
  • One of the ways to increase the production for aquaculture is through the cultivation of monosexuals by ensuring genital reversal from which energy for reproduction is diverted towards growth. Masculinization has been identified as one of the most prominent techniques, where sex development was directed from female to male. This approach only altered the phenotype and not the genotype. The red claw crayfish (Cherax quadricarinatus) was a relatively new commercial commodity, and the males were known to grow faster than females. Hence, it was proposed to use monocultures comprising an all-male population to increase yield using steroid hormone, synthetic 17α-methyltestosterone. However, this technique generated residues that detrimentally affect human health, the environment, and cultivated organisms. Therefore, finding new safe natural steroid sources was essential, and one of which is exploring of natural hormones extracted from the viscera of sea cucumbers (Holothuria scabra Jaeger). This study focused on the determination of male formation and testosterone levels among juvenile crayfish, after immersing in sea cucumber steroid extract (SCSE). A completely random design with factorial was used with two variables, encompassing the varied doses (0, 2, 4 mg/L, 2 mg/L 17α-methyl testosterone as control group) and immersion times of 18 and 30 h. The result showed the dose-dependent ability of SCSE increase the male genital formation and promote the testosterone level of juvenile crayfish. In addition, the testosterone was influenced by dose and immersion duration time, with the highest level of testosterone observed in treatments of 4 mg/L SCSE with 30 h immersion was 0.248 ng/mL, while the male percentage was 77%. In conclusion, the combination of dose and immersion time significantly affected growth and testosterone levels.

Effects of Ojawhan on the ethanol-induced erectile dysfunction in rats (오자환(五子丸)이 Ethanol로 발기부전을 유도한 흰쥐의 성기능 개선에 미치는 영향)

  • An, Tae-Geon;Jeong, Ji-Cheon
    • The Journal of Internal Korean Medicine
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    • v.26 no.3
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    • pp.605-614
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    • 2005
  • Objectives : Ojawhan was formulated to contain various natural products known to cure erectile dysfunction. This study was aimed to investigate the effects of Ojawhan on the nitric oxide synthase(NOS) activity, nitrite level, antioxidation and erectile responses in rat's corpus cavernosum penis. Methods : Ojawhan was washed, dried in the shade and crushed. The crushed Ojawhan ,was extracted 3 times, each time with 3 volumes of methyl alcohol at $60^{\circ}C$ for 24 h. The extract was filtered and evaporated under a reduced pressure using a rotary evaporator to yield 62g. Ojawhan extract oral-administered 100 mg per 1 kg of body weight for 30 days. First, samples were treated with Ojawhan, then ethanol-treated rats and L-N-Nitroarginine methyl ester(L-NAME) treated rats were put with the samples. Result : The level of urethral lipid peroxide in the ethanol-Ojawhan double administered rats was decreased as low as in the normal group, while the one in the ethanol-treated group was increased. The urethral NOS activity, the level of urethral nitrite, the level of testosterone and the erectile response to cavernous nerve stimulation in the ethanol-Ojawhan double administered rats were increased as high as in the normal group while the one in the ethanol-treated group was decreased. The electile response to cavernous nerve stimulation and the level of nitrite in L-NAME ($10^{-4}$)-treated rats was restored by the administration of Ojawhan as high as in the normal group. Conclusions : Ojawhan was effective in restoring the ethanol-induced or L-NAME-induced erectile dysfunction in rats.

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Effects of Mantidis Vagina Ovorum on the Cimetidine-Induced Erectile Dysfunction in Rats (상표소(桑螵蛸)가 Cimetidine으로 발기부전을 유도한 흰쥐의 성기능 개선에 미치는 영향)

  • Kim, Min-Su;Jeong, Ji-Cheon;Shin, Hyeon-Cheol
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.25 no.2
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    • pp.234-241
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    • 2011
  • Mantidis Vagina Ovorum was formulated to contain various natural products known to cure erectile dysfunction. This study was aimed to investigate the effects of Mantidis Vagina Ovorum on the nitric oxide synthase (NOS) activity, nitrite level, antioxidation and erectile responses in rat's corpus cavernosum penis. The crushed Mantidis Vagina Ovorum was extracted 3 times, each time with 3 volumes of methyl alcohol at $60^{\circ}C$ for 24 h. The extract was filtered and evaporated under a reduced pressure using a rotary evaporator to yield 16.6 g. Mantidis Vagina Ovorum extract oral-administered 75 mg per 1 kg of body weight for 30 days. First, samples were treated with Mantidis Vagina Ovorum, and then cimetidine-treated rats and L-N-Nitroarginine methyl ester (L-NAME) treated rats were put with the samples. The level of urethral lipid peroxide in the cimetidine-Mantidis Vagina Ovorum double administered rats was decreased as low as in the normal group, while the one in the cimetidine-treated group was increased. The urethral NOS activity, the level of urethral nitrite, the level of testosterone and the electile response to cavernous nerve stimulation in the cimetidine-Mantidis Vagina Ovorum double administered rats were increased as high as in the normal group while the one in the cimetidine-treated group was decreased. The electile response to cavernous nerve stimulation and the level of nitrite in L-NAME ($10^{-4}$)-treated rats was restored by the administration of Mantidis Vagina Ovorum as high as in the normal group. Mantidis Vagina Ovorum was effective in restoring the cimetidine-induced or L-NAME-induced erectile dysfunction in rats.

Isotope-Dilution Mass Spectrometry for Quantification of Urinary Active Androgens Separated by Gas Chromatography

  • Lee, Su-Hyeon;Choi, Man-Ho;Lee, Won-Yong;Chung, Bong-Chul
    • Mass Spectrometry Letters
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    • v.1 no.1
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    • pp.29-32
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    • 2010
  • Cross reacting antibodies can cause an overestimation of the results of immunoassays. Therefore, alternative methods are needed for the accurate quantification of steroids. Gas chromatography combined with isotope-dilution mass spectrometry (GC-IDMS) is developed to quantify urinary active androgens, testosterone, epitestosterone and dihydrotestosterone, which are clinically relevant androgens to both hair-loss and prostate diseases. The method devised involves enzymatic hydrolysis with $\beta$-glucuronidase, solid-phase extraction, liquid-liquid extraction using methyl tert-butyl ether and subsequent conversion to pentafluorophenyldimethylsilyl-trimethylsilyl (flophemesyl-TMS) derivatives for sensitive and selective analysis in selected-ion monitoring mode. Flophemesyl-TMS derivatization not only eliminates matrix interference but also has a good peak resolution within a 6 min-run. A selective and sensitive GC technique with flophemesyl-TMS derivatives also allows accurate quantitative analysis of three active androgens when combined with IDMS. The limit of quantification of the three analytes was <50 pg/mL, and extraction recoveries ranged from 91.9 to 102.1%. The precision and accuracy were 1.2~6.5% and 89.0~106.7%, respectively. This GC-IDMS method can be useful for evaluating the drug efficacy and monitoring the biological processes responsible for male-pattern baldness and prostate diseases.

In Vitro Metabolism of a New Neuroprotective Agent, KR-31543 in the Human Liver Microsomes : Identification of Human Cytochrome P450

  • Ji, Hye-Young;Lee, Seung-Seok;Yoo, Sung-Eun;Kim, Hosoon;Lee, Dong-Ha;Lim, Hong;Lee, Hye-Suk
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.239-245
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    • 2004
  • KR-31543, (2S,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(2 -methyl-2H-tetrazol-5-ylmethyl) amino]-3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-1-benzopyran, is a new neuroprotective agent for preventing ischemia-reperfusion damage. This study was performed to identify the metabolic pathway of KR-31543 in human liver microsomes and to characterize cytochrome P450 (CYP) enzymes that are involved in the metabolism of KR-31543. Human liver microsomal incubation of KR-31543 in the presence of NADPH resulted in the formation of two metabolites, M1 and M2. M1 was identified as N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine on the basis of LC/MS/MS analysis with a synthesized authentic standard, and M2 was suggested to be hydroxy-KR-31543. Correlation analysis between the known CYP enzyme activities and the rates of the formation of M 1 and M2 in the 12 human liver microsomes have showed significant correlations with testosterone 6$\beta$-hydroxylase activity (a marker of CYP3A4). Ketoconazole, a selective inhibitor of CYP3A4, and anti-CYP3A4 monoclonal antibodies potently inhibited both N-hydrolysis and hydroxylation of KR-31543 in human liver microsomes. These results provide evidence that CYP3A4 is the major isozyme responsible for the metabolism of KR-31543 to M1 and M2.

Effects of Albizzia Julibrissin on Chronic Ethanol-treated Erectile Dysfunction in Rats (Ethanol 에 의해 발기부전을 유도한 흰쥐의 성기능 개선에 미치는 합환피(合歡皮)의 영향)

  • Lee Min-Dong;Jeong Ji-Cheon
    • The Journal of Korean Medicine
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    • v.27 no.2 s.66
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    • pp.232-243
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    • 2006
  • Objectives : Albizzia Julibrissin was formulated to contain various natural products known to cure erectile dysfunction. This study was aimed to investigate the effects of Albizzia Julibrissin on the nitric oxide synthase (NOS) activity, nitrite level, antioxidation and erectile responses induced by ethanol in corpus cavernosum penis of rats. Methods : The crushed Albizzia Julibrissin was extracted 3 times, each time with 3 volumes of methyl alcohol at $60^{\circ}C$ for 24 h. The extract was filtered and evaporated under a reduced pressure using a rotary evaporator to yield 45.3 g. Albizzia Julibrissin extract was oral-administered 100 mg per 1 kg of body weight for 20 days, while the normal group was administered only with a saline. The efficacy of Albizzia Julibrissin against erectile function was examined as described in the text. Results : The level of urethral NOS activity and nitrite were increased by Albizzia Julibrissin. The level of lipid peroxide was decreased by Albizzia Julibrissin. The level of urethral lipid peroxide in the ethanol-Albizzia Julibrissin double administered rats was decreased as low as in the norma! group, while the one in the ethanol-treated group was increased. The level of urethral nitrite, NOS activity, glutathione and serum testosterone in the ethanol-Albizzia Julibrissin double administered rats were as high as in the normal group, while the one in the ethanol-treated group was decreased. The erectile response to cavernous nerve stimulation in the ethanol-Albizzia Julibrissin double administered rats increased as high as in the normal group while the one in the ethanol-treated group decreased. Conclusions : Albizzia Julibrissin was shown to be effective for the treatment of erectile dysfunction induced by ethanol in rats.

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