• Archives of Pharmacal Research
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• 제28권10호
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• pp.1105-1110
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• 2005

Novel anomeric branched carbocyclic nucleosides were synthesized from 1,3-dihydroxy acetone. 4'-Hydroxymethyl was installed by [3,3]-sigmatropic rearrangement reaction and 1'-methyl group was introduced by carbonyl addition of methylmagnesium bromide. The coupling of nucleosidic bases and desilylation afforded a series of novel nucleosides. The synthesized compounds $16{\~}19$ were evaluated for their antiviral activity against HIV-1, HSV-1, HSV-2, and EMCV. Compounds 16 and 19 exhibit toxicity non-related to any anti-HIV-1 activity.

• 한국미생물·생명공학회지
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• 제32권1호
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• pp.29-36
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• 2004

토양으로부터 CGTase를 생산하는 새로운 호열성 세균을 분리하였으며, 형태 및 생리적 특성과 16S ribosomal DNA의 염기서열을 분석한 결과 Geobacillus thermosacchalytycus 로 동정하였다. 호열성 G. thermosacchalytycus가 분비하는 CGTase를 한외여과, 소수성 Phenyl Sephadex CL-4B 클로마토그래피 , 그리고 gel filtration의 순서로 분리 정제하여 정제도 28.2배, 정제수율 12.2%, 그리고 specific activity가 4952.5 units/mg인 CGTase를 얻을 수 있었다. 정제된 CGTase의 분자량은 69,000 dalton이었고, terminal amino sequence는 Asn-Leu-Asn-Lys-Val-Asn-Phe-Thr-Ser-Asp-Val-Val-Tyr-Gln-Ile이었다. 최적 pH 및 온도는 각각 pH 6와$ 50^{\circ}C$였고, pH 6-8과 $60^{\circ}C$에서 장기간 보존할 수 있는 중성 pH의 내열성 효소임을 알 수 있었다. 내열성 CCTase의 cyclization과 coupling 반응의 특정을 검토한 결과 G. thermosacchalytycus가 생산하는 내열성 효소는 $\alpha$-type CGTase이었고, cyclization 반응보다는 coupling반응에 적합한 당전이성이 높은 효소임을 알 수 있었다. 당전이 반응에서 기질 특이성을 검토한 결과 당공여체로는 가용성 전분 그리고 당수용체로는 배당체인 stevioside에 대해 높은 기질 특이성을 보였다. 당전이 반응은 당수용체와 당공여체가 효소와 무작위로 결합하여 진행되는 random ternary complex mechanism으로 반응이 수행되었다.

• 한국안전학회지
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• 제24권2호
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• pp.83-88
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• 2009

The objective of this paper was to evaluate the effectiveness of horizontal, vertical, asymmetric and coupling multipliers for manual material handling. Lifting tasks with 5 different horizontal distances ($30{\sim}70cm$) for 6 vertical distances(ankle, knee, waist, elbow, shoulder and head height) were experimented. The muscle activity and muscle exertion level during asymmetric load handling(without trunk flexion) was experimented. Lifting tasks with and without handle tote box for three postures(straight, bending, right angle posture) were experimented. The degrading tendency did not appeared almost in $60{\sim}70cm$ interval's horizontal distance. As a result of ANOVA, MVC paid attention to horizontal and vertical distance but cross effect was insignificant(p<0.01). The change of the MVC according to the horizontal, vertical distance appeared similar from of RWL. The results of normalized MVC measurement were decreased about 16%, 24%, 34% respectively as the asymmetry angle was $30^{\circ}$, $60^{\circ}$, $90^{\circ}$. RMS EMG values of right erector spinae muscles were decreased as the work posture went to $90^{\circ}$ and those of left erector spinae muscles were increased until the asymmetry angle was $40^{\circ}$ but decreased continually over $40^{\circ}$. 7 subjects, activities of left and right latissimus dorsi muscles were maintained constantly, while for remainer, those were irregular. MVC reduced maximum 23% by type of handle. MVC was highest in straight posture, but was lowest in right angle posture. As a result of ANOVA, MVC paid attention to posture, coupling(p<0.01). To all handle types, biceps brachii activity was increased in right angle posture, but reduced in straight posture. Based on the results of this study, it is suggested that the NIOSH guideline should not be directly applied to Korean without reasonable reexamination. In addition, we need to afterward study through an age classification.

• International Journal of Oral Biology
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• 제44권1호
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• pp.1-7
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• 2019

Osteoporosis is a common disease characterized by bone mass reduction, leading to an increased risk of bone fracture, and it is caused by an imbalance of osteoblastic bone formation and osteoclastic bone resorption. Current osteoporosis drugs aim to reduce the risk of bone fracture, either by increasing osteoblastic bone formation or decreasing osteoclastic bone resorption. However, osteoblasts and osteoclasts are closely coupled, such that any reagent altering the differentiation or activity of one eventually affects the other. This tight coupling between osteoblasts and osteoclasts not only limits the therapeutic efficacy but also threatens the safety of osteoporosis drugs. This review will discuss the biological mechanisms of action of currently approved medications for osteoporosis treatment, focusing on the osteoblast-osteoclast coupling.

• 대한화학회지
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• 제36권1호
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• pp.147-156
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• 1992

${\alpha}-{\beta}-,{\gamma}$-알루미나 및 MgO를 담체로 사용하여 담지된 납산화물 촉매를 제조하였다. 담지된 납산화물 촉매상에서 메탄의 $C^{2+}$ 탄화수소로의 전환반응은 MgO 담지촉매에서 $C^{2+}$ 선택도가 최대로 얻어졌으며, ${\gamma}$-알루미나 담지 PbO 촉매에서는 $CO_2$ 선택도가 높았다. 그리고 ${\alpha}$-알루미나 담지촉매에서는 중간정도의 활성이 얻어졌으며, ${\beta}$-알루미나 담지촉매에서는 활성이 거의 나타나지 않았다. 이러한 반응특성은 촉매의 격자산소의 활성에 크게 의존하였으며, 또한 격자 산소의 활성은 담체와 산화물간의 상호작용과 담체의 성질에 영향받았다. 특히 MgO 담지 촉매에서는 X-선 회절분석에서 여타의 담체에서보다 PbO 산화물의 (002)면의 피크 세기가 (111)면의 세기에 비해 훨씬 크게 나타난 것으로 볼 때 메탄의 Oxidative Coupling 반응에서의 표면산화물-담체 상호작용(SOSI)의 한 예로 여겨졌다.

• Journal of Microbiology and Biotechnology
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• 제13권4호
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• pp.501-508
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• 2003

Artificial coupling of one enzyme with another can provide an efficient means for the production of industrially important chemicals. Xylose reductase has been recently discovered to be useful in the reductive production of xylitol. However, a limitation of its in vitro or in vivo use is the regeneration of the cofactor NAD(P)H in the enzyme activity. In the present study, an efficient process for the production of xylitol from D-xylose was established by coupling two enzymes. A NADH-dependent xylose reductase (XR) from Pichia stipitis catalyzed the reduction of xylose with a stoichiometric consumption of NADH, and the resulting cofactor $NAD^+$ was continuously re-reduced by formate dehydrogenase (FDH) for regeneration. Using simple kinetic analyses as tools for process optimization, suitable conditions for the performance and yield of the coupled reaction were established. The optimal reaction temperature and pH were determined to be about $30^{\circ}C$ and 7.0, respectively. Formate, as a substrate of FDH, affected the yield and cofactor regeneration, and was, therefore, adjusted to a concentration of 20 mM. When the total activity of FDH was about 1.8-fold higher than that of XR, the performance was better than that by any other activity ratios. As expected, there were no distinct differences in the conversion yields of reactions, when supplied with the oxidized form $NAD^+$ instead of the reduced form NADH, as a starting cofactor for regeneration. Under these conditions, a complete conversion (>99%) could be readily obtained from a small-scale batch reaction.

• Journal of Ginseng Research
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• 제9권2호
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• pp.154-162
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• 1985

We report a newassay method on the measurement of the catalase activity, whose utilzation value is considered to be remarkable in the field of plant biochemistry. We named this method as a De-Coupling method. The essence of de-coupling method is the separation between the enzyme reaction and the indicator reaction. The optimum condition of the enzyme reaction was found to be following: on addition of 1 ml of substrate (H2O2: 20mM) to the fixture of the crude extract of enzyme (volume: 0.2 ml) and the ammonium phosphate buffer (volume: 1.8 ml; 0.93 M phosphate, 1.6M NHB, 2.5 M methanol, pH 7.0). After 30, 60 and 90 seconds of the enzyme reactions are proceeded, the reactions are terminated by 25% of tai-chloro-acetate (final concentration of 5%), respectively. The precipitated materials by tai-chloro-acetate was removed by the centrifugation (2000g, 10minutes). Formaldehyde produced in the enzymatic reaction was reacted with 2ml of acetylacetone (60mM). The indicator reaction -(HANTSCH REAKT10N)- in which lutidine is formed, was proceeded for 60 minutes at $25^{\circ}C$.

• 한국환경농학회지
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• 제18권3호
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• pp.292-297
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• 1999

수중에서 유기합성화합물의 oxidative coupling을 통한 제거에 촉매제로서 식물체의 직접적인 이용 가능성을 검토하기 위하여 제지, 염료 및 전자회사 등에서 배출되고 있는 phenol성 화합물인 2,4-DCP를 이용하였다. 이 제거반응은 식물체에 포함된 산화환원효소에 의해 매개되어지는 oxidative coupling반응에 의해 유기독성화합물들간의 중합 반응으로 생성된 polymer가 침전됨으로서 야기되었다. 여러식물체들을 선별하여 이들 식물체가 가지고 있는 peroxidase의 활성을 측정한 결과 냉이에서 가장 높은 peroxidase의 활성이 관찰되었고 순무, 고구마, 배추 그리고 무 뿌리의 순이었다. Peroxidase의 활성이 비교적 높은 것으로 나타난 순무와 냉이를 이용해 다양한 실험조건하에서 2,4-DCP의 제거정도를 조사한 결과 2,4-DCP의 최대제거는 냉이의 경우 3분 이내, 순무의 경우 15분 이내로 아주 신속하게 이루어졌으며, 실험을 수행한 pH 전 범위(pH 3.0-8.0)에서 높은 제거율(90% 이상)을 유지하였다. 전자수용체로 작용하는 hydrogen peroxide를 9mM 첨가하였을 때 최대 제거율을 보였으며, 그 농도를 증가시키더라도 제거율은 더 이상 증가되지 않았다. 초기농도를 달리하여 냉이와 순무에 의한 2,4-DCP의 제거율을 조사한 결과 냉이로 매개된 2,4-DCP의 제거율은 초기농도 1,600ppm까지 90% 이상의 제거율을 나타내었으나, 순무로 매개된 2,4-DCP의 경우 초기농도 1,200ppm까지 90%이상의 제거율을 나타내다가 초기농도가 1,600ppm로 증가되었을 때 78.8%로 제거율이 감소되어 유기독성물질의 초기농도는 식물체를 이용한 유기독성물질의 제거에 약간의 영향을 미치는 것으로 나타났다.

• 한국환경농학회지
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• 제15권2호
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• pp.239-245
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• 1996

Hydrazone 결합을 지닌 화합물 중 농용으로 사용되는 것은 ferimzone, drazoxolon, metazoxolon 등으로 그 수가 매우 제한되어 있다. 본 연구에서는 hydrazone 결합 및 유사 결합구조인 formamidine, triazene 등의 toxophore로서 작용 여부를 규명하고자 하는 시도의 일환으로 일차적으로 hydrazone계 화합물 중 isoxazolone 유도체를 합성, 살균력을 검정하였다. Ethyl acetoacetate와 hydroxyl amine에서 합성된 isoxazolone에 aromatic diazonium coupling을 통하여 최종 산물을 얻었다. 합성된 16종 화합물들의 항균 활성을 Rhizoctonia solani, Colletotrichum gloeosporioides, Cladosporium cucumerinum, Pythium ultimum에 대하여 검정한 결과, 난균강에 속하는 Pythium ultimum에 강한 활성을 보였으며 이를 공시 균주로, $EC_{50}$을 계산하여 그 활성 정도를 비교하였다. p-methyl, o-fluoro, m-chloro 치환체가 강한 활성을 보였다.

• Archives of Pharmacal Research
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• 제15권2호
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• pp.130-133
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• 1992

A series of copper complexes of some amino acid derivatives of 6-methoxy 3-methyl-coumarilic acid were prepared. The infrared, visible spectra and magnetic susceptibility of these compounds were reported. All copper complexes were foundt to have antimicrobial activity against gram-positive bacteria only.