• Bulletin of the Korean Chemical Society
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• 제32권1호
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• pp.251-262
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• 2011

Human ether-a-go-go related gene (hERG) potassium channel blockade, an undesirable side effect which might cause sudden cardiac death, is one of the major concerns facing the pharmaceutical industry. The purpose of this study is to develop an in silico QSAR model which uncovers the structural parameters of T-type calcium channel blockers to reduce hERG blockade. Comparative molecular similarity indices analysis (CoMSIA) was conducted on a series of piperazine and benzimidazole derivatives bearing methyl 5-(ethyl(methyl)amino)-2-isopropyl-2-phenylpentanoate moieties, which was synthesized by our group. Three different alignment methods were applied to obtain a reliable model: ligand based alignment, pharmacophore based alignment, and receptor guided alignment. The CoMSIA model with receptor guided alignment yielded the best results : $r^2$ = 0.955, $q^2$ = 0.781, $r^2_{pred}$ = 0.758. The generated CoMSIA contour maps using electrostatic, hydrophobic, H-bond donor, and acceptor fields explain well the structural requirements for hERG nonblockers and also correlate with the lipophilic potential map of the hERG channel pore.

• Bulletin of the Korean Chemical Society
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• 제33권11호
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• pp.3767-3771
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• 2012

In this study, we investigate the potential use of $TiO_2@SiO_2$ and $ZnO@SiO_2$ core/shell nanoparticles (NPs) as effective UV shielding agent. In the typical synthesis, $SiO_2$ was coated over different types of $TiO_2$ (anatase and rutile) and ZnO by sol-gel method. The synthesized $TiO_2@SiO_2$ and $ZnO@SiO_2$ NPs were characterized by UV-Vis, XRD, SEM and TEM. The UV-vis absorbance and transmittance spectra of core@shell NPs showed an efficient blocking effect in the UV region and more than 90% transmittance in the visible region. XRD and SAED studies confirmed the formation of amorphous $SiO_2$ coated over the $TiO_2$ and ZnO NPs. The FESEM and TEM images shows that coating of $SiO_2$ over the surface of anatase, rutile $TiO_2$ and ZnO NPs resulted in the increase in particle size by ~30 nm. In order to study the UV light shielding capability of the samples, photocatalytic degradation of methylene blue dye on $TiO_2@SiO_2$ and $ZnO@SiO_2$ NPs was performed. Photocatalytic activity for both types of $TiO_2$ NPs was partially suppressed. In comparison, the photocatalytic activity of ZnO almost vanished after the $SiO_2$ coating.

• 한국해양공학회지
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• 제21권1호
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• pp.7-17
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• 2007

Based on the Boussinesq wave model, the wave distribution in the Chagui-Do sea area in Jeju was simulated by applying the directional irregular waves at an incident boundary. The time and spatial variations of monthly mean wave height and period were investigated, which aims to provide basic information on optimal sites for wave power generation. The grid size and time interval of the Boussinesq wave model were validated by examining wave distributions around a surface piercing wall, fixed at sea bottom with a constant slope. Except for the summer season, the significant wave height is dominated by wind waves and appears to be relatively high at the north sea of Chagui-Do, which is open to the ocean, while it is remarkably reduced at the rear sea of Chagui-Do because of its blocking effect on incident waves. In the summer, the significant wave height is higher at the south sea, and it is dominated by the swell waves, which is contributed by the strong south-west wind. The magnitude of significant wave height is the largest in the winter and the lowest in the spring. Annual average of the significant wave height is distinctively high at the west sea close to the Chagui-Do coast, due to a steep variation of water depth and corresponding wave focusing effect. The seasonal and spatial distribution of the wave period around Chagui-Do sea reveals very similar characteristics to the significant wave height. It is suggested that the west sea close to the Chagui-Do coast is the mast promising site for wave power generation.

• 한국정보통신학회:학술대회논문집
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• 한국정보통신학회 2017년도 춘계학술대회
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• pp.499-502
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• 2017

전력의 효율적인 사용과 전기 안전(electrical Safety)을 위한 전류 측정에 대한 요구가 늘고 있다. 이에 전류 센서가 사용되며, 특히 홀 효과(hall effect)를 이용하여 회로를 차단하지 않고 전류를 측정할 수 있는 비접촉식 전류 센서가 많이 사용되고 있다. 하지만 이러한 전류 센서에는 다양한 잡음 등의 유입으로 인하여 전류 센서의 정확한 측정을 방해한다. 본 논문은 기존의 전류 센서에 저역통과 FIR필터를 사용하여, 보다 잡음에 강인한 전류 센서를 제안한다. 전류 센서의 출력단에 일정 주파수 이상의 영역을 차단하는 FIR필터를 설계하여 외부 잡음 등을 제거하였으며, 그 결과 기존 전류센서 보다 정확하고 정밀한 측정을 할 수 있었다.

• Elastomers and Composites
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• 제44권3호
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• pp.290-298
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• 2009

본 논문에서 Fe-활성탄소 섬유(ACF)/$TiO_2$ 복합체 광촉매를 졸-겔 방법에 의하여 제조하였다. 합성된 광촉매는 UV조사하에서 MB용액의 광분해에 사용되었다. BET 데이터는 Fe와 Ti의 여러 가지 농도를 가지고 처리된 ACF의 표면에서 흡착 특성을 보여준다. SEM 사진에서 보여지는 것처럼, 철 혼합물과 $TiO_2$는 ACF 표면에 활착되어 있음을 나타내었다. X선 분말 회절법으로부터 얻어진 결과는 복합체로부터 FeO+$TiO_2$, Anatase 및 Rutile 구조의 결정상을 나타내었다. 원소분석을 위한 EDX spectra는 Fe와 함께 C, O, Ti의 peak들이 존재함을 나타내었다. MB 분해에 대한 활성은 $TiO_2$의 광분해와 Fe의 photo-Fenton 효과로 인해 전자/hole쌍 반응으로부터 파생된 -OH 라디칼들에 의한 것으로 여겨진다.

• IMMUNE NETWORK
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• 제14권6호
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• pp.296-306
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• 2014

There is growing evidence that crosstalk between mantle cell lymphoma (MCL) cells and stromal microenvironments, such as bone marrow and secondary lymphoid tissues, promotes tumor progression by enhancing survival and growth as well as drug resistance of MCL cells. Recent advances in the understanding of lymphoma microenvironment have led to the identification of crucial factors involved in the crosstalk and subsequent generation of their targeted agents. In the present study, we evaluated the combinatory effect of blocking antibodies (Ab) targeting CXCR4 and VLA-4, both of which were known to play significant roles in the induction of environment-mediated drug resistance (EMDR) in MCL cell line, Jeko-1. Simultaneous treatment with anti-CXCR4 and anti-VLA-4 Ab not only reduced the migration of Jeko-1 cells into the protective stromal cells, but also enhanced sensitivity of Jeko-1 to a chemotherapeutic agent to a greater degree than with either Ab alone. These combinatorial effects were associated with decreased phosphorylation of ERK1/2, AKT and NF-${\kappa}B$. Importantly, drug resistance could not be overcome once the adhesion of Jeko-1 to the stromal occurred despite the combined use of Abs, suggesting that the efforts to mitigate migration of MCLs should be attempted as much as possible. Our results provide a basis for a future development of therapeutic strategies targeting both CXCR4 and VLA-4, such as Ab combinations or bispecific antibodies, to improve treatment outcomes of MCL with grave prognosis.

• Bulletin of the Korean Chemical Society
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• 제34권2호
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• pp.482-488
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• 2013

Two piperazine-containing 3,4-dihyroquinazolines (BK10007S/8S) have been synthesized, based on our previous work on the synthesis and antitumoral activity of 3,4-dihyroquinazolines. After evaluating them for T-type calcium channel blocking effect and in vitro anti-cancer effect, they were profiled for acute and repeat dose toxicity (40 mg/kg, 2 weeks) to BALB/c mice. BK10007S/8S were further in vivo evaluated against human pancreatic MIA PaCa-2 carcinoma in $BALB/c^{nu/nu}$ nude mice, which exhibited 54 and 61% tumor growth inhibition through 57-day oral administration of 2 mg/kg of body weight, respectively.

• Mycobiology
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• 제43권3호
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• pp.319-326
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• 2015

Fomes fomentarius is a fungus of the Polyporaceae family and is used in traditional oriental therapies. Although the anti-inflammatory activities of this species have been previously reported, the identity of the bioactive compounds responsible for this activity remains unknown. Here, we investigated whether methyl 9-oxo-(10E,12E)-octadecadienoate (FF-8) purified from F. fomentarius exerts anti-inflammatory activity in murine macrophages stimulated with lipopolysaccharide (LPS). FF-8 suppressed secretion of nitric oxide (NO) and prostaglandin $E_2$ through downregulation of inducible NO synthase and cyclooxygenase-2 expression induced by LPS. In addition, pretreatment of cells with FF-8 led to a reduction in levels of secreted inflammatory cytokines such as tumor necrosis factor-${\alpha}$ and interleukin-6 in macrophages stimulated with LPS. Conversely, FF-8 did not affect nuclear factor ${\kappa}B$, p38, c-Jun NH2-terminal kinase, and extracellular signal-regulated kinase pathways. Instead, FF-8 specifically interfered with signal transducer and activator of transcription 3 (STAT3) phosphorylation induced by LPS. Collectively, this study demonstrated that FF-8 purified from F. fomentarius suppresses inflammatory responses in macrophages stimulated with LPS by inhibiting STAT3 activation. Further studies will be required to elucidate the anti-inflammatory effect of FF-8 in vivo.

• 대한화장품학회지
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• 제43권4호
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• pp.321-327
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• 2017

본 연구는 기존의 인공적으로 합성된 유기 자외선 차단제를 대체하는 안정적인 식물유래 천연 자외선 차단제(BHC-S)를 개발하기 위하여 수행하였다. 땅콩싹추출물, 병출추출물 및 곰피추출물로 구성된 천연 자외선 차단제(BHC-S)는 합성 자외선 차단제인 Parsol MCX-XR (OMC)와 동등 수준의 자외선 차단 효과를 가질뿐만 아니라, 피부에 대한 안전성을 가지며, 주름개선 등 다기능성 효과를 가지는 것으로 확인되었다. 이로써, 자외선 차단 및 항노화을 위한 천연 화장품 원료로서의 이용이 가능할 것으로 판단된다.

• 약학회지
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• 제49권2호
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• pp.140-146
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• 2005

Candida albicans, a polymorphic fungus, causes systemic and local infections. Recent reports show that the fungus is a main etiological agent for the arthritis. For trea tment, antifungal drugs and/or rheumatoid drugs are used, but resistance and side effects limit application of the drugs. In search of new sources for treatment of the fungal arthritis, we choose Egb 761 (extract of Ginkgo leaves 761), one of the most popular over-the-counter herbal medicines. The Egb 761 contains two major ingredients such as terpene and flavonoid. In the present study, we examined if the terpene portion of Egb 761 had anti-inflammatory activity against C.albicans-caused arthritis. The terpene was extracted with combination of methanol and water from the Egb 761, followed by gel-permeation chromatography. Presence of terpene was determined by the Salkowski colorimetric method and HPLC analysis. For an animal model of inflammation induction, mice were given an emulsion form of C.albicans cell wall mixed with Complete Freund's Adjuvant (CFA) by footpad-injection. Results showed that intraperitoneal administration of the water-soluble portion that contained terpene and flavonoid reduced the inflammation. Whereas the terpene had anti-inflammatory activity, flavonoid portion had no such activity, For determination of possible mechanism of the activity, the terpene seemed to be suppression of nitric oxide (NO) production from LPS-treated macrophages. Taken together the Ginkgo terpene may have anti-inflammatory effect against C.albicans-caused arthritis, possibly by blocking NO production.