• Title/Summary/Keyword: $\beta$-protection$

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Synthesis of New Benzylpiperidinyl Ether Derivatives as Amyloid-beta Aggregation Inhibitors (베타아밀로이드응집 억제제 도출을 위한 새로운 벤질피페리디닐에터 유도체의 합성)

  • Kwon, Young-Ee
    • YAKHAK HOEJI
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    • v.50 no.5
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    • pp.326-331
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    • 2006
  • We designed and synthesized new benzylpiperidinyl ether derivatives as beta-amyloid aggregation inhibitors for the development of novel anti-Alzheimer's disease agents. As starting material, 4-hydroxypiperidine was used. For protection of the amine group in piperidine (2), di-tert-butyl dicarbonate was reacted with 4-hydroxypiperidine in the presence of triethylamine. For introduction of benzyl group, benzylbromide was treated with compound 2 in dioxane. After deprotection of Boc group on amine in compound 3, ester (5) was synthesized by addition of ethyl-4-chlorobutyrate. The alcohol 6 was synthesized by hydride reduction of 5 using $LiAlH_4$. To obtain final products (7-14), the alcohol 6 was condensed with each of substituted benzoic acids. To screen beta-amyloid aggregation inhibition of the products, thioflavinT assay was performed using $A{\beta}1-42\;at\;37^{\circ}C$ for 26 h incubation, in vitro. From the result of screening, compound 8, 9, 11 and 12 showed effective activity about $65{\sim}85\;{\mu}M\;as\;IC_{50}$ value. Among the prepared compounds, 4-[4-(benzyloxy)piperidino]butyl-4-chlorobenzoate (8) was the most effective inhibitor having $IC_{50}\;of\;65.4{\mu}M$.

Gross Beta Screening and Monitoring Procedure using Urine Bioassay for Radiation Workers of Radioisotope Production Facilities (뇨시료 전베타 분석법을 이용한 동위원소 생산시설 종사자 내부오염 스크리닝 및 감시절차 개발)

  • Yoon, Seokwon;Kim, Mee-Ryeong;Park, Seyoung;Pak, Min-Jeong;Yoo, Jaeryong;Jang, Han-Ki;Ha, Wi-Ho
    • Journal of Radiation Protection and Research
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    • v.38 no.2
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    • pp.52-59
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    • 2013
  • The internal contamination screening method using gross beta measurement was performed for radioisotope workers. 24 h and spot urine samples from workers of medical isotope production facilities were collected and measured. Most of the results were similar with the background level of gross beta activity except for a specific worker. Gross beta activity was slightly increased in several hours after finishing work. And the environmental factor of production facilities causing internal contamination were estimated based on screening results. The additional detailed internal dose assessment must be followed after the screening for protection of workers. Moreover, a procedure was established to apply a simple internal contamination assessment for radiation workers.

Spinacia oleracea Extract Protects against Chemical-Induced Neuronal Cell Death (시금치 추출물에 의한 뇌세포 사멸 보호 효과)

  • Park, Ja-Young;Heo, Jin-Chul;Woo, Sang-Uk;Shin, Heung-Mook;Kwon, Taeg-Kyu;Lee, Jin-Man;Chung, Shin-Kyo;Lee, Sang-Han
    • Food Science and Preservation
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    • v.14 no.4
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    • pp.425-430
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    • 2007
  • To investigate the potential therapeutic value of a plant extract against amyloid ${\beta}-peptide-induced$ cell damage, we first screened extracts of 250 herbs, and finally selected a water extract of Spinacia oleracea for further study. This extractshowed the potential to inhibit the reactions of oxidants. We measured the angiotensin-converting-enzyme (ACE) inhibitory activity of the extract, and assessed the ability of the extract to protect neuronal cells from chemical-induced cell death. SH-SY5Y neuroblastoma cells were used in this assay. The extract exerted protective effects on $H_2O_2-induced$ cell death, when $H_2O_2$ was used at 100 M, 200 M, and 500 M (protection of 87%, 73%, and 58%, respectively). When 50 M of amyloid ${\beta}-peptide$ was added to the test cells, however, the extract had no protective effect on cell death. The extract inhibited ACE activity in a dose-dependent manner, and exhibited potent protection against the deleterious effects of $H_2O_2$. In sum, these results suggest that a water extract of Spinacia oleracea has the potential to afford protection against chemical-induced neuronal cell death, and the extract may be useful in the treatment of neurodegenerative diseases. The precise molecular mechanism of neuroprotection is under investigation.

Protective Effect of Radix Trichosanthis Extracts on Cytotoxicity of Pancreatic ${\beta}-Cells$ by Cytokines (싸이토카인 유발 췌장 ${\beta}$세포 독성에 대한 천화분 추출물의 방어효과)

  • Song, Mi-Young;Kim, Eun-Kyung;Song, Je-Ho
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.2
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    • pp.422-426
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    • 2008
  • In this study, the preventive effects of Radix Trichosanthis extracts (RTE) against cytokine-induced ${\beta}-cell$ death were assessed. Cytokines generated by immune cells infiltrating pancreatic islets are crucial mediators of ${\beta}-cell$ destruction in insulin-dependent diabetes mellitus. The treatment of RIN cells with $interleukin-1{\beta}$ ($IL-1{\beta}$) and $interferon-{\gamma}$ ($IFN-{\gamma}$) resulted in a reduction of cell viability. RTE protected $IL-1{\beta}$ and $IFN-{\gamma}$-mediated viability reduction in a concentration-dependent manner. Incubation with RTE also induced a significant suppression of $IL-1{\beta}$ and $IFN-{\gamma}$-induced inducible nitric oxide synthase (iNOS) protein expression. The molecular mechanism by which RTE inhibited iNOS protein expression appeared to involve the inhibition of $NF{-\kappa}B$ activation. The $IL-1{\beta}$ and $IFN-{\gamma}$-stimulated RIN cells showed increases in $NF{-\kappa}B$ binding activityand $I{\kappa}B{\alpha}$ degradation in cytosol compared to unstimulated cells. However, pretreatment with RTE inhibited cytokines-induced $I{\kappa}B{\alpha}$ degradation and $NF{-\kappa}B$ activation in RINm5F cells. Furthermore, the protective effects of RTE were verified via protection of impairment in glucose-stimulated insulin secretions in $IL-1{\beta}$ and $IFN-{\gamma}$-treated islets.

Thermoluminescent Response of Thin LiF:Mg,Cu,Na,Si Detectors to Beta Radiation (얇은 LiF:Mg,Cu,Na,Si 검출기의 베타선장에 대한 TL 반응)

  • Nam, Y.M.;Kim, J.L.;Chang, S.Y.;Cho, H.W.;Kim, H.J.
    • Journal of Radiation Protection and Research
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    • v.24 no.1
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    • pp.39-43
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    • 1999
  • Thermoluminescent (TL) response characteristics of a thin LiF:Mg,Cu,Na,Si Teflon detectors have been studied for use in beta radiation detection. The detectors were fabricated from a mixture of LiF:Mg,Cu,Na,Si phosphor and Teflon powder which was molded into a thin disk form of $50mg/cm^2$ thickness. These detectors were irradiated to beta fields of $^{147}Pm,\;^{204}Tl\;and\;^{90}Sr/^{90}Y$ sources with a covering of Kapton foil ($2mg/cm^2$) and photon irradiation was carried out with a $^{137}Cs$ source at the Korea Atomic Energy Research Institute (KAERI). Batch uniformity was estimated to be 4.7% and the beta dose response presented linear relationship from 0.1 mGy to 100 Gy. The beta energy responses of thin detectors normalized to $^{137}Cs$ were presented as 0.46, 1.09 and 1.06 for $^{147}Pm,\;^{204}Tl\;and\;^{90}Sr/^{90}Y$ beta rays, respectively. The evaluated values for angular responses were $0.93{\pm}0.03\;(^{147}Pm),\;0.94{\pm}0.04\;(^{204}Tl),\;and\;0.92{\pm}0.05\;(^{90}Sr/^{90}Y)$. The results satisfied well a proposed ISO Standard for beta ray dosimeters.

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Absolute $^{56}Mn$ Activity Measurement by $4{\pi}{\beta}-{\gamma}$ Conincidence Counting Technique ($4{\pi}{\beta}-{\gamma}$ 동시계수기술에 의한 $^{56}Mn$방사능 절대측정)

  • Hwang, Sun-Tae;Choi, Kil-Oung;Oh, Pil-Jae;Lee, Kyung-Ju;Lee, Kun-Jai
    • Journal of Radiation Protection and Research
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    • v.12 no.2
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    • pp.19-27
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    • 1987
  • In order to determine the $^{56}Mn\;{\gamma}$-detection efficiency of a $MnSO_4$ bath system, it is essential to do the absolute activity measurement of $^{56}Mn$ solution. For the fabrication of $^{56}Mn$ samples, a 13.718 mg of $^{56}Mn$ metal flake with 99.99% purity was irradiated for 12 minutes at the thermal neutron field of about $10^{13}n/cm^2s$ of flux density. The neutron activated $^{56}Mn$ metal sample was dissolved in 50 ml of 0.1 N-HCl solution. The $^{56}Mn$ samples were fabricated by using the dissolved stock solution and the activity of each of them was measured by the $4{\pi}{\beta}-{\gamma}$ coincidence counting technique. The obtained result was 408.070 kBq/mg with total uncertainty of 0.366% at reference date, 0 h on October 15, 1987.

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Development of Prototype Liquid Scintillator System for Monitoring Liquid Radioactive Waste (배수 모니터링 액체섬광검출시스템의 프로토 타입 개발)

  • Nam, Uk-Won;Seon, Kwang-Il;Kong, Kyoung-Nam;Kim, Chang-Kyu;Lee, Dong-Myung;Lee, Sang-Kook
    • Journal of Radiation Protection and Research
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    • v.28 no.3
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    • pp.173-182
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    • 2003
  • A prototype liquid scillatillator system for measurement of multiple beta-labeled mixtures was developed and its characteristic was investigated. The signal processing system consists of two photomultiplier tubes and the coincident count circuit. The characteristic of the system was analyzed using 4 beta-labeled samples $(^3H,\;^{14}C,\;^{36}Cl\;and\;^{90}Sr)$. Beta spectra from the samples were obtained without radiation shielding, and the detection limits for each nuclides were estimated based on the spectra. The estimated detection limits were compared to the legal regulation values. It is found that the liquid radioactive nuclides are detectable well below the legal regulation values.

Development of the ZnS(Ag)/BC-408 phoswich detector for monitoring radioactive contamination inside pipes (배관 내부 방사능 오염도 측정용 ZnS(Ag)/BC-408 phoswich 검출기 개발)

  • Kim, Gye-Hong;Park, Chan-Hee;Jung, Chong-Hun;Lee, Kune-Woo;Seo, Bum-Kyoung
    • Journal of Radiation Protection and Research
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    • v.31 no.3
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    • pp.123-128
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    • 2006
  • A small radiation detection system is necessary for the direct characterization of alpha/beta-ray contamination inside pipes generated during the decommission of a nuclear facility. In this work, the new type phoswich detector consisting of the ZnS(Ag) and plastic scintillator for ${\alpha}/{\beta}$ simultaneous counting was designed as part of a development of a equipment capable of monitoring radiological contamination inside pipes. The optimum counting conditions in dimensions of scintillator and a detection system were experimentally confirmed and a performance of alpha/beta-ray discrimination was evaluated. As a result, optimum conditions of a detector suitable for monitoring radiological contamination inside pipes and a feasibility of application to pipe-inside were confirmed.

Preliminary Study on Rapid Measurement of Gross Alpha/Beta and 90Sr Activities in Surface Soil by Mobile ZnS(Ag)/PTV Array and Handheld PVT Rod with Gated Energy Channels

  • Lee, Chanki;Kim, Hee Reyoung
    • Journal of Radiation Protection and Research
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    • v.46 no.4
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    • pp.194-203
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    • 2021
  • Background: Surface soil radiation monitoring around nuclear facilities is important to classify and characterize the contaminated areas. A scanning and direct measurement technique can survey the sites rapidly before starting sampling analysis. Materials and Methods: Regarding this, we test and suggest a measurement technique for gross alpha/beta and 90Sr activities in surface soil based on a mobile ZnS(Ag)/PVT (polyvinyltoluene) array and a handheld PVT rod, respectively. To detect 90Sr selectively in soil mixed with naturally occurring radioactive materials, chosen energy channel counts from the multichannel analyzers were used instead of whole channel counts. Soil samples contaminated with exempt liquid 90Sr with 1 Bq·g-1, 3 Bq·g-1, and 10 Bq·g-1 were prepared and hardened by flocculation. Results and Discussion: The mobile ZnS(Ag)/PVT array could discriminate gross alpha, gross beta, and gamma radiation by the different pulse-shaped signal features of each sensor material. If the array is deployed on a vehicle, the scan minimum detectable concentration (MDC) range will be about 0.11-0.17 Bq·g-1 at 18 km·h-1 speed, highly sensitive to actual sites. The handheld PVT rod with 12 mm (Φ) × 20 mm (H) size can directly measure 90Sr selectively if channels on which energies are from 1,470 and 2,279 keV are gated, minimizing crossdetection of other radionuclides. These methods were verified by measuring soil samples fabricated with homogeneous 90Sr concentrations, showing static MDC of 2.16 Bq·g-1 at a measurement time of 300 seconds. Conclusion: Based on the results, comprehensive procedures using these detectors are suggested to optimize soil sites survey.

The MAP Kinase Kinase Gene AbSte7 Regulates Multiple Aspects of Alternaria brassicicola Pathogenesis

  • Lu, Kai;Zhang, Min;Yang, Ran;Zhang, Min;Guo, Qinjun;Baek, Kwang-Hyun;Xu, Houjuan
    • The Plant Pathology Journal
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    • v.35 no.2
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    • pp.91-99
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    • 2019
  • Mitogen-activated protein kinase (MAPK) cascades in fungi are ubiquitously conserved signaling pathways that regulate stress responses, vegetative growth, pathogenicity, and many other developmental processes. Previously, we reported that the AbSte7 gene, which encodes a mitogen-activated protein kinase kinase (MAPKK) in Alternaria brassicicola, plays a central role in pathogenicity against host cabbage plants. In this research, we further characterized the role of AbSte7 in the pathogenicity of this fungus using ${\Delta}AbSte7$ mutants. Disruption of the AbSte7 gene of A. brassicicola reduced accumulation of metabolites toxic to the host plant in liquid culture media. The ${\Delta}AbSte7$ mutants could not efficiently detoxify cruciferous phytoalexin brassinin, possibly due to reduced expression of the brassinin hydrolase gene involved in detoxifying brassinin. Disruption of the AbSte7 gene also severely impaired fungal detoxification of reactive oxygen species. AbSte7 gene disruption reduced the enzymatic activity of cell walldegrading enzymes, including cellulase, ${\beta}$-glucosidase, pectin methylesterase, polymethyl-galacturonase, and polygalacturonic acid transeliminase, during host plant infection. Altogether, the data strongly suggest the MAPKK gene AbSte7 plays a pivotal role in A. brassicicola during host infection by regulating multiple steps, and thus increasing pathogenicity and inhibiting host defenses.