• Title/Summary/Keyword: ${\beta}_{3}$-AR

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The Inhibitory Effects of So-yangin Biman-bang on the Obese-Mice Induced by High-Fat Diet (소양인(少陽人) 비만방(肥滿方)이 생쥐의 비만 억제에 미치는 영향)

  • Park, In-Sun;Yoon, Il-Ji
    • Journal of Korean Medicine Rehabilitation
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    • v.20 no.2
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    • pp.35-50
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    • 2010
  • Objectives : In order to investigate the effects of So-yangin Biman-bang(here in after referred to BM) on the obese gene and obese inhibitory, C57BL/6 mice were distinctively induced by high fat diet. Methods : C57BL/6 mice were divided into four groups(normal, high fat diet with control, high fat diet with Reductil(here in after referred to RDT), high fat diet with BM extract) and have been fed for 8 weeks. Through observing the process, the weight change of the adipocytes in body and liver, total cholesterol, LDL-cholesterol, HDL-cholesterol, triglyceride, glucose, leptin change in the serum, the expression of ${\beta}3AR$ and leptin gene in 3T3-L1 cell and primary adipocyte cell. Results : The following results have been found in this study. 1. Losing weight have significantly been shown. 2. The weight change of the body adipocyte and liver have been decreased but no significance has been found. 3. With close observation on the change of blood, HDL-cholesterol has positively been increased in numbers but the level of glucose, LDL-cholesterol, triglyceride have distinctively been decreased. 4. The manifestation of ${\beta}3AR$ in 3T3-L1 cell and primary adipocyte cell have shown a definite increase in numbers but the manifestation of leptin has shown certain decrease in its amount. Conclusions : As results of this, So-yangin Biman-bang is thought to be effective in metabolic syndrom and lipid metabolism disorder that can possibly be occurred by obesity control and treatment. The clinical research will be needed in order to apply to So-yangin constitution in the future.

Optimization of the Channel of a Plate Heat Exchanger wits Ribs (리브가 있는 판형 열교환기 관내부 최적화)

  • 이관수;양동근
    • Korean Journal of Air-Conditioning and Refrigeration Engineering
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    • v.14 no.3
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    • pp.199-205
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    • 2002
  • In this paper, the optimum shape and arrangement of ribs in the channel of a plate heat exchanger are studied. The following dimensionless geometric parameters of ribs are selected as design variables: rib height ($H_R$), angle of attack ($\beta$), rib pitch ($P_R$), rib distance (L) and aspect ratio of rib (AR). The optimization is performed by minimizing the objective function consisting of the Nusselt number and the friction factor. The optimal values of design variables are as follows: $H_R$=0.263, $\beta$=0.290, $P_R$=3.142, L: 3.954, AR=0.342. The pressure drop and the heat transfer of the optimum model, compared to those of the reference model, are increased by 15.1% and 41.6%, respectively.

Recognition of Pharmacophore of ar-Turmerone for its Anticancer Activity

  • Baik, Kyong-Up;Jung, Sang-Hun;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.16 no.3
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    • pp.254-256
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    • 1993
  • For the evaluation of the role of .alpha., .betha.-unsaturated ketone portion of ar-tumerone for its activity, the structural variation of this structural unit was performed to omit its alkylating propery. Thus compounds 2, 3, and 4 were prepared and their cytotoxicities were determined against three different leukemiz cell lines (HL-60, K-562, and $L_{1210})$ in vitro. The biological inactivity against three different cell lines of these analogues implies that the $\alpha, \beta$-unsaturated ketone of ar-tumerone is the essential pharmacophore for its activity.

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Novel and Efficient Palladium Complexes with β-Ketoiminate Ligands for the Polymerization of Norbornene

  • Lee, Dong-Hwan;Hwang, Yoon-Joo;Yoon, Jin-San;Choi, Moon-Kun;Lee, Ik-Mo
    • Bulletin of the Korean Chemical Society
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    • v.30 no.3
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    • pp.636-646
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    • 2009
  • A series of the noble palladium complexes containing $\beta$-ketoiminate ligands with internal bases, [Pd(${\eta}^3$-allyl)($\beta$- ketoiminate)], [Pd(Me)($PPh_3$)($\beta$-ketoiminate)] and [Pd(Me)($\beta$-ketoiminate)], have been successfully prepared. Crystallographically determined structures showed that these complexes are distorted square planar and pendant bases of the $\beta$-ketoiminate ligands fail to coordinate to the metal in the first two classes of complexes while bases do coordinate in the 3rd class complexes. These complexes are active towards norbornene polymerization on activation with $H(OEt_2)_2BAr^'_4$ (Ar' = 3,5-bistrifluoromethylphenyl) and modified methylalumioxane (MMAO). MMAO is more efficient for the activation for polymerization. Generally, the polymerization activity increases with the following order; [Pd(allyl)($\beta$-ketoiminate)] < [Pd(Me)($PPh_3$)($\beta$-ketoiminate)] < [Pd(Me)($\beta$-ketoiminate)].

Disturbance in Testosterone Production in Leydig Cells by Polycyclic Aromatic Hydrocarbons

  • Oh, Seunghoon
    • Development and Reproduction
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    • v.18 no.4
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    • pp.187-195
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    • 2014
  • Polycyclic aromatic hydrocarbons (PAHs), which are ubiquitous in the air, are present as volatile and particulate pollutants that result from incomplete combustion. Most PAHs have toxic, mutagenic, and/or carcinogenic properties. Among PAHs, benzo[a]pyrene (B[a]P) and dimethylbenz[a]anthracene (DMBA) are suspected endocrine disruptors. The testis is an important target for PAHs, yet effects on steroidogenesis in Leydig cells are yet to be ascertained. Particularly, disruption of testosterone production by these chemicals can result in serious defects in male reproduction. Exposure to B[a]P reduced serum and intratesticular fluid testosterone levels in rats. Of note, the testosterone level reductions were accompanied by decreased steroidogenic acute regulatory protein (StAR) and $3{\beta}$-hydroxysteroid dehydrogenase isomerase ($3{\beta}$-HSD) expression in Leydig cells. B[a]P exposure can decrease epididymal sperm quality, possibly by disturbing the testosterone level. StAR may be a key steroidogenic protein that is targeted by B[a]P or other PAHs.

Metabolic Interactions of Cannabinoids with Steroid Hormones

  • Watanabe, Kazuhito
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2007.11a
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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.

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Effects of Panax ginseng, zearalenol, and estradiol on sperm function

  • Gray, Sandra L.;Lackey, Brett R.;Boone, William R.
    • Journal of Ginseng Research
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    • v.40 no.3
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    • pp.251-259
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    • 2016
  • Background: Estrogen signaling pathways are modulated by exogenous factors. Panax ginseng exerts multiple activities in biological systems and is classified as an adaptogen. Zearalenol is a potent mycoestrogen that may be present in herbs and crops arising from contamination or endophytic association. The goal of this study was to investigate the impact of P. ginseng, zearalenol and estradiol in tests on spermatozoal function. Methods: The affinity of these compounds for estrogen receptor (ER)-alpha and beta ($ER{\alpha}$ and $ER{\beta}$)-was assessed in receptor binding assays. Functional tests on boar spermatozoa motility, movement and kinematic parameters were conducted using a computer-assisted sperm analyzer. Tests for capacitation, acrosome reaction (AR), and chromatin decondensation in spermatozoa were performed using microscopic analysis. Results: Zearalenol-but not estradiol ($E_2$)- or ginseng-treated spermatozoa-decreased the percentage of overall, progressive, and rapid motile cells. Zearalenol also decreased spontaneous AR and increased chromatin decondensation. Ginseng decreased chromatin decondensation in response to calcium ionophore and decreased AR in response to progesterone ($P_4$) and ionophore. Conclusion: Zearalenol has adverse effects on sperm motility and function by targeting multiple signaling cascades, including $P_4$, $E_2$, and calcium pathways. Ginseng protects against chromatin damage and thus may be beneficial to reproductive fitness.

Expression of Codon Optimized β2-Adrenergic Receptor in Sf9 Insect Cells for Multianalyte Detection of β-Agonist Residues in Pork

  • Liu, Yuan;Wang, Jian;Liu, Yang;Yang, Liting;Zhu, Xuran;Wang, Wei;Zhang, Jiaxiao;Wei, Dong
    • Journal of Microbiology and Biotechnology
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    • v.29 no.9
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    • pp.1470-1477
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    • 2019
  • ${\beta}_2$-adrenergic receptor (${\beta}_2-AR$) was expressed efficiently using Bac-to-Bac Baculovirus Expression System in Sf9 cells as a bio-recognition element for multianalyte screening of ${\beta}$-agonist residues in pork. Sf9 cells were selected as the expression system, and codon optimization of wild-type nucleic acid sequence and time-dependent screening of expression conditions were then carried out for enhancing expression level and biological activity. Under optimum conditions of multiplicity of infection (MOI) = 5 and 48 h post transfection, the protein yield was up to 1.23 mg/ml. After purification by chromatographic techniques, the purified recombinant protein was applied to develop a direct competitive enzyme-linked receptor assay (ELRA) and the efficiency and reliability of the assay was determined. The IC50 values of clenbuterol, salbutamol, and ractopamine were 28.36, 50.70, and $59.57{\mu}g/l$, and clenbuterol showed 47.61% and 55.94% cross-reactivities with ractopamine and salbutamol, respectively. The limit of detection (LOD) was $3.2{\mu}g/l$ and the relevant recoveries in pork samples were in the range of 73.0-91.2%, 69.4-84.6%, and 63.7-80.2%, respectively. The results showed that it had better performance compared with other present nonradioactive receptorbased assays, indicating that the genetically modified ${\beta}_2-AR$ would have great application potential in detection of ${\beta}$-agonist residues.

Synthesis and Exploratory Photochemistry of ${\beta},\;{\gamma}$-unsaturated Carboxylic Acid, Carboxamide and Nitrile Derivatives (${\beta},\;{\gamma}$-불포화카르복시산, 카르복시아미드와 니트릴 유도체의 합성과 이들의 광화학적 반응에 관한 연구)

  • Givens Richard S.;Woo Ki Chae
    • Journal of the Korean Chemical Society
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    • v.26 no.2
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    • pp.99-106
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    • 1982
  • The ketone chromophore of 1-Acetyl-1-methyl-2-cyclopentene (1) was replaced by nitrile, carboxylic acid and acetamide group, and their photochemical reactions were investigated. While the ${\beta},\;{\gamma}$-unsaturated ketone 1 afforded 1,2 ar 1,3-Acyl shift product, these replaced chromophores did not afford any monomeric rearranged products. 1-Cyano-1-methyl-2-cyclohexene also afforded no product anology of the 1,2-acyl shift reaction. The replacement of the ketone chromophore by nitrile, carboxylic acid and carboxamide has greatly altered the photochemistry of ${\beta},\;{\gamma}$-unsaturated ketones.

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Isolation of Hyaluronidase Inhibitory Component from the Roots of Astraglus membranaceus Bunge (Astragali Radix)

  • Lee, Yun-Mi;Choi, Soo-Im;Lee, Jae-Won;Jung, Sun-Mi;Park, Sang-Min;Heo, Tae-Ryeon
    • Food Science and Biotechnology
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    • v.14 no.2
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    • pp.263-267
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    • 2005
  • In order to isolate hyaluronidase (HAase) inhibitor from Astragali radix (AR), dried roots were extracted with ethanol, prior to sequential fractionations with n-hexane, chloroform, ethyl acetate, n-butanol, and aqueous fractions. The n-butanol soluble fraction was found to exhibit the most pronounced inhibitory effect (68%) on HAase, and the active components were separated using various chromatographic methods, including column chromatography and preparative HPLC. The active component was isolated from the n-butanol soluble fraction of AR and was structurally identified as calycosin-7-O-${\beta}$-D-glucopyranoside by LC-MS, IR, $^1H$ NMR, and $^{13}C$ NMR analysis. The $IC_{50}$ of calycosin-7-O-${\beta}$-D-glucopyranoside's HAase activity was found to be 3.7 mg/mL.