• Title/Summary/Keyword: 저해모델

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Melanogenesis Inhibitory Activities of Mulberry Seed Ethanol Extracts (오디씨 에탄올 추출물의 멜라닌 합성 억제효과)

  • Jeong, Yong Tae;Kang, Min Ju;Kim, Jin Hee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.41 no.3
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    • pp.263-268
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    • 2015
  • The purpose of this study was to investigate anti-melanogenesis effects of mulberry seed extracts (MSE). MSE inhibited melanogenesis in melan-a cells at $10{\mu}g/mL$ without cytotoxicity. Also, MSE decreased tyrosinase, tyrosinase-related protein-1 (TRP-1) protein expression in the melan-a cells. To identify the signaling pathway of MSE, the ability of MSE to influence extracellular signal-regulated protein kinase (ERK) activation was investigated. MSE induced ERK protein expression in a dose-dependent manner. In addition, MSE presented inhibition of the body pigmentation in vivo zebrafish model. These results suggest that MSE may be an effective anti-melanogenesis agent regulating the expression of ERK protein and melanogenic enzymes.

유전독성물질의 평가방법과 그 기작에 관한 연구

  • 이정섭;박종근;박종광;박상대
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.170-170
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    • 1993
  • 유전독성물절외 검출과 평가에 용이하게 사용할 수 있는 모델 시스템의 개발 및 DNA 회복기작을 규명할 목적으로 수종의 돌연변이, 발암원을 이용하여 배양 포유동물세포 및 어류세포에서 세포생존률, DNA 합성 및 복제억제의 양상 등을 비교 분석하였다. MMS및 MNNG 와 같은 알칼라제는 CHO 세포에서 유의한 DNA 합성저해, DNA 복재억제, DNA 단사절단 및 비주기성 DNA 합성률의 증가를 유발하였다. Benzo(a)pyrene과 3-methylcholanthrene좌 같은 DNA 상해 전구물질의 경우 유전독성 여부의 판정에는 반드시 S-9/15과 같은 대사활성계 또는 mouse embryonic fibroblast와 같은 대사 활성능이 있는 세포와의 co-culture system들이 필요함을 확인하였으며, 이들에 의한 DNA 상해와 복재억제 유도의 작용양상은 자외선의 작용양상과 유사하였다. 배양 어류세포에서 자외선에 의한 세포생존율의 측정, 광재활성능의 분석 및 자외선에 의해 유발된 피리미딘 이량체 절제능 검토 및 DNA 합성 저해능의 결과를 분석함으로써 유전독성 평가를 위한 모델 시스템 구축의 기초결과를 얻었다.

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Edge model based digital still image enlargement considering low-resolution CCD device characteristics (저해상도 CCD 소자 특성을 고려한 경계 모델 기반 디지털 정지 영상 확대)

  • 전준근;최영호;김한주;박규태
    • The Journal of Korean Institute of Communications and Information Sciences
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    • v.23 no.9A
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    • pp.2345-2354
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    • 1998
  • There have been many researches to yield higher resolution image quality from the low resolution CCD device. The resolution of it is primary factor for the image quality of digital still camera and in manufacturing price. IN this paper, image enlargement algorithm, which reduces blocking effect of enlarged low resolution image and minimizes ringing and blur effect occurring around edge in linear interpolation, is proposed. This algorithm is composed of gaussian low pass filter which eliminates aliasing, least square spline interpolation and non-linear interpolation based on step edge model.

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Antibiotics; Methicillin, Cefamandole and Oxytetracycline, Can Modulate the Activity of Human Neutrophil Elastases (Methicillin, Cefamandole, Oxytetracycline에 의한 사람 호중구 Elastase의 변화)

  • Ghim, Sa-Youl;Jeong, Hye-Young;Bae, Sung-Jun;Kang, Koo-Il
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.109-113
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    • 1989
  • Human neutrophil elastase (HNE, EC 3, 4 21, 11), a major causative factor in the induction of pulmonary emphysema, were purified by two steps of liquid chromatography. Purified elastases were cross-reacted with antibody to human neutrophil elastases. Methicillin and cefamandole, which are known as inhibitors of cell wall synthesis of microorganisms, could inhibit the activity of human neutrophil elastase up to 50% with 10mM of both agents and $IC_{50}$ of methicillin was 9.8 mM. Gentamicin, one of the aminoglycosides, also inhibits human neutrophil elastases up to 60% of original activity with 10 mM of this agent and $IC_{50}$ was 9.0 mM. We could demonstrate similar effects in oxytetracycline. 10 mM of oxytetracycline inhibited 95% of human neutrophil elastase and $IC_{50}$ was 0.3 mM. Overall, oxytetracycline, cefamandole and methicillin are strong inhibitors of human neutrophil elastase, and they could be a drug of cholice for the diseases which were known as pathogenesis related to elastase. We also suggest that the mechanism of action of these antibitics are different from the mechanism of antimicrobial effects like inhibition of both cell wall synthesis and protein synthesis.

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Simulation Study of Dynamic Network Model for L-Threonine Biosynthesis in Escherichia coli (대장균의 동역학 네트워크 모델을 이용한 L-threonine 생합성에 관한 모사 연구)

  • Jung, Uisub;Lee, Jinwon
    • Korean Chemical Engineering Research
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    • v.44 no.1
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    • pp.97-105
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    • 2006
  • In order to investigate the effect of inhibitors on L-threonine biosynthesis in Escherichia coli, we have constructed a metabolic network model of amino acid biosynthesis from L-aspartate to L-threonine by using available informations from literatures and databases. In the model, the effects of inhibitors on the biosynthesis of L-threonine was included as an appropriate mathematical form. For simulation study, we used initial values as L-aspartate 5 mM, ATP 5 mM, NADPH 2 mM, and observed the concentration changes of intermediate metabolites over concentration changes of respective inhibitors. As a result, we found that concentrations of intermediate metabolites were not significantly changed over concentration changes of L-lysine, L-methionine, and L-glutamate. But, there were considerable changes of intermediates over concentration changes of L-serine, L-cysteine, and L-threonine, which can be considered as essential effectors on L-threonine synthesis. Contrary, the synthesis of L-threonine seems to be not related to the amounts of L-aspartate, and inversely proportional to the accumulated amount of D,L-aspartic ${\beta}$-semialdehyde.

Vehicle Segmentation Scheme Based on the Hidden Markov Model in Traffic Sequence (교통 영상에서 은닉 마르코프 모델을 이용한 차량 분할 기법)

  • Lee, Dae-Ho;Park, Young-Tae
    • Proceedings of the Korean Information Science Society Conference
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    • 2005.11b
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    • pp.850-852
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    • 2005
  • 본 논문에서는 교통 영상에서 실시간으로 차량을 검출하는 새로운 기법을 소개한다. 차량의 검출을 위하여 구배도의 방향 정보를 사용하며 차량 영역의 정확한 분할을 위하여 은닉 마르코프 모델을 사용한다. 구배도 방향정보를 이용하므로 그림자 영역의 영향을 줄일 수 있으며 은닉 마르코프 모델을 이용하므로 배경과 비슷한 차량과 근접한 차량의 분리가 가능하다. 따라서 저해상도의 교 통 영상에서 다양한 기상 조건, 그림자의 존재와 교통 상황에 강건한 검출 결과를 나타낸다.

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3D-QSAR Analyses on the Inhibition Activity of 4-Hydroxybenzyl alcohol Analogues Against Tyrosinase (4-Hydroxybenzyl alcohol 유도체들의 Tyrosinase 활성 저해에 대한 3D-QSAR 분석)

  • Kim, Sang Jin;Sung, Nack Do
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.39 no.4
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    • pp.329-335
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    • 2013
  • Three-dimensional quantitative structure-activity relationships (3D-QSARs) models between the substituents with changing groups ($R_1$ & $R_2$) of 4-hydroxybenzyl alcohol (4-HBA) derivatives as substrate molecule and their inhibitory activities against tyrosinase were derived and discussed quantitatively. The optimized CoMSIA FF model showed the best predictability and fitness ($r^2$ = 0.858 & $q^2$ = 0.951). The contour maps of the optimized CoMSIA FF model showed that, the inhibitory activities of the analogues against tyrosinase were expected to increase when hydrophobic (Hy) favor, negative charge (E) favor, steric (S) disfavor and hydrogen bond donor (HD) disfavor groups were substituted at the $R_2$ position. When the hydrogen bond donor (HD) favor groups were substituted at the $R_1$ position, it is predicted that the substituents will be able to increase the inhibitory activity.

한국 남해 대륙붕 후 제4기 퇴적층의 순차 층서 모델

  • 유동근;이호영;남승일
    • Proceedings of the Korean Quaternary Association Conference
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    • 2004.06a
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    • pp.7-7
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    • 2004
  • 한국 남동해역 대륙붕에서 취득된 고해상 탄성파 탐사자료와 퇴적물 시료의 분석에 의하면 후 제4기 퇴적층은 마지막 빙하기 이후의 해수면 변화에 의해 조절되는 저해수면계열, 해침계열, 고해수면계열로 구성된다. 시퀀스 경계면 위의 저해수면계열(층서단위 I)은 마지막 빙하기 동안 퇴적된 니질사 혹은 사질니 퇴적물로 구성되며 대륙붕단과 해곡의 외해역에 분포한다. 해침면과 최대 해침면 사이에 위치하는 해침계열(층서단위 II)은 지난 15,000-6,000년 사이에 퇴적되었으며 주로 사질퇴적물로 구성된다. 해침계열은 연구해역 전반에 걸쳐 넓게 분포하지만 저해수면계열과 고해수면계열에 비해 박층으로 분포한다. 이러한 해침계열은 분포특성에 따라 3개의 소퇴적단위로 세분된다. 즉, 대륙붕단의 초기해침계열(Unit IIa), 중간대륙붕의 중기해침계열(Unit IIb), 내대륙붕의 후기해침계열(Unit IIc)등으로 이들은 후배열층서의 특성을 가진다. 최대해침면 상부에 놓이는 고해수면계열(층서단위 III)은 해수면이 현 수준에 도달한 지난 약 6,000년 이후에 퇴적된 현생 니질 퇴적물로 구성되며 내대륙붕의 연안을 따라 제한적으로 분포한다.

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2D-QSAR analysis for hERG ion channel inhibitors (hERG 이온채널 저해제에 대한 2D-QSAR 분석)

  • Jeon, Eul-Hye;Park, Ji-Hyeon;Jeong, Jin-Hee;Lee, Sung-Kwang
    • Analytical Science and Technology
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    • v.24 no.6
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    • pp.533-543
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    • 2011
  • The hERG (human ether-a-go-go related gene) ion channel is a main factor for cardiac repolarization, and the blockade of this channel could induce arrhythmia and sudden death. Therefore, potential hERG ion channel inhibitors are now a primary concern in the drug discovery process, and lots of efforts are focused on the minimizing the cardiotoxic side effect. In this study, $IC_{50}$ data of 202 organic compounds in HEK (human embryonic kidney) cell from literatures were used to develop predictive 2D-QSAR model. Multiple linear regression (MLR), Support Vector Machine (SVM), and artificial neural network (ANN) were utilized to predict inhibition concentration of hERG ion channel as machine learning methods. Population based-forward selection method with cross-validation procedure was combined with each learning method and used to select best subset descriptors for each learning algorithm. The best model was ANN model based on 14 descriptors ($R^2_{CV}$=0.617, RMSECV=0.762, MAECV=0.583) and the MLR model could describe the structural characteristics of inhibitors and interaction with hERG receptors. The validation of QSAR models was evaluated through the 5-fold cross-validation and Y-scrambling test.

CoMSIA Analysis on The Inhibition Activity of PTP-1B with 3${\beta}$-Hydroxy-12-oleanen-28-oic Acid Analogues (3${\beta}$-Hydroxy-12-oleanen-28-oic Acid 유도체들의 PTP-1B저해활성에 대한 CoMSIA분석)

  • Kim, Sang-Jin;Chung, Young-Ho;Kim, Se-Gon;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.51 no.3
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    • pp.171-176
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    • 2008
  • The comparative molecular similarity indices analysis (CoMSIA) models between 3${\beta}$-Hydroxy-12-oleanen-28-oic acid (1-30) analogues as substrate molecule and their inhibitory activities ($pI_{50}$) against protein tyrosine phosphatase (PTP)-1B were derived and discussed quantitatively. Listing in order, the CoMFA>CoMSIA${\geq}$HQSAR>2D-QSAR model, these QSAR models had the better statistical values. The optimized CoMSIA F1 model at grid 3.0${\AA}$ had the best predictability and fitness ($q^2$=0.754 and $r^2$=0.976) by field fit alignment. The order of contribution ratio (%) of CoMSIA fields concerning the inhibitory activities was a H-bond acceptor (48.9%), steric field (25.8%) and hydrophobic field (25.4%), respectively. Therefore, the inhibitory activities of substrate molecules against PTP-1B were dependent upon H-bond acceptor field (A) of $R_4$-group. From the analytical results of CoMSIA contour maps, oleanolic acid derivatives will have better inhibition activities if $R_1$ group has H-bond acceptor disfavor, $R_3$group has steric disfavor and $R_4$ group has steric, hydrophobic, H-bond favor.