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Development of Cholinesterase Inhibitors using 1-Benzyl Piperidin-4-yl (α)-Lipoic Amide Molecules

  • Lee, Seung-Hwan;Kim, Beom-Cheol;Kim, Jae-Kwan;Lee, Hye Sook;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • v.35 no.6
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    • pp.1681-1686
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    • 2014
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

Prvalence and Morphological Identification of Eimeria bukidnonensis and E. wyomingensis in Cattle, Korea (국내(國內)소의 Eimeria bukidnonensis와 E. wyomingensis의 감염율조사(感染率調査)와 형태학적(形態學的) 특징(特徵)에 관한 연구(硏究))

  • Wee, Sung-hwan;Kang, Yung-bai;Kim, Sang-hee
    • Korean Journal of Veterinary Research
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    • v.28 no.1
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    • pp.169-174
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    • 1988
  • To determine the prevalence and the morphological identification of two Eimeria species in fecal examinations, a total of 1092 fecal specimens collected during the period of March to December in 1987 was tested by means of flotation technique. The results obtained were summarized as follow: 1. The prevalence of two species was revealed as 1.83% and 0.92% in E. bukidnonensis and E. wyomingensis, respectively. 2. The oocysts of E. bukidnonensis measured in range of $41.3{\mu}m$ to $49.4{\mu}m(mean\;45.5{\pm}1.7){\times}28.8{\mu}m$ to $35.3{\mu}m(mean\;32.2{\pm}1.2)$, and E. wyomingensis $36.9{\mu}m$ to $44.5{\mu}m(mean\;39.8{\pm}1.7){\times}26.5{\mu}m$ to $29.9{\mu}m(mean\;28.2{\pm}0.9)$. 3. The oocysts of E. bukidnonensis appeared darker and more robust than those of E. wyomingensis. 4. The striations in the oocyst wall of E. bukidnonensis were more peculiar than in E. wyomingensis. 5. Among the morphological characteristic, the widths could be reliably taken as a differential point of view for two Eimeria species.

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Effect Of Substituted-Fe for the Charge-discharge behavior Of $LiMn_{2}O_{4}$cathode materials (Fe 치환이$LiMn_{2}O_{4}$정극 활물질의 충방전 특성에 미치는 영향)

  • 정인성;김민성;구할본;손명모;이헌수
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2000.07a
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    • pp.548-551
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    • 2000
  • Spinel phase LiF $e_{y}$M $n_{2-y}$ $O_4$samples are synthesized by calcining a LiOH.$H_2O$, Mn $O_2$and F $e_2$ $O_3$mixture at 80$0^{\circ}C$ for 36h in air. Preparing LiF $e_{y}$M $n_{2-y}$ $O_4$showed spinel phase with cubic phase. The ununiform distortion of the crystallite of the spinel LiF $e_{y}$M $n_{2-y}$ $O_4$was more stable than that of the pure. The discharge capacity of the cathode for the Li/LiF $e_{0.1}$M $n_{1.9}$ $O_4$cell at the first than that of the pure. The discharge capacity of the cathode for the Li/LiF $e_{0.1}$M $n_{1.9}$ $O_4$cell at the first cycle and at the 70th cycle was about 113 and 90mAh/g, respectively. This cell capacity was retained about 82% of the first cycle after 70th cycle. Impedance profile of this cell was more stable than that pure. The resistance, the capacitance and chemical diffusion coefficients of lithium ion showed approximately 80$\Omega$, 36133.87$\mu$F ; 1.4$\times$10$^{-8}$ c $m^2$ $s^{-1}$ , respectively. , respectively.ely.

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Associations between Anemia and Glomerular Filtration Rate and Albuminuria in Korean Adults by Metabolic Syndrome Status: Analysis of KNHNES V-3 Data (대한민국 성인의 대사증후군 유무에 따른 빈혈과 사구체 여과율 및 알부민뇨의 연관성: 국민건강영양조사 V-3 분석)

  • Hyun YOON
    • Korean Journal of Clinical Laboratory Science
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    • v.56 no.2
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    • pp.125-134
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    • 2024
  • The present study was conducted to explore relationships between anemia and estimated glomerular filtration rate (eGFR) and urine microalbumin/creatinine ratio (uACR) in Korean adults with or without metabolic syndrome (MetS). The data of 4,943 adults aged ≥20 years who participated in KNHNES V-3 (2012) were analyzed. In the non-MetS group, the odds ratio (OR) for anemia of those with a decreased eGFR {eGFR<60 mL/min/1.73 m2, 3.85 (95% confidence interval [CI], 2.03~7.30)} was significant as was the OR of those with decreased eGFR plus elevated uACR (eGFR<60 mL/min/1.73 m2 and uACR≥30 mg/g, 5.81 [95% CI, 2.60~13.02]). In the MetS group, ORs for anemia for those with an elevated uACR (2.18 [95% CI, 1.11~4.27]), a decreased eGFR (3.74 [95% CI, 1.11~12.55]), or a decreased eGFR plus an elevated uACR (16.79 [95% CI, 5.93~47.57]) were significant. In conclusion, in non-MetS, anemia was associated with a low eGFR, whereas in MetS, anemia was associated with a low eGFR and an elevated uACR. In addition, the OR for anemia was greatly increased when eGFR was diminished and uACR was elevated regardless of MetS and MetS status.

Dose evaluation of workers according to operating time and outflow rate in a spent resin treatment facility

  • Byun, Jaehoon;Choi, Woo Nyun;Kim, Hee Reyoung
    • Nuclear Engineering and Technology
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    • v.53 no.11
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    • pp.3824-3836
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    • 2021
  • Workers' safety from radiological exposure in a 1 ton/day capacity spent resin treatment facility was evaluated according to the operating times and outflow rate due to process related leakages. The conservative annual dose based on the operating times of the workers exceeded the dose limit by at least 7.38E+01 mSv for close work. The realistic dose range was derived as 1.62E+01 mSv-6.60E+01 mSv. The conservative and realistic annual doses for remote workers were 1.33E+01 mSv and 3.00E+00 mSv respectively, which were less than the dose limit. The MWR was identified as the major contributor to worker exposure within the 1 h period required for removal of radioactive materials. The dose considering both internal and external exposures without APF was derived to be 1.92E+01 mSv for conservative evaluation and 4.00E+00 mSv for realistic evaluation. Furthermore, the dose with APF was derived as 7.27E-01 mSv for conservative evaluation and 1.51E-01 mSv for realistic evaluation. Considering the APF for leakage from all parts, the dose range was derived as 1.25E+00 mSv-2.03E+00 mSv for conservative evaluation and 2.61E-01 mSv-4.23E-01 mSv for realistic evaluation. Hence, it was confirmed that radiological safety was secured in the event of a leakage accident.

Some Characterizations of Modules via Essentially Small Submodules

  • Le, Van Thuyet;Phan, Hong Tin
    • Kyungpook Mathematical Journal
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    • v.56 no.4
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    • pp.1069-1083
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    • 2016
  • In this paper, the structure of e-local modules and classes of modules via essentially small are investigated. We show that the following conditions are equivalent for a module M: (1) M is e-local; (2) $Rad_e(M)$ is a maximal submodule of M and every proper essential submodule of M is contained in a maximal submodule; (3) M has a unique essential maximal submodule and every proper essential submodule of M is contained in a maximal submodule.

RADIATION DOSE TO HUMAN AND NON-HUMAN BIOTA IN THE REPUBLIC OF KOREA RESULTING FROM THE FUKUSHIMA NUCLEAR ACCIDENT

  • Keum, Dong-Kwon;Jun, In;Lim, Kwang-Muk;Choi, Yong-Ho
    • Nuclear Engineering and Technology
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    • v.45 no.1
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    • pp.1-12
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    • 2013
  • This paper describes the radiation doses to human and non-human biota in the Republic of Korea, as a result of the Fukushima nuclear accident. By using the measured airborne activity and ground deposition, the effective and thyroid doses of five human age groups (infant, 5 years, 10 years, 15 years and adult) were estimated by the ECOSYS code, and the whole body absorbed dose rate of the eight Korean reference animals and plants (RAPs) was estimated by the K-BIOTA (the Korean computer code to assess the risk of radioactivity to wildlife). The first-year effective and thyroid human doses ranged from 5.7E-5 mSv in the infant group to 2.0E-4 mSv in the 5 years group, and from 5.0E-4 mSv in the infant group to 3.4E-3 mSv in the 5 years group, respectively. The life-time (70 years) effective and thyroid human doses ranged from 1.5E-4 mSv in the infant group to 3.0E-4 mSv in the 5 years group, and from 6.0E-4 mSv in the infant group to 3.5E-3 mSv in the 5 years group, respectively. The estimated maximum whole body absorbed dose rate to the Korean RAPs was 6.7E-7 mGy/d for a snake living in soil (terrestrial biota), and 2.0E-5 mGy/d for freshwater fish (aquatic biota), both of which were far less than the generic dose criteria to protect biota from ionizing radiation. Also, the screening level assessment for ERICA's (Environmental Risks from Ionizing Contaminants: Assessments and management) limiting organisms showed that the risk quotient (RQ) for the estimated maximum soil and water activity was significantly less than unity for both the terrestrial and freshwater organisms. Conclusively, the radiological risk of the radioactivity released into the environment by the Fukushima nuclear accident to the public and the non-human biota in the republic of Korea is considered negligible.

Odd Harmonious and Strongly Odd Harmonious Graphs

  • Seoud, Mohamed Abdel-Azim;Hafez, Hamdy Mohamed
    • Kyungpook Mathematical Journal
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    • v.58 no.4
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    • pp.747-759
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    • 2018
  • A graph G = (V (G), E(G) of order n = |V (G)| and size m = |E(G)| is said to be odd harmonious if there exists an injection $f:V(G){\rightarrow}\{0,\;1,\;2,\;{\ldots},\;2m-1\}$ such that the induced function $f^*:E(G){\rightarrow}\{1,\;3,\;5,\;{\ldots},\;2m-1\}$ defined by $f^*(uv)=f(u)+f(v)$ is bijection. While a bipartite graph G with partite sets A and B is said to be bigraceful if there exist a pair of injective functions $f_A:A{\rightarrow}\{0,\;1,\;{\ldots},\;m-1\}$ and $f_B:B{\rightarrow}\{0,\;1,\;{\ldots},\;m-1\}$ such that the induced labeling on the edges $f_{E(G)}:E(G){\rightarrow}\{0,\;1,\;{\ldots},\;m-1\}$ defined by $f_{E(G)}(uv)=f_A(u)-f_B(v)$ (with respect to the ordered partition (A, B)), is also injective. In this paper we prove that odd harmonious graphs and bigraceful graphs are equivalent. We also prove that the number of distinct odd harmonious labeled graphs on m edges is m! and the number of distinct strongly odd harmonious labeled graphs on m edges is [m/2]![m/2]!. We prove that the Cartesian product of strongly odd harmonious trees is strongly odd harmonious. We find some new disconnected odd harmonious graphs.

Relationship between Hypertension and the Declining Renal Function in Korean Adults (한국 성인에서 고혈압과 신기능 저하와의 관련성)

  • Lee, Jun Ho
    • Korean Journal of Clinical Laboratory Science
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    • v.53 no.1
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    • pp.32-40
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    • 2021
  • This study examined the association between hypertension (HTN), estimated glomerular filtration rate (eGFR), and urine microalbumin/creatinine ratio (ACR) in Korean adults. Data for 8,922 adults (3,941 men and 4,981 women) aged ≥20 years from the Sixth Korean National Health and Nutrition Examination Survey VI (2013~2014) were analyzed. In men, after adjusting for the related variables, the odds ratios (ORs) of HTN [systolic blood pressure (SBP) ≥140 mmHg, diastolic blood pressure (DBP) ≥90 mmHg, or use of HTN medications] were significantly higher in the decreased eGFR group [eGFR <60 mL/min/1.73 ㎡, 1.98 (95% CI, 1.21~3.24)], elevated ACR group [ACR ≥30 mg/g, 2.03 (95% CI, 1.54~2.69)], and decreased eGFR plus elevated ACR group [eGFR <60 mL/min/1.73 ㎡ and ACR ≥30 mg/g, 6.03 (95% CI, 2.82~12.92)] than in the normal group (eGFR ≥60 mL/min/1.73 ㎡ and ACR <30 mg/g). In women, after adjusting for the related variables, the ORs of HTN were significantly higher in the decreased eGFR group (2.29, 95% CI, 1.27~4.13), elevated ACR group (2.22, 95% CI, 1.68~2.94), and decreased eGFR plus elevated ACR group (10.77, 95% CI, 3.89~29.82) than the normal group. In conclusion, HTN was associated with a decreased eGFR and elevated ACR in Korean men and women. In addition, the prevalence of HTN increased greatly when a decreased eGFR and elevated ACR occurred simultaneously.

Comparison of Radical Scavenging, Anticytotoxic, and Anti-Inflammatory Effects of Euphorbia Maculata and E. supina (큰땅빈대와 애기땅빈대의 라디칼 소거, 세포독성 억제 및 항염증 활성 비교)

  • Rhim, Tae-Jin
    • Journal of Environmental Science International
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    • v.25 no.8
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    • pp.1131-1142
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    • 2016
  • This study was conducted to compare the antioxidant, anticytotoxic, and anti-inflammatory properties of Euphorbia maculata ethanol extract with those of E. supina ethanol extract. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical and superoxide scavenging activities of E. maculata at $50{\mu}g/mL$ were $38.3{\pm}3.7$ and $21.5{\pm}1.2%$, respectively, whereas those of E. supina at the same concentration were $109.4{\pm}0.9$ and $59.5{\pm}4.8%$, respectively. Oxygen radical absorbance capacities of E. maculata and E. supina at $10{\mu}g/mL$ were $14.70{\pm}0.63$ and $26.17{\pm}1.36nmol/mL$ Trolox, respectively. Cupric reducing antioxidant capacities of E. maculata and E. supina at $10{\mu}g/mL$ were $10.22{\pm}0.97$ and $62.99{\pm}5.28nmol/mL$ Trolox, respectively. Total phenolic contents of E. maculata and E. supina at $50{\mu}g/mL$ were $29.03{\pm}0.14$ and $87.89{\pm}0.20nmol/mL$ gallic acid, respectively. E. maculata and E. supina were reported to prevent supercoiled DNA breakage induced by peroxyl and hydroxyl radicals in a concentration-dependent manner, where protection against the supercoiled DNA breakage provided by E. supina was greater than that provided by E. maculata. E. maculata and E. supina at $100{\mu}g/mL$ inhibited tert-butyl hydroperoxide-induced cytotoxicity in HepG2 cells by $49.4{\pm}4.3$ and $87.3{\pm}4.5%$, respectively. E. maculata and E. supina at $500{\mu}g/mL$ inhibited lipopolysaccharide-induced nitric oxide production in RAW 264.7 cells by $63.1{\pm}7.0$ and $85.2{\pm}1.6%$, respectively. The antioxidant capacities including DPPH radical scavenging, superoxide scavenging, oxygen radical absorbance, and cupric reducing antioxidant activity were found to be highly correlated with total phenolic content (0.896 < r < 0.983, p < 0.01) and anticytotoxic activities (0.915 < r < 0.960, p < 0.01). However, the superoxide scavenging activity was not significantly correlated (r = 0.604, p > 0.05) with the anti-inflammatory activity. Thus, these findings demonstrated that the radical scavenging, anticytotoxic, and anti-inflammatory capacities of E. supina were more potent than those of E. maculata. Further studies are needed to elucidate the properties of polyphenolic constituents in E. supina responsible for these effects and the underlying mechanisms.