• 약학회지
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• 제40권4호
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• pp.428-437
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• 1996

The in vitro and in vivo antibacterial activities of a new fluoroquinolone, DWP20364(1-cyclopropyl-5-amino-6,8-difluoro-7-(2,7-diazabicyclo[3.3.0]oto-4-ene-7-yl)-1 ,4-di-hydro-4-oxoquinoline-3-carboxylic acid) were evaluated in comparison with those of ciprofloxacin(CPFX), sparfloxacin(SPFX) and ofloxacin(OFLX). DWP20364 was more potent than CPFX and OFLX against Staphylococcus spp., Streptococcus spp. and Enterococcus faecium MD8b and it was similarly or slightly less active than CPFX against Escherichia spp. and Pseudomonas spp.. For MRSA and OFLX resistant strains (Staphylococcus spp.(14),Enterococcus spp.(4), Acinetobacter spp.(2), Pseudomonas spp.(9), Klebsiella spp.(2) and Serratia spp.(6)),DWP20364(MICs for 90% of strains,0.025 and 12.5${\mu}$g/ml, respectively) was 4 to 32 folds more potent than SPFX and CPFX. The activity of DWP20364 decreased moderately in the presence of 5mM $Mg^{2+}$. However, various pHs and the concentrations of various serum had no effect on the activity of DWP20364. DWP20364 possessed a bacteriocidal effect at the 1MIC against gram positive and gram negative strains. The protective effect of DWP20364 against systemic infections in mice caused by S. aureus Smith or S. aureus L2379 was superior to that of CPFX and SPFX but it was less active than that of CPFX against infection by P. aeruginosa E-2.

• Bulletin of the Korean Chemical Society
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• 제32권5호
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• pp.1650-1656
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• 2011

A series of potent tricyclic derivatives with a non-aromatic amide as potent PARP-1 inhibitors were successfully synthesized and their PARP-1 inhibitory activity was evaluated. Among the derivatives, 2-(1-propylpiperidin-4-yloxy)-7,8,9,10-tetrahydrophenanthridin-6(5H)-one 23c displayed potent activity in a PARP-1 enzymatic assay and cell-based assay ($IC_{50}$ = 0.142 ${\mu}M$, $ED_{50}$ = 0.90 ${\mu}M$) with good water solubility. Further, molecular modeling studies confirmed the obtained biological results.

• 대한화장품학회지
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• 제23권2호
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• pp.63-70
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• 1997

It has been observed that local increase in melanin synthesis or uneven distribution can cause local hyperpigmintation or spot. Pigmentary disorders are caused by various factors, including inflammation, imbalance of hormones, and genetic disorder. Recently the harmfulness of Ultraviolet radiation is increasing due to destruction of ozone layer. Excessive exposure to UV radiation caused post-inflammatory pigmentation. Most women want to avoid uneven skin pigmentation. To satisfy this desire many cosmetic companies have been developing melanogenesis inhibitors and finding promising active agents for use in cosmetic preparations for skin whitening. In cosmetic preparations, many inhibitors such as kojic acid, arbutin, ascorbic acid, and licorice extracts6 have been used as whitening purpose. Plant extracts having an inhibitory effect on melanin formation may be a good choice for cosmetic purpose because of their relatively lower side effects. Therefore, we screened 285 plant extracts for their inhibitory activity in tyrosinase. Of the plant extracts, ramulus mori extracts showed potent tyrosinase inhibition activity. We also identified the active compound in the extract.

• 대한화장품학회지
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• 제40권1호
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• pp.89-94
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• 2014

물푸레나무 수피 추출물은 주요 생활성 물질로서 esculetin과 esculin을 포함하고 있다. 이 가운데, Esculetin은 B16F10 melanoma cells에서 $IC_{50}$ value $2.8{\mu}M$의 아주 좋은 melanogenesis 억제 활성을 나타내며, 이를 통해 Melan-A cell에서 melanin 합성을 감소시킨다. 더욱이, esculetin은 mushroom tyrosinase에서도 $IC_{50}$ value $40{\mu}M$의 억제 활성을 나타내어 melanin biosynthesis를 저해한다. 위의 결과들로서, 우리는 melanogenic enzyme 활성 조절에 의해 melanin 생성을 저해하는 효과적인 피부미백 물질로서 esculetin을 제안하고자 한다.

• 한국식품과학회지
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• 제32권1호
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• pp.168-173
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• 2000

애사과 polyphenol의 충치예방효과를 확인하고자, S. mutans 4 균주 가운데 GTase 활성이 가장 높은 S. mutans MT 8148 균주에 대하여 애사과 polyphenol의 GTase 활성억제효과, cell adherence 억제효과, 산 생성억제효과를 측정하였다. S. mutans GTase에 대한 활성 억제효과는 애사과 polyphenol 성분 중 (+)-catechin과 tannic acid가 1 mg/ml의 농도에서 60% 이상, 5mg/ml의 농도에서 90% 이상으로 높게 나타났다. S. mutans의 adherence에 대해서는 tannic acid가 약 50% 정도의 억제효과를 나타냈으며, 애사과 추출물도 약 30%정도의 억제효과를 보였다. 그러나 S. mutans의 산 생성에 대해서는 애사과 polyphenol 성분들이 억제효과를 나타내지 못하는 것으로 나타났다. 애사과 polyphenol 성분들의 S. mutans에 대한 항균활성을 확인한 결과, 이들은 항균활성은 갖지 않는 것으로 나타났다. 애사과 polyphenol의 충치억제효과는 주성분중의 하나인 catechin과 tannic acid의 S. mutans GTase 활성억제와 cell adherence 억제효과로부터 기인된 것임을 알 수 있었다. 따라서 애사과 추출물은 충치예방을 위한 기능성 식품소재로 사용 가능할 것으로 생각된다.

• 대한의생명과학회지
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• 제13권1호
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• pp.39-45
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• 2007

Numerous psychological stressors playa role in development of the cardiovascular disease. The aim of this study was to determine whether a combined mental activity with experimental subway noise affects hematological physiology. Fifty-four healthy volunteers were divided group I which underwent subway noise (n=24) and group II which underwent a combined mental activity with subway noise (n=30). Venous blood samples were collected for measuring CBC, prothrombine time (PT), activated partial thromboplastine time (APTT), erythrocyte sedimentation rate (ESR), D-dimer and high sensitive C-reactive protein (H-CRP) levels before, 50 min of stress task (S-50m) and 60 min of recovery (R-60m). Changed ratios of granulocyte, lymphocyte, monocyte and platelet counts at S-50m and R-60m were higher in group II compared to group I. RBC count and hematocrit level in group I increased whereas those in group II decreased at S-50m. PT, APTT and ESR in the both groups were shortened at R-60m and the decreased ratios were high in group II compared to group I. H-CRP and D-dimer in the both groups were elevated at S-50m and R-60m while the increased ratios in group II were greater than those in group I. These observations imply that a combined mental activity with experimental subway noise may be a stressor which affects hematological physiology.

• Fisheries and Aquatic Sciences
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• 제18권4호
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• pp.417-420
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• 2015

We investigated the relationship between viability and IGF-1 receptor (IGF-1R) activity in D-shaped and umbo larvae of the surf clam Spisula sachalinensis after treatment with vitrification solution (VS) or freezing. In a toxicity assay, VS1, containing 5 M dimethyl sulfoxide (DMSO), was very harmful to D-shaped and umbo larvae. However, VS2, containing 5 M ethylene glycol (EG), was not harmful to either larval stage. Although VS2 had a promising toxicity test outcome, none of the larvae survived vitrification. After immersion into VSs and freezing, IGF-1R ${\beta}$-subunits were detected in all larvae; however, tyrosine phosphorylation of intracellular ${\beta}$-subunits was detected only in the control and live groups. These results suggest that activation of IGF-1R may influence surf clam larvae viability.

• 산업경영시스템학회지
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• 제20권44호
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• pp.257-261
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• 1997

Patents often serve as leading indicators of technological change. This patenting activity reflected R&D (Research & Development) of new technology. The purpose of this study is to set up a forecasting model that anticipate the number of domestic patent applications and the number of patents granted relating to R&D inputs (R&D expenditure, R&D manpower) at the level of three industrial sectors in Korea : electrical-electronic, machinery, chemical etc. In this study, forecasting models were used trend extrapolation and a set of regressions. Both Theil's inequality coefficient and MAE(Mean Absolute Error) were utilized to test the precision of predicted value. The patent data and the R&D data were based on Indicators of Industrial Technology data throught 1980 to 1996. The major results obtained in this study are as follows (1) The regression model is more useful for forecasting the trends of the number of patent applications and patents granted than the trend extrapolation method. (2) The variance of Theil's inequality is smaller in patent applications than in patent granted.

• 대한화장품학회지
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• 제36권3호
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• pp.199-205
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• 2010

기질 화합물로써 일련의 phenyl-2,2'-methylenebis(cyclohexane-1,3-dione) 유도체(1-22)들의 치환기($R_1$ 및 $R_2$)가 변화함에 따른 tyrosinase 활성저해에 대한 분자 홀로그래피적인 정량적 구조-활성관계(HQSAR) 모델을 유도하였다. 그리고 tyrosinase 저해활성에 미치는 구조상 요소들의 분석결과에 근거하여 높은 tyrosinase 저해활성을 보이는 새로운 tyrosinase 저해활성 분자를 설계하였다. 또한, 통계적으로 양호한 E-2 모델(상관성; $r_2$ = 0.929 및 예측성; $q_2$ = 0.564)을 유도하였으며 설계된 화합물, P1 ($Pred.pI_{50}$ = 5.48)는 기준물질로 사용된 kojic acid에 비하여 약 13.4배 높은 저해활성을 나타낼 것으로 예측되었다.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
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• pp.192-202
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• 2003

The wrinkles correspond to the most obvious expression of skin ageing and are manifested by changes on the organization and dermal structure. In the extracellular matrix, decreased quantities of collagens and glycosaminoglycans as well as a deterioration of the fibrillary network is noted, result in a reduction of dermal thickness. In addition, the activity of the collagenases increases in contrast to the synthesis of collagen fibers. Nor are cells spared during the aging process. We thus studied and compared the contractile capacity as well as the synthesis capacity of normal human fibroblasts and human fibroblasts obtained from biopsies of forehead wrinkles. The capacity of the fibroblasts to be adhered to the collagen network and to maintain a three-dimensional structure of dermis was studied on a model of equivalent dermis. The metabolic activity was studied by evaluating the capacities of synthesis of collagen I, main component of dermis. Human fibroblasts resulting from the forehead wrinkle contract less the gel of collagen than the normal human fibroblasts and present an activity of biosynthesis of collagen I less important than normal human fibroblasts. These results show that fibroblasts with aging present a deceleration of their metabolic activity and lose their capacity of adhesion to collagen fibers thus limiting the possibility of organizing the dermal tissue. We investigated the potential of an active ingredient able to compensate for the reduction of the metabolic activity and to restore the contractile capacity of fibroblasts obtained from forehead wrinkles. This effect was compared with a reference molecule: the vitamin C.