• 약학회지
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• 제49권2호
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• pp.156-161
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• 2005

Tetrahydropapaveroline (THP) at 5-15 ${\mu}$M has been found to induce L-DOPA-induced oxidative apoptosis in PC12 cells. In this study, the inhibitory effects of THP on dopamine bios ynthesis in PC12 cells and tyrosine hydroxylase (TH) activity in bovine adrenal were investigated. Treatment of PC12 cells with THP at 2.5-10 ${\mu}$M significantly decreased the intracellular dopamine content in a concentration-dependent manner (18.3% inhibition at 10 ${\mu}$M THP). In these conditions, TH activity was markedly inhibited by the treatment with THP at 2.5-10 ${\mu}$M in PC12 cells (23.4% inhibition at 10 $\mu$ M THP). In addition, THP had an inhibitory effect on bovine adrenal TH activity IC50 value, 153.9${\mu}$M). THP exhibited uncompetitive inhibition on bovine adrenal TH activity with a substrate L-tyrosine with the KI value of 0.30 mM. Treatment with L-DOPA at 20~50 ${\mu}$M increased the intracellular dopamine content in PC12 cells, and the increase in dopamine content by L-DOPA was inhibited in part when THP at non-cytotoxic (5-10 ${\mu}$M) or cytotoxic (15${\mu}$M) concentrations was associated with L-DOPA (20 and 50 ${\mu}$M) for 24 h incubation. These results suggest that THP at 5-10${\mu}$M decreases the basal dopamine content and reduces the increased dopamine content induced by L-DOPA in part by the inhibition of TH activity, and that THP at 15${\mu}$M also decreases dopamine content by oxidative stress in PC12 cells.

• Journal of Microbiology and Biotechnology
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• 제9권6호
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• pp.798-803
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• 1999

Prolyl endopeptidase [PEP; EC 3.4.21.26], a serine protease which is known to cleave peptide bonds on the carboxy side of a proline residue, plays an important role in the degradation of proline-containing neuropeptides that have been suggested to participate in learning and memory processes. An abnormal increase in the level of PEP, which can lead to generation of $A{\beta}$, is also suggested to be involved in Alzheimer's type senile dementia. In the course of screening PEP inhibitors from Basidiomycetes, the mushroom Polyozellus multiplex exhibited a high inhibitory activity against PEP. Two active compounds were isolated from the ethyl acetate soluble fraction by consecutive purification, using silica gel, Sephadex LH-20, and Lobar RP-18 chromatography. The chemical structures of these compounds were identified as thelephoric acid and 12-acety1-2,3,7,8-tetrahydroxy-[12H]-12-hydroxymethylbenzobis[I.2b,3.4b'] benzofuran-11-one (kynapcin-9) by spectral data including UV, IR, MS, HR-MS, $^1H-,{\;}^{13}C-$, and 2D-NMR. The $IC_{50}$ values of the thelephoric acid and kynapcin-9 were 0.157 ppm (446nM) and 0.087 ppm (212nM) and their inhibitor constants ($K_i$) were 0.73ppm ($2.09{\;}\mu\textrm{m}$) and 0.060 ppm (146 nM), respectively. Furthermore, they were non-competitive with a substrate in Dixon plots.

• 한국막학회:학술대회논문집
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• 한국막학회 1998년도 추계 총회 및 학술발표회
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• pp.15-18
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• 1998

Membrane reactors are systems which combine a chemical reactor with a membrane separation process allowing to carry out simultaneously conversion and product separation. The catalyst can be immobilized on the membrane or simply compartmentalized in a reaction space by the membrane. Membrane reactors are today investigated to produce optically pure isomers and/or resolve racemic mixture of enantiomers. The interest towards these systems is due to the increasing demand of enantiomerically pure compounds to be used in the pharmaceutical, food, and agrochemical industries. In fact, enantiomers can have different biological activities, which often influence the efficacy or toxicity of the compound. On the basis of current literature there are basically two schemes on the use of membrane technology to produce enantiomers. In one case, the membrane itseft is intrinsically enantioselective: the membrane is the chiral system which selectively separates the wanted isomer on the basis of its conformation. In the other, a kinetic resolution using an enantiospecific biocatalyst is combined with a membrane separation process; the membrane separates the product from the substrate on the basis of their relative chemical properties (i.e. solubility). This kind of configuration is widely used to carry out kinetic resolutions of low water soluble substrams in biphasic membrane reactors [Giomo, 1995, 1997; Lopez, 1997]. These are systems where enzyme-loaded membranes promote reactions between two separate phases thanks to the properties of enzymes, such as lipases, to catalyse reactions at the org ic/aqueous interface; the two phases are maintained in contact and separated at the membrane level by operating at appropriate transmembrane pressure. A schematic representation of biphasic membrane reactor is shown in figure 1, while an example of enantiospecific reaction and product separation carried out with these systems is reported in figure 2.

• Archives of Pharmacal Research
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• 제28권12호
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• pp.1328-1332
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• 2005

In the course of screening for anti-dementia agents from natural products, two $\beta$-secretase (BACE1) inhibitors were isolated from the husk of pomegranate (Punica granatum) by activity-guided purification. They were identified as ellagic acid and punicalagin with $IC_{50}$ values of 3.9 $\times$$10^{-6}$ and 4.1$\times$$10^{-7}$ M and Ki values of 2.4$\times$$10^{-5}$and 5.9$\times$$10^{-7}$ M, respectively. The compounds were non-competitive inhibitors with a substrate in the Dixon plot. Ellagic acid and punicalagin were less inhibitory to $\alpha$-secretase (TACE) and other serine proteases such as chymotrypsin, trypsin, and elastase, thus indicating that they were relatively specific inhibitors of BACE1.

• 센서학회지
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• 제30권5호
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• pp.320-325
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• 2021

Biochemical oxygen demand (BOD) and chemical oxygen demand (COD) methods are conventional analytical methods to analyze water quality. Both of these methods are technically indirect measurement methods, require complicated preconditions, and are time-consuming. On the other hand, the total organic carbon (TOC) method is a direct and fast measurement method which is more intuitive and accurate than the BOD and COD methods. However, general TOC analysis methods involve complicated processes and high power consumption owing to the process of phase transition from liquid to gas by a high-temperature heater. Furthermore, periodic consumables are also required for the removal of inorganic carbon (IC). Titanium dioxide (TiO₂) is one of the most suitable photocatalysts for simple processes. Its usage involves low power consumption because it only reacts with the organic carbon (OC) without the requirement of any other reagents and extra processes. We investigated a TiO₂ photocatalyst-based TOC analysis for simple and affordable products. TiO₂-coated fiber substrate maintained under carbon included water was exposed to ultraviolet (UV) radiation of wavelength 365 nm. This method is suitable for the real-time monitoring of water pollution because of its fast reaction time. Its linear property is also sufficient to match the real value.

• 한국동물학회지
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• 제39권1호
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• pp.36-46
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• 1996

붉은 지렁이(Lumbricus rubellus)로부터 체내에 존재하는 phenoloxidase (EPO)를 ammonium sulfate. Blue-2, Phenyl-, Q-sepharose chromatography등을 이용하여 정제하였다. 이 효소는 SDS-PAGE상에서 59 kDa의 분자량을 갖는 단일 단백질로 나타났으며 nondenatudng-PAGE를 이용하여 DL-dopa를 기질로 in situ 염색 결과, 210 kDa 보다 다소 큰 단일 band가 dopachrome 침착에 의해 형성되었다. 이는 곧 이 효소가 자연상태에서 복합체의 형태로 존재하고 있음을 의미한다. 또한 이 효소는 monophenolase 활성도, 즉 tyrosine을 dopa로 전환시키는 활성도도 갖고 있음을 470nm에서 dopachrome축적을 관찰함으로써 확인할 수 있었다. Phenyithiourea(PUT), 1, 10-phenanthroline, EDTA, EGTA등을 사용한 효소억제 실험 결과, PTU만이 65 $\mu$M의 IC 0.5로 효소 활성도를 효과적으로 억제시켰다. 이는 EPO의 촉매기작에서 구리가 매우 중요한 역할을 하고 있음을 의미한다. 이 효소는 L-dopa를 기질로 사용하였을 때 35$^{\circ}C$와 pH8.0에서 최적의 활성도를 나타내었다. EPO의 L-dopa에 대한 Km은 pH6.5와 8.0에서 각각 1.86 mM과 13.8 mM로 나타났다. 또한, pH 8.0에서 Vmax는 pH 6.5에서 보다 약 6.6배 높은 반면, 각 조건에서 촉매 효율성은 거의 차이가 없음 [(kat/Km)pH8.0/(kcat/Km)pH6.5 = O.92]을 알 수 있었다. 따라서, 이 사실은 EPO 촉매기작에 미치는 pH의 효과가 효소 자체에보다는 기질 또는 효소-기질 복합체 형성과정에 영향을 줌을 의미한다. 이와 같은 사실을 종합해 보면, L. rubellus에 존재하는 phenoloxidase는 oligomeric form을 가지며 활성화 되기 위한 제한적 단백질 가수분해를 필요로 하지 않는다. 따라서, prophenoloxidase activating system의 존재 가능성을 완전히 배재할 수는 없으나 지렁이 체내의 PO는 최소한 부분적으로나마 latent from으로 존재함을 확인할 수 있었다. 이는 외부 침입시 host를 보호하기 위한 방법으로 EPO를 latent from으로 유지 시킬 수 있는 또는 활성화 시킬 수 있는 조절기작의 존재를 예측하게 한다.

• 한국환경생태학회지
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• 제30권6호
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• pp.986-995
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• 2016

본 연구에서는 금강 대권역에 서식하는 멸종위기 담수어류의 분포, 이들 종에 대한 화학적 지표와의 관계 및 물리적 서식지 특성을 분석하였다. 금강 대권역에 서식하는 멸종위기종의 개체수는 감돌고기(Pseudopungtungia nigra), 꾸구리(Gobiobotia macrocephala), 돌상어(Gobiobotia brevibarba), 퉁사리(Liobagrus obesus), 미호종개(Iksookimia choii) 순으로 나타났다. 멸종위기 야생생물 I급 어류인 감돌고기는 금강 대권역 내 18개 하천에서 가장 광범위하게 분포하여, 향후 감돌고기의 I급 어종 선정에 대한 재평가가 필요한 것으로 사료되었다. 또한 초강 중권역에서 멸종위기어종이 총 4종 384개체가 채집되어 종수 및 개체수가 풍부하였다. 멸종위기어종 서식지에서 이화학적 수질내성도 분석에 따르면, 생물학적 산소요구량(BOD) 및 총인(TP)은 각각 매우 좋음(Ia), 좋음(Ib)으로 평가 되었으며. 암모니아성 질소($NH_{4+}$), 총질소(TN), 인산염 인($PO_{4^-}P$) 등의 수질 항목도 멸종위기종 비 출현지점에 비해 훨씬 양호한 것으로 분석되었다. 한편, 미호종개의 경우 수질의 내성범위가 다른 어종에 비해서 광범위하게 나타나, 화학적 수질특성이 크게 악화되지 않을 경우 수질특성 보다는 미소서식처의 하상구조, 수리수문학적 특성 등의 물리적 서식지 조건이 더 중요한 것으로 나타났다. 또한, 멸종위기종의 분포는 1~3차의 소형하천보다 4~6차 대형하천에서 높게 나타났으며, 주로하천의 상류 및 중상류에 작은 무리를 이루며 서식하는 것으로 나타났다. 멸종위기종 미출현지역과 출현지역의 생태건강도 다변수 평가모델 값은 각각 21.6 "보통상태(Fair)" 및 30.5 "양호상태(Good)"로 나타나 뚜렷한 차이를 보여, 생태건강도가 잘 유지된 곳에서 멸종위기종이 잘 서식하는 것으로 나타났다. 본 연구를 요약해 보면, 감돌고기와 같은 어종의 멸종위기종 선정에 대한 재평가가 향후 필요하며, 수질오염 및 서식지교란이 가속화되고 있어 멸종위기종에 대한 체계적인 보호 및 관리가 필요하다.

• 대한화장품학회지
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• 제30권3호
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• pp.393-397
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• 2004

L-Carnitine $({\beta}-hydroxy-\gamma-trimethyl-ammoniumbutyric{\;}acid)$은 분자량이 적은 수용성 분자로서 세포 내 지방 대사에서 중요한 역할을 수행한다. 지방산의 운반 분자인 아실-코에이(acyl-CoA)가 미토콘드리아의 세포막을 투과하지 못하기 때문에 지방산은 CoA로부터 카르니틴으로 운반되어 미토콘드리아에서 작용한다. 노화와 연관된 L-carnitine의 기능을 확인하기 위하여 MMP inhibition assay와 자외선 조사에 의해 유도된 MMP 발현에 대한 영향을 확인하였다. MMP inhibition assay는 콜라겐을 이용한 형광분석법을 실시하였고 자외선 조사에 의해 유도된 MMP 발현양은 ELISA로 정량하였으며 그 활성은 젤라틴 기질 zymography로 확인하였고 MMP mRNA 발현양은 RT-PCR ELISA로 확인하였다. 또한, 사람을 이용한 임상 실험을 통하여 주름 개선 효과를 평가하였다. L-carnitine은 농도 의존적으로 MMP 저해 활성을 나타났으며 $IC_{50}$값은 2.45 mM이었으며 자외선 조사에 의해 발현된 MMP 활성을 강하게 저해하였다. 자외선 조사에 의해 발현되는 MMP에 대해 단백질의 양적인 변화는 $40\%$ 정도 감소되었으며 L-carnitine 처리에 의해 농도 의존적으로 MMP mRNA의 발현양은 감소되었다. 이러한 실험결과를 통하여 L-carnitine은 MMP 효소의 저해능 뿐만 아니라 자외선 조사에 의해 유도되는 MMP 단백질 발현과 mRNA 유전자 수준에서의 조절이 가능함을 확인하였다. 사람을 이용한 임상 실험에서는 $1\%$ 카르니틴을 함유하는 화장품을 약 3개월간 사용 후에는 유의적으로 주름 개선 효과를 확인하였다. 결론적으로 L-Carnitine은 광노화에 관여하는 MMP 활성과 발현 조절 메커니즘을 통하여 광손상에 대응하는 항노화 소재로서의 화장품에 매우 효과적이었음을 확인하였다.

• 한국전기전자재료학회:학술대회논문집
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• 한국전기전자재료학회 2009년도 춘계학술대회 논문집
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• pp.3-3
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• 2009

In order to investigate the possibility of using mixed rare earth $(Nd_{1/3}Eu_{1/3}Gd_{1/3})Ba_2Cu_3O_{7-x}$ (NEG123) as the superconducting layer of the HTS coated conductor, the NEG123 thin film was deposited epitaxialy on LAO(100) single crystal and IBAD_YSZ metal templates by pulsed laser deposition. Systematic studies were carried out to investigate the influences of deposition parameters of PLD on the micro structure, texture and superconducting properties of NEG-123 coated conductor. Deposition at oxygen partial pressure of 600 mTorr was needed to routinely obtain high quality NEG123 films with $J_c$'s (77K) over 2 MA/$cm^2$ and Tc's over 90K (${\Delta}T{\sim}2\;K$). We verified from magnetization study that the NEG123 has an improved in-field Jc as the field increases at temperatures between 10 K and 77 K compared with Gd123. The $J_c$ (77K, self field) and the value of onset $T_c$ of NEG123 thin film on LAO substrate was $4.0MA/cm^2$ and 92K, respectively. This is the first report, to the best of our knowledge, of coated conductors with NEG123 film as the superconducting layer which have Ic and Jc over 40 A/cm-width and 1.6 MA/$cm^2$ at 77K, self field. This study shows the possibility of using NEG123 film as the superconducting layer of the HTS coated conductor which can be used in high magnetic field power electric devices.

• Archives of Pharmacal Research
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• 제21권1호
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• pp.6-11
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• 1998

The activities of two types of antiulcer agents against 9 strains of Helicobacter pylori (H. pylori) were determined by the agar dilution method. The antiulcer agents were YJA20379, a newly synthesized proton pump inhibitor developed by Yung-jin Pharmaceutical company, and omeprazole. Both compounds were found to have significant activities against this organism. The MIC values of YJA20379 and omeprazole were 11.7 and $31.25{\mu.g/ml}$ respectively. In addition, the inhibitory potency of both compounds was investigated on H. pylori urease which is believed to be an important colonization and virulence factor in the pathogenesis of gastritis and peptic ulcers. These compounds dose-dependently inhibited urease extracted with distilled water and their $IC_50$ values were $16.4{\times}10^{-5} M and 14.3{\times}10^{-5}M,$ respectively. In addition, a pH-dependent study to determine whether inhibitory potency would be activated by acid condition was performed. It was found that unlike omeprazole, YJA20379 was not affected by acid condition. To determine the inhibition pattern and optimal concentration of substrate, kinetics were evaluated at various pH levels (pH 5.0, 7.0, and 8.5). The data show that YJA20379 noncompetitively inhibited H. pylori urease and $K_M/K_i$values were 0.96 $mM/60{\mu}M (pH 5.0), 0.56 mM/141.5 {\mu}M (pH 7.0)$, and $1.94mM/34{\mu}M (pH 8.5)$, respectively. Based on data obtained, it is concluded that YJA20379 is a significant inhibitor of H. pylori growth and urease and therefore, taking these results into consideration, YJA20379 might be a beneficial therapy for gastritis and peptic ulcers induced by H. pylori.