• Development and Reproduction
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• v.12 no.3
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• pp.275-281
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• 2008

Endocrine disrupting chemiclas (EDCs) such as bisphenol A (BPA) and nonylphenol (NP) have estrogenic activity and can alter reproduction in fish. In the present study, the effects of BPA and NP on in vitro steroid production from oocytes of maturation stage (oocyte diameter$\fallingdotseq$1.88 mm) from the greenling (Hexagrammos agrammus) were evaluated. Oocytes were incubated with different concentrations of BPA and NP (0.1, 1, 10, 100 and 1,000 ng/$m{\ell}$) in the presence or absence of 50 IU human chorionic gonadotropin (HCG) for 48 hours. After incubation, levels of $17{\alpha},\;20{\beta}$-dihydroxy-4-pregnen-3-one ($17{\alpha}20{\beta}OHP$), estradiol-$17{\beta}(E_2)$ and testosterone (T) from incubated media were quantified by radioimmunoassay (RIA). In BPA treatment, 100 ng/$m{\ell}$ of BPA stimulated $E_2$ production regardless HCG supplement. Every concentration of BPA inhibited T production without HCG although 0.1 ng/$m{\ell}$ of BPA stimulated T production with HCG. In NP treatment, 10 ng/$m{\ell}$ of NP stimulated $17{\alpha}20{\beta}OHP$ and T production without HCG. 1 ng/$m{\ell}$ of NP inhibited $E_2$ production. Taken toghther, these results suggest that BPA might have weak estrogen-agonistic effect and NP has estrogenantagonistic effect at final oocyte maturation stage of H. agrammus.

• Journal of the Korea Convergence Society
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• v.8 no.1
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• pp.115-121
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• 2017

AHR is a transcription factor activated by aryl hydrocarbons, regulating the expression of XMEs (xenobiotics Metabolizing Enzymes). Even though the role of AHR in human physiology has been intensively investigated for the past decades, our understandings are still largely limited due to the deficiency of adequate chemical agents. In addition, it has been demonstrated that AHR correlates to pathogeneses for some diseases. Furthermore, emerging data suggest that the study on the AHR may provide a valid therapeutic target. Classical antagonists in current use are reported to be partial agonistic whereas a pure antagonist is demanded. In this study, o-toluidinyl ring structure of 2-methyl-4-(2-methylphenyldiazenyl)phenyl picolinamide has been modified into various structures to optimize the AHR antagonistic activity by means of convergence study of organic synthesis and molecular biology.

• Asian-Australasian Journal of Animal Sciences
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• v.30 no.6
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• pp.902-906
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• 2017

Objective: This study was conducted to characterize the behaviors and the body weight of suckling piglets in different social environments. Methods: Two groups of sows and suckling piglets housed either in individual farrowing crates in separate pens ($1.8{\times}2.4m$, the control group) or in groups of three sows with their piglets in farrowing crates in a large common enclosure ($5.4{\times}2.2m$, the treatment group) were observed with the aid of video technology for 9 consecutive hours on days 1, 2, and 3, after mixing. Results: Suckling, agonistic, and elimination behaviors of suckling piglets were significantly higher in the control group than in the treatment group. Inactive behavior was higher in the treatment group than in the control group. Most of the effects of the social environment on the suckling piglets seem to be the result of large reductions in behaviors and body weight for piglets switching from high activity to low activity. Moreover, suckling behavior and birth body weight were highly correlated with body weight at the end of the test. Conclusion: The social environment that resulted from mixing, thus, had significant effects on the behavior and body weight of suckling piglets, and behavioral characteristics, therefore, should be considered when making improvements to the husbandry and care methods used in swine production.

• Biomolecules & Therapeutics
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• v.12 no.4
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• pp.215-220
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• 2004

In an attempt to develop new anti-diabetic agents, a series of aryloxypropanolamine derivatives was synthesized to serve as ${\beta}_3$ adrenoceptor agonists. Among these derivatives, 1-{1-methyl-3-[4-(2-methyl-2H-1,2,3,4-tetrazol-5-yl)phenyl]propylamino}-3-phenoxy-2-propanol (KR60886) possessed a high affinity for the ${\beta}_3$ adrenoceptor (Ki = 28 nM) and moderate affinities for ${\beta}_1$ and ${\beta}_2$ adrenoceptors (Ki = 95 nM and 100 nM, respectively). In addition, KR60886 stimulated cAMP production with an EC$_{50}$ of 0.4 ${\mu}M$, confirming its agonistic activity for the ${\beta}_3$ adrenoceptor. In vivo activities of KR60886 were examined by using a fat-fed/streptozotocin (STZ)-treated rat model and the ob/ob mouse model. Oral administration of KR60886 (10 mg/kg) for 3 days (b.i.d.) to fat-fed/STZ-treated rats significantly lowered plasma glucose levels and reduced plasma free fatty acid concentrations. Similarly, KR60886 treatment (10 mg/kg/day for 7 d) resulted in a reduction of plasma glucose concentrations in ob/ob mice. The present study suggests that KR60886 is a potent ${\beta}_3$ receptor agonist with in vivo anti-diabetic properties.

• Korean Journal of Applied Biomechanics
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• v.25 no.3
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• pp.265-274
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• 2015

Objective : The purpose of this study was to analyze the effect of the elastic band on ballet arabesque based on kinematics analysis. Methods : To observe the effect of the elastic band, the availability of the elastic band during movement was set as the independent variable, and the dependent variables were set by using factors from two different categories such as motor mechanics and kinematics variables. For motor mechanics variable, the muscle activity and the center of pressure(COP)'s trajectory and velocity were used. Furthermore, the physical angle was used for kinematic variables. Data samples from the experiment was used to understand the correlation between independent and dependent variables while using paired samples t-test as a data analysis tool. Results : After analyzing the result of experiment, the usage of the Elastic band on ballet arabesque movement seemed to increase the activity of the agonistic muscle, which is mainly used for movement, and to improve the stability of the supporting leg by decreasing the trajectory and velocity of the center of pressure(COP). Moreover, the elastic band increased the level of elevation of the stretching leg with reducing the angle of the hip joint that resulted into a more stable movement and furthermore providing more beauty while standing on it. Conclusion : The movement training program while the using elastic band are expected to lead to appropriate muscular development and reduce the muscle imbalance, which usually occurs to dancers, during training with unfamiliar specific movements or strengthening muscular strength for a specific movement. In addition, this work is expected to be used as a training reference to understand and learn the fundamentals of movements of ballet and other dance fields.

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.325-330
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• 1997

Methanol extract of G. elata inhibited the binding of [/sup 3/H]Rol5-1788, a selective benzodiazepine receptor antagonest, to benzodiazepine receptor of rat cortices. Saturation experiments followed by Scatchard analysis of the results showed that the inhibition of [sub 3/H]Ro15-1788 binding by G. dlata. appeared to be com-petitive. These competitive inhibiton of the butanol fraction was observed to be higher than the methanol extract. Methanol extract of G. efara inhibited a [sub 3/H]flunitrazepam, a selective benzodiazepine receptor agonist, binding to benzodiazepine receptor. GABA significantly enhanced the inhibition of [/sub 3/H]flunitrazepam binding by G. elata, and these "positive GABA shift" supported the strong possibility of agonestic activity to benzodiazepine receptor Butanol fraction was observed to be higher than crude extract by methanol in an agonistic activity to benzodiazepine receptor, furthermore enhanced the binding of [sub 3/H]SR95531 to GABA receptor. Butanol fraction of G. elata significantly diminished the pentylenetetrazole-induced lethality of mice. From these results, it can be concluded that substance or substances with neurochemical properties characteri- stic of a benzodiazepine receptor agonist may be important components, and contribute to the anticonvulsant property of G. elata.

• Journal of the Korea Convergence Society
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• v.10 no.1
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• pp.285-290
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• 2019

AHR regulates the expression of xenobiotics metabolizing enzymes (XMEs) as a transcription fact upon binding of ligands that are mainly aryl hydrocarbons. The role of AHR in human physiology has been intensively investigated for the past decades, however our understanding on AHR yet to be elucidated largely due to the lack of proper chemical agents. It has been demonstrated that AHR correlates to pathogenesis for some diseases in recent studies suggesting that the study on the AHR may provide a valid therapeutic target. Classical antagonists in current use are reported to be partially agonistic whereas a pure antagonist is yet to be found. In this study, phenyldiazenylaniline has been designed based on the structure of two known AHR antagonist, Resveratrol and CH223191. The derivatives of phenyldiazenylaniline have been prepared and subjected to assessment as an AHR antagonist in order to optimize the AHR antagonistic activity of the designed structure by means of convergence study of organic synthesis and molecular biology.

• Biomolecules & Therapeutics
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• v.26 no.6
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• pp.539-545
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• 2018

4-Hydroxy-2-(4-hydroxyphenethyl)isoindoline-1,3-dione (PD1) is a synthetic phthalimide derivative of a marine compound. PD1 has peroxisome proliferator-activated receptor (PPAR) ${\gamma}$ agonistic and anti-inflammatory effects. This study aimed to investigate the effect of PD1 on allergic asthma using rat basophilic leukemia (RBL)-2H3 mast cells and an ovalbumin (OVA)-induced asthma mouse model. In vitro, PD1 suppressed ${\beta}$-hexosaminidase activity in RBL-2H3 cells. In the OVA-induced allergic asthma mouse model, increased inflammatory cells and elevated Th2 and Th1 cytokine levels were observed in bronchoalveolar lavage fluid (BALF) and lung tissue. PD1 administration decreased the numbers of inflammatory cells, especially eosinophils, and reduced the mRNA and protein levels of the Th2 cytokines including interleukin (IL)-4 and IL-13, in BALF and lung tissue. The severity of inflammation and mucin secretion in the lungs of PD1-treated mice was also less. These findings indicate that PD1 could be a potential compound for anti-allergic therapy.

• Korean journal of applied entomology
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• v.43 no.2
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• pp.143-153
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• 2004

Non-spinning syndrome of Bombyx mori has been serious issue in sericulture industry near Kyungbuk area. This study was focused on the analysis of the mechanism and on screening candidate chemicals inducing the anti-metamorphosis of the silkworms. Rearing temperatures or initial body weight of the final instar larvae did not affect a normal larval to pupal metamorphosis of B. mori. However, pyriproxyfen (a juvenile hormone (JH) agonist) induced follicle patency significantly even at its 10$\^$-8/ M concentration and inhibited metamorphosis of B. mori in both developmental time and dose dependent manners. Pyriproxyfen induced JH esterase (JHE) activity and downregulated expression of JH binding protein of 5. mori. These results suggests that pyriproxyfen induced JHE activity as a JH agonist and that the elevated JHE activity degraded endogenous JH and resulted in JHBP gene expression. Based on the fact that the JH agonist induced follicle patency and inhibited metamorphosis of B. mori, follicle patency bioassay suggested that three commercial pesticides including simazine, molinate or alachlor were proved to give potent JH agonistic effect on B. mori. Further direct exposure experiments to these candidates are required to determine the chemicals responsible for the non-spinning syndrome of 8. mori.

• IMMUNE NETWORK
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• v.3 no.4
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• pp.302-309
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• 2003

Background: CTLA4 (CD152), which is expressed on the surface of T cells following activation, has a much higher affinity for B7 molecules comparing to CD28, and is a negative regulator of T cell activation. In contrast to stimulating and agonistic capabilities of monoclonal antibodies specific to CTLA-4, CTLA4Ig fusion protein appears to act as CD28 antagonist and inhibits in vitro and in vivo T cell priming in variety of immunological conditions. We've set out to confirm whether inhibition of the CD28-B7 costimulatory response using a soluble form of human CTLA4Ig fusion protein would lead to persistent inhibition of alloreactive T cell activation. Methods: We have used CHO-$dhfr^-$ cell-line to produce CTLA4Ig fusion protein. After serum free culture of transfected cell line we purified this recombinant molecule by using protein A column. To confirm characterization of fusion protein, we carried out a series of Western blot, SDS-PAGE and silver staining analyses. We have also investigated the efficacy of CTLA4Ig in vitro such as mixed lymphocyte reaction (MLR) & cytotoxic T lymphocyte (CTL) response and in vivo such as experimental autoimmune encephalomyelitis (EAE), graft versus host disease (GVHD) and skin-graft whether this fusion protein could inhibit alloreactive T cell activation and lead to immunosuppression of activated T cell. Results: In vitro assay, CTLA4Ig fusion protein inhibited immune response in T cell-specific manner: 1) Human CTLA4Ig inhibited allogeneic stimulation in murine MLR; 2) CTLA4Ig prevented the specific killing activity of CTL. In vivo assay, human CTLA4Ig revealed the capacities to induce alloantigen-specific hyporesponsiveness in mouse model: 1) GVHD was efficiently blocked by dose-dependent manner; 2) Clinical score of EAE was significantly decreased compared to nomal control; 3) The time of skin-graft rejection was not different between CTLA4Ig treated and control group. Conclusion: Human CTLA4Ig suppress the T cell-mediated immune response and efficiently inhibit the EAE, GVHD in mouse model. The mechanism of T cell suppression by human CTLA4Ig fusion protein may be originated from the suppression of activity of cytotoxic T cell. Human CTLA4Ig could not suppress the rejection in mouse skin-graft, this finding suggests that other mechanism except the suppression of cytotoxic T cell may exist on the suppression of graft rejection.