• Archives of Pharmacal Research
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• 제22권5호
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• pp.491-495
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• 1999

In order to examine the effects of N-substituted alkyl group on the anticonvulsant activities of N-Cbz-$\alpha$-aminoglutarimides as novel anticonvulsants with broad spectrum, a series of (R) or (S) N-Cbz-$\alpha$-amino-N-alkylglutarimides (1 and 2) were prepared from the corresponding (R) or (S) N-Cbz-glutamic acid and evaluated for the anticonvulsant activities in the maximal electroshock seizure (MES) test and pentylenetetrazol induced seizure(PTZ) test, including the neurotoxicity. The most potent compound in the MES test was (S) N-Cbz-$\alpha$-amino-N-methylglutarimide($ED_{50}$=36.3 mg/kg, PI=1.7). This compound was also most potent in the PTZ test ($ED_{50}$=12.5 mg/kg, PI=5.0). The order of anticonvulsant activities against the MES test as evaluated form $ED_{50}$ values for (R) series was N-methyl > N-H > N-ethyl > N-allyl ; for the (S) series N-methyl > N-H > N-ethyl > N-alkyl > N-isobutyl compound. Against the PTZ tests, the order of anticonvulsant activities showed similar pattern ; for the (R) series, N-methyl > N-H > N-ethyl > N-allyl ; for the (S) series N-methyl > N-H > N-ethyl > N-allyl > N-isobutyl compound. From the above results, N-substituted alkyl groups were though to play an important role for the anticonvulsant activities of N-Cbz-$\alpha$-amino-N-alkylgutarimides.

• 한국의학물리학회지:의학물리
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• 제32권3호
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• pp.59-69
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• 2021

Purpose: The relationship between computed tomography (CT) number and electron density (ED) has been investigated in previous studies. However, the role of these measures for guiding cancer treatment remains unclear. Methods: The CT number was plotted against ED for different imaging protocols. The CT number was imported into ED tables for the Pinnacle treatment planning system (TPS) and was used to determine the effect on dose calculations. Conversion tables for radiation dose calculations were generated and subsequently monitored using a dosimeter to determine the effect of different CT scanning protocols and treatment sites. These tables were used to retrospectively recalculate the radiation therapy plans for 41 patients after an incorrect scanning protocol was inadvertently used. The gamma index was further used to assess the dose distribution, percentage dose difference (DD), and distance-to-agreement (DTA). Results: For densities <1.1 g/cm³, the standard deviation of the CT number was ±0.6% and the greatest variation was noted for brain protocol conditions. For densities >1.1 g/cm³, the standard deviation of the CT number was ±21.2% and the greatest variation occurred for the tube voltage and head and neck (H&N) protocol conditions. These findings suggest that the factors most affecting the CT number are the tube voltage and treatment site (brain and H&N). Gamma index analyses for the 41 retrospective clinical cases, as well as brain metastases and H&N tumors, showed gamma passing rates >90% and <90% for the passing criterion of 2%/2 and 1%/1 mm, respectively. Conclusions: The CT protocol should be carefully decided for TPS. The correct protocol should be used for the corresponding TPS based on the treatment site because this especially affects the dose distribution for brain metastases and H&N tumor recognition. Such steps could help reduce systematic errors.

• Membrane and Water Treatment
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• 제14권1호
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• pp.47-54
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• 2023

In this study, high concentrations of cadmium-containing wastewater were treated by electrodialysis (ED) with a channel stack. The limiting current density (LCD), cadmium removal efficiency, and current efficiency were investigated under each experimental condition according to the Reynolds number (Re), membrane area, and pH. With the increase in the film area to 111, 333, 555, and 777 cm² at Re (109.1), LCDs decreased to 408.11, 44.45, 35.32, and 13.64 A/m², respectively. The highest cadmium removal efficiency (99.6%) and current efficiency were obtained for the membrane area of 111 and 777 cm², respectively. Under changing Re in the pH range of 1 to 4, Re and LCD were proportional under the same pH condition, and pH and LCD tended to be inversely proportional under the same Re condition. Cadmium removal rate was the best at the pH range 3 - 4. It has been found that ED with channeled stacks can be successfully applied to treat wastewater containing high concentrations of cadmium.

• Tuberculosis and Respiratory Diseases
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• 제40권3호
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• pp.236-249
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• 1993

연구배경 : 정상 폐상피세포에서는 항상 생성되고 있는 활성산소(oxygen radical)에 의한 유해작용에 노출되어 있고, 이들 유해 산소들은 폐기종과 같은 폐질환의 원인 기전으로 생각되고 있다. 본 연구에서는 이 방법을 이용하여 만든 폐상피세포 단일막에서 전기생리학적인 관점에서 물질의 이동지표인 short-circuit current(Isc)와 조직저항(R)에 대한 활성산소의 하나인 $H_2O_2$(hydrogen peroxide)가 어떤 영향을 미치는지를 연구함으로서 세포생리학적 기전을 구명하고자 한다. 방법 : Tissue culture-treated polycarbonant membrane filter 에서 배양시킨 쥐 제 2 형 폐상피세포 배양 단일막에서 $H_2O_2$의 능동적 이온 이동 (Isc) 과 수동적 용질이동에 대한 조직저항(R)에 미치는 효과를 관찰하였다. 배양 제 3 일과 제 4 일째 단일막을 수정된 Ussing chamber에 설치하고 막 양측에 HEPES-buffered Ringer 용액으로 incubation 하였다. 외부에서 0~100 mM 농도의 $H_2O_2$를 apical 또는 basolateral side에 작용시켜 Isc와 R의 변화를 관찰하였다. 폐상피세포 장벽이 외부의 $H_2O_2$에 대하여 방어작용을 가지는 세포내 catalase 활성도를 측정하고, catalase 억제제인 aminotriazol(ATAZ) 20 mM의 효과도 함께 관찰하였다. 결과 : 이 단일막은 형태학적으로 보아서 in vivo 에서의 포유류 제 1 형 폐상피세포 장벽의 특성을 나타내고 세포들 사이는 tight junction을 이루며(조직저항 R: 2,000 ohm-$cm^2$ 이상) sodium ion의 능동적 이동 (Isc: 5 ${\mu}A/cm^2$)을 보였다. $H_2O_2$는 dose-dependent 양식으로 Isc와 R 모두 감소시켰다. Apical side에 작용하는 $H_2O_2$에 있어서는 60분에 50% 억제하는 농도인 $ED_{50}$는 Isc와 R은 약 4mM 이었으나 basolateral side의 경우는 약 0.04mM 로서 그 작용 강도는 apical에 비하여 약 100배 정도 더 컸다. ATAZ 존재시 apical side의 $ED_{50}$는 0.4mM로 감소하였으나 basolateral side의 경우 변화가 없었다. $H_2O_2$의 제거율은 apical 또는 basolateral side 어느 쪽에 존재하든 같았으며, 세포내 catalase 활성도는세포배양기간이 길어짐에 따라 증가함을 보였다. 결론 : 이상의 실험결과는 basolateral side에 작용하는 $H_2O_2$는 세포내 막구성성분 중 basolateral 측에 존재하는 곳에(예, $Na^+,\;K^+$-APTase) 직접 장애를 미칠 것으로 생각된다. 한편 apical side에 작용하는 $H_2O_2$는 막성분에 도달하기 전에 세포내에 존재하는 catalase에 의하여 대부분 그 작용을 잃게 된다. 결론적으로 Isc와 R로 측정된 폐상피세포 장벽의 특성은 $H_2O_2$에 의하여 손상을 받고 apical side 보다는 basolateral side 측정이 더 손상을 잘 받게 된다.

• Journal of Pharmaceutical Investigation
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• 제25권1호
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• pp.9-17
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• 1995

To stabilize omeprazole(OMP), ethylenediamine(ED) complex of omeprazole(OMPED) was prepared by reaction between OMP and ED in methanol, and the complex formation was confirmed by the instrumental analysis, i.e., IR, DSC, EA, NMR, MS and XRD. The rates of decomposition of OMP and OMPED in aqueous solution and the shelf lives at standard temperature were measured by accelerated stability analysis. The results are summarized as follows; The mole ratio of OMP and ED in OMPED complex is 1:1, the energy of formation within OMPED might be combined between polar imidazole group of OMP with induced a dipole amine group in the readily polarizable ED molecule. At standard temperature the degradation rate constant of OMP in aqueous solution is $2.540{\times}10^{-2}\;hr^{-1}$ and the shelf life is 4.15 hrs, and in the case of OMPED the degradation rate constant is $7.986{\times}10^{-4}\;hr^{-1}$ and the shelf life is 131.96 hrs. So, the OMPED has about 31 times longer shelf life than OMP. The activation energy of OMP and OMPED are 5.23 and 18.55 kcal $mole^{-1}$ respectively. The stability of OMP is dependent chiefly on pH in the solutions and it decomposes readily in acidic medium by hydrogen ion catalized reaction but becomes stable beyond pH 9.0. In case of the ED-complex, OMPED is stable in neutral as well as in dilute acidic solutions even in pH 6, OMPED is very stable to light(UV), that is, the rate constant and shelf life of OMP are $k=1.0188{\times}10^{-2}\;day^{-1}$, $T_{90%}=4.5 \;days$, on the other hand, the those of OMPED are $k=7.138{\times}10^{-4}\;day^{-1}$, $T_{90%}=64.1\;days$, respectively. From the above results, it is thought that new dosage forms could be developed by using the OMPED as a potential OMP complex.

• Journal of Pharmaceutical Investigation
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• 제39권6호
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• pp.393-400
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• 2009

PHEA (hydroxyethyl-aspartamide)-mPEG (methoy-polyethyleneglycol)-$C_{16}$ (hexadecylamine)-ED (ethylenediamine) was prepared as a drug delivery carrier. The structure and molecular weight of polymers were characterized by $^1H$-NMR and gel permeation chromatography. Micelle size and shape were measured by electro-photometer light scattering and transmission electron microscope. The mean diameter of micelles was 23 nm in aqueous solution. To evaluate the potential of these polymeric micelles as a drug carrier, PSI-mPEG-$C_{16}$-ED was conjugated with Cy5.5 for Near-Infrared Fluorescent (NIRF) based optical imaging. PSI-mPEG-$C_{16}$-ED-Cy5.5 was injected intravenously into mice (n=5) and in vivo NIRF imaging was performed during 48 h after injection. The biodistribution study at 24 h after injection showed the longcirculation property of PSI-mPEG-$C_{16}$-ED-Cy5.5. Therefore, PSI-mPEG-$C_{16}$-ED micelles could be a promising drug carrier and imaging agent.

• 한국식품영양과학회지
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• 제34권9호
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• pp.1450-1458
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• 2005

우리나라 동해심해수의 효율적 활용을 위한 방안의 하나로 chitosan-ascorbate(CA) $0.1\%$를 함유하는 동해심 해수로 담근 물김치의 품질특성을 조사하였다. 물김치 제조는 담금 용수로 mineral salt $1\%$ 함유 증류수(DW), 염도 $1\%$ 동해심 해수(ED), DW+CA(DW-CA) 및 ED + EA(ED-CA)로 구분하여 $10^{\circ}C$에서 12일간 숙성시켰다. 그 결과, ED-CA는 물김치 숙성시 pH의 감소와 산도의 증가를 상당히 지연시키며, 총균수를 감소시키면서 젖산균비율을 높여 위생성을 증진시키며, 항산화성을 높이는 효과가 있었다. 또한 탁도를 감소시켜 국물을 맑고 투명하게 유지하며, 김치 조직의 연화현상을 막아 경도유지와 조직의 알코올 불용성 물질의 용출을 지연시키며, 종합적 기호도를 증진시키는 효과를 나타내어 물김치 담금용수로서의 활용이 기대된다.

• 한국발생생물학회지:발생과생식
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• 제17권3호
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• pp.289-297
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• 2013

Bisphenol A (BPA) is an estrogenic endocrine disrupter. However, depending on a way of treatment, the harmful effects of BPA have not been confirmed. Also, trans-generational effects of BPA on male reproduction are still controversial. Because the reabsorption of testicular fluid in the efferent ductules (ED) and initial segment (IS) is important for sperm maturation, the present study was designed to determine trans-generational effect of BPA administrated orally on expression of water transport-related molecules in the mouse ED and IS. Ethanol-dissolved BPA was diluted in water to be 100 ng (low), $10{\mu}g$ (medium), and $1mg/m{\ell}$ water (high). BPA-containing water was provided for two generations. Expression of ion transporters and water channels in the ED and IS were measured by relative real-time PCR analysis. In the ED, BPA treatment caused expressional increases of carbonic anhydrase II, cystic fibrosis transmembrane regulator, $Na^+/K^+$ ATPase ${\alpha}1$ subunit, and aquaporin (AQP) 1. No change of $Na^+/H^+$ exchange (NHE) 3 expression was detected. BPA treatment at medium dose resulted in an increase of AQP9 expression. In the IS, the highest expressional levels of all molecules tested were observed in medium-dose BPA treatment. Generally, high-dose BPA treatment resulted in a decrease or no change of gene expression. Fluctuation of NHE3 gene expression by BPA treatment at different concentrations was detected. These findings suggest that trans-generational exposure to BPA, even at low dose, could affect gene expression of water-transport related molecules. However, such effects of BPA would be differentially occurred in the ED and IS.

• 분석과학
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• 제29권6호
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• pp.300-304
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• 2016

폐지방산과 ethylenediamine 또는 N,N'-bis (2-hydroxyethyl)ethylenediamine으로부터 아스팔트 박리방지제를 합성하였다. FT-IR과 NMR을 이용하여 분석한 결과 아마이드결합의 생성 및 박리방지제의 합성이 성공적으로 수행되었음이 확인하였다. 합성된 여러 종류의 박리방지제의 접착특성은 접촉각과 BBS 시험을 통해 비교하였다. 접촉각 측정으로부터 에틸렌다이아민과 동물유지로부터 제조된 시료가 가장 소수성이 컸으며, BBS 시험으로부터 수분저항성도 94%로 가장 우수한 것으로 나타났다. 그러나 에틸렌다이아민과 폐식용유의 반응생성물이 수분처리 전과 후의 절대적인 접착력은 각각 약 3610 및 3227 kPa로 가장 우수하였다. 전반적으로 접착력은 ED의 반응생성물이 HEED의 반응생성물보다 우수하였으며, 폐식용유나 동물유지의 반응생성물들이 순수한 콩기름의 반응생성물들보다 우수하였다.

• 농업과학연구
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• 제38권1호
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• pp.65-70
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• 2011

Development of mouse fetus brains can be defined morphologically and functionally by three developmental stages, embryo day (ED) 16, postnatal stage one week and eight weeks. These defined stages of brain development may be closely associated with differential gene expression rates due to limited cellular resources such as energy, space, and free water. Complex patterns of expressed genes and proteins during brain development suggests the changes in relative concentrations of proteins rather than the increase in numbers of new gene products. This study was designed to evaluate early protein expression pattern in mouse fetus brain. The mouse brain proteome of fetus at ED 15.5, and 19.5 was obtained using 2-dimensional gel electrophoresis (DE). Analysis of the 2-DE gels in pH 3-10 range revealed the presence of 15 differentially expressed spots, of which 11 spots were identified to be known proteins following MALDI-TOF analysis; 3 spots were up-regulated and 8 spots were down-regulated in the mouse fetus brain at ED 15.5. UP-regulated proteins were identified as MCG18238, isoform M2 of pyruvate kinase isozymes M1/M2, isoform 2 of heterogeneous nuclear ribonucleoprotein K, heterogeneous nuclear ribonucleoprotein H2, creatine kinase B-type, 40S ribosomal protein SA and hemoglobin subunit beta-H1. Down-regulated proteins were putative uncharacterized protein, lactoylglutathione lyase and secreted acidic cysteine rich glycoprotein. Our results revealed composite profiles of mouse fetus brain proteins related to mouse fetus development by 2-DE analysis implying possible roles of these proteins in neural differentiation.