• Biomolecules & Therapeutics
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• v.32 no.4
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• pp.442-450
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• 2024

The type-1 cannabinoid receptor (CB₁R) is a potential therapeutic target in several pathological conditions, including neuropsychological disorders and neurodegenerative diseases. Owing to their structural diversity, it is not easy to derive general structure-activity relationships (SARs) for CB₁R ligands. In this study, CB₁R ligands were classified into six structural families, and the corresponding SAR was determined for their affinities for CB₁R. In addition, we determined their functional activities for the activation of extracellular signal-regulated kinases (ERKs). Among derivatives of indol-3-yl-methanone, the highest ligand affinity was observed when a pentyl and a naphthalenyl group were attached to the N1 position of the indole ring and the carbon site of the methanone moiety, respectively. In the case of adamantane indazole-3-carboxamide derivatives, the presence of fluorine in the pentyl group, the substituent at the N1 position of the indazole ring, strongly increased the affinity for CB₁R. For (naphthalen-1-yl) methanone derivatives, the presence of 4-alkoxynaphthalene in the methanone moiety was more beneficial for the affinity to CB₁R than that of a heterocyclic ring. The functional activities of the tested compounds, evaluated through ERK assay, were correlated with their affinity for CB₁R, suggesting their agonistic nature. In conclusion, this study provides valuable insight for designing novel ligands for CB₁R, which can be used to control psychiatric disorders and drug abuse.

• 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.

• Transactions of the Korean Society of Mechanical Engineers A
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• v.38 no.10
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• pp.1147-1155
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• 2014

Biomechanical models are often used to predict muscle and joint forces in the human body. For estimation of muscle forces, the body and muscle properties have to be known. However, these properties are difficult to measure and differ from person to person. Therefore, it is necessary to predict the change in muscle forces depending on the body and muscle properties. The objective of the present study is to develop a numerical procedure for estimating the muscle forces in the human lower extremity under uncertainty of body and muscle properties during rising motion from a seated position. The human lower extremity is idealized as a multibody system in which eight Hill-type muscle force models are employed. Each model has four degrees of freedom and is constrained in the sagittal plane. The eight muscle forces are determined by minimizing the metabolic energy consumption during the rising motion. Uncertainty analysis is performed using a first-order reliability method. The one-standard-deviation range of agonistic muscle forces is calculated to be about 150-300 N.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.3
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• pp.309-316
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• 2017

Transient receptor potential vanilloid 3 (TRPV3) is a non-selective cation channel with modest permeability to calcium ions. It is involved in intracellular calcium signaling and is therefore important in processes such as thermal sensation, skin barrier formation, and wound healing. TRPV3 was initially proposed as a warm temperature sensor. It is activated by synthetic small-molecule chemicals and plant-derived natural compounds such as camphor and eugenol. Schisandra chinensis (Turcz.) Baill (SC) has diverse pharmacological properties including antiallergic, anti-inflammatory, and wound healing activities. It is extensively used as an oriental herbal medicine for the treatment of various diseases. In this study, we investigated whether SC fruit extracts and seed oil, as well as four compounds isolated from the fruit can activate the TRPV3 channel. By performing whole-cell patch clamp recording in HEK293T cells overexpressing TRPV3, we found that the methanolic extract of SC fruit has an agonistic effect on the TRPV3 channel. Furthermore, electrophysiological analysis revealed that ${\gamma}$-schisandrin, one of the isolated compounds, activated TRPV3 at a concentration of $30{\mu}M$. In addition, ${\gamma}$-schisandrin (${\sim}100{\mu}M$) increased cytoplasmic $Ca^{2+}$ concentrations by approximately 20% in response to TRPV3 activation. This is the first report to indicate that SC extract and ${\gamma}$-schisandrin can modulate the TRPV3 channel. This report also suggests a mechanism by which ${\gamma}$-schisandrin acts as a therapeutic agent against TRPV3-related diseases.

• 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.

• Journal of the Korean Society of Radiology
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• v.7 no.6
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• pp.427-431
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• 2013

The purpose of this study in the patient suffering from scoliosis analyse the degree of scoliosis, Cobb's angle, by Yoga exercise therapy and then find the effects of Yoga program on idiopathic scoliosis. In this study, yoga program restores flexibility and elasticity by relaxing and contracting muscles around vertebrea. It could help scoliosis from balancing agonistic muscle, antagonistic muscle and synergistic muscle during exercise. so did pelvis movement and vertebral twisting movement. The subject for this experiment was a meddle school girl diagnosed with scoliosis in C hospital in Gwang-ju city. In order to find the effects of yoga program on idiopathic scoliosis, conducted yoga program 60minutes a day, 5days a week for 12weeks. Before and after experiment, measured Cobb's angle by radiation and verified effects. First, master of yoga and chiropractor studied and made movement together. Second, Yoga program-developed about scoliosis was prescribed for the meddle school girl suffering from scoliosis during 12weeks. Third, Feasibility and effect was verified on idiopathic scoliosis by yoga program. As a result, the amount of curvature was reduced about 5degrees than before and improved the idiopathic scoliosis. Lots of Yoga movements help patients of idiopathic scoliosis to be improved. It shows that Yoga program could give adolescent scoliosis a hand.

• Korean Journal of Poultry Science
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• v.38 no.1
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• pp.1-4
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• 2011

A 35-day trial was conducted to examine the influence of floor density on the behaviour of broiler chickens. Day-old male broilers (n=756) were randomly assigned to one of four stocking densities (6 replicates of n=13, 25, 38 and 50) in 24 identical 2.6 $m^2$ pens. These stocking densities were coded very low (VL), low (L), medium (M) and high (H) and contained a floor space allowance per bird of 2,000 $cm^2$, 1,000 $cm^2$, 667 $cm^2$ and 500 $cm^2$, respectively. Scan sampling of all groups was carried out at 15-min intervals during two 1-h periods (10.00 h~11.00 h and 14.00 h~15.00 h) for five days each week. The numbers of birds engaged in different behavioural activities were recorded. It was found that the most common behaviour in all densities was lying. There was no clear effect of density during wks 1~4 of the trial, but in wk 5 birds in the L, M and H groups showed lower levels (P=0.07) of lying behaviour when compared to birds in the VL group suggesting that an increase in animal density results in decreased opportunities for undisturbed rest. This observation is supported by standing and walking behaviour, which was lower (P<0.05) in the VL group in wk 5. Foraging behaviour measured in the study by the numbers of birds pecking the ground declined as the trial progressed, but scratching increased in 2 wk then decreased. Birds in the VL group showed higher (P<0.05) level of pecking the ground behaviour compared to birds in the L, M and H groups, but scratching behaviour higher (P<0.05) and lower (P<0.05) in VL of 1 wk and 2 wk respectively. However, a peak in aggressive behaviour was observed in wk 2 and birds in the VL group showed less (P<0.05) agonistic behaviour than birds in the H and M groups. Other behaviours (dustbathing, preening, eating or drinking) were not influenced (P>0.05) by stocking density.

• Journal of Life Science
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• v.20 no.7
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• pp.969-976
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• 2010

In vivo studies of KR-31125 (2-butyl-5-dimethoxymethyl-6-phenyl-7-methyl-3-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) were performed in pithed rats, conscious angiotensin II (AII) challenged normotensive rats, renal hypertensive rats (RHRs) and furosemide-treated beagle dogs. KR-31125 induced a non-parallel right shift in the dose-pressor response curve to AII ($ID_{50}$: 0.095 mg/kg) with a dose-dependent reduction in the maximum responses in pithed rats. Compared to losartan, this antagonistic effect was about 18 times more potent, presenting competitive antagonism. Other agonists such as norepinephrine and vasopressin did not alter the responses induced by KR-31125. Orally administered KR-31125 had no agonistic effect and dose-dependently inhibited the pressor response to AII with a slightly weaker potency ($ID_{50}$: 0.25 and 0.47 mg/kg, respectively) in the AII-challenged normotensive rat model, but with a more rapid onset of action than losartan (time to $E_{max}$: 30 min for KR-31125 and 6 hr for losartan). KR-31125 produced a dose-dependent antihypertensive effect with a higher potency than losartan in RHRs, and these effects were confirmed in furosemide-treated dogs where they presented a dose-dependent and long-lasting (>8 hr) antihypertensive effect with a rapid onset of action (time to $E_{max}$: 2-4 hr), as well as a 20-fold greater potency than losartan. These results suggest that KR-31125 is a potent, orally active $AT_1$ receptor antagonist that can be applied to the development of new diagnostic and research tools as an added exploratory potential of $AT_1$ receptor antagonist.

• Information Systems Review
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• v.24 no.1
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• pp.105-123
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• 2022

Thanks to the remarkable success of Artificial Intelligence (A.I.) techniques, a new possibility for its application on the real-world problem has begun. One of the prominent applications is the bankruptcy prediction model as it is often used as a basic knowledge base for credit scoring models in the financial industry. As a result, there has been extensive research on how to improve the prediction accuracy of the model. However, despite its impressive performance, it is difficult to implement machine learning (ML)-based models due to its intrinsic trait of obscurity, especially when the field requires or values an explanation about the result obtained by the model. The financial domain is one of the areas where explanation matters to stakeholders such as domain experts and customers. In this paper, we propose a novel approach to incorporate financial domain knowledge into local rule generation to provide explanations for the bankruptcy prediction model at instance level. The result shows the proposed method successfully selects and classifies the extracted rules based on the feasibility and information they convey to the users.

• Microbiology and Biotechnology Letters
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• v.36 no.3
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• pp.227-232
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• 2008

Biological antagonists of Phytophthora capsici were isolated from soil in Gyeongbuk, Korea. Among the isolated bacteria, a Bacillus sp. was identified from l6S rDNA sequence analysis and named Bacillus sp. AM-651. Bacillus sp. AM-65l strain which can strongly a antifungal activity against Phytophthora capsici. Culture conditions for the maximum production of the antagonistic substance were optimized. The production of antibiotic were high on modified Davis mineral medium pH 7 at $30^{\circ}C$. The medium for highest production of the agonistic substance optimized. It is composed the best activity on glucose, $(NH_4)_2SO_4$ and $K_2HPO_4$ at 0.5%, 0.1%, and 0.7%, respectively. By time course of culture solution selected Bacillus sp. AM-65l, the culture solution after 48hrs had strongly growth inhibition rate against P. capsici. And culture solution of Bacillus sp. AM-651 was stable within a pH range $5{\sim}11$ and temperature range $4{\sim}70^{\circ}C$. Bacillus sp. AM-651 cultured broth shown fungal growth inhibitory activity against B. sorokiniana, B. cinerea, R. solani avove and beyond P. capsici and comparatively showed a high activity against C. gloeosporioides, B. dothidea, B. cinerea and F. graminearum by agar diffusion method.