• Title/Summary/Keyword: 중기유도

Search Result 89, Processing Time 0.026 seconds

Syntheses and Central Nervous Depressant Activities of Piperine Derivatives (V) (피페린 유도체의 합성 및 중추 억제작용에 관한 연구(V) -Methylenedioxyphenylalkenoic Acid Amide 유도체-)

  • 도경삼;임중기;우경식;이은방
    • YAKHAK HOEJI
    • /
    • v.30 no.4
    • /
    • pp.163-168
    • /
    • 1986
  • Thirteen compounds were synthesized by condensing the N-heterocyclic amines (piperidine, pyrrolidine, morpholine) and secondary aliphatic amines (dimethylamine, diethylamine) with 3,4-methylenedioxyphenylalkenoic acid chlorides for developing CNS depressants. Among them, N, N-diethyl-3,4-methylenedioxycinnamamide (IX) and N, N-dimethyl-5-(3,4-methylenedioxyphenyl)-2, 4-pentadienoic acid amicle (XII) exhibited strong activity in antagonism against pentylenetetrazole-induced convulsion, strychnine-induced convulsion and maximal electroshock seizure. N, N-Dimethyl-3, 4-methylenedioxycinnamide (VIII) showed more potent activity in antagonism against strychnine-induced convulsion and maximal electroshock seizure and in the prolongation of hexobarbital sleeping time.

  • PDF

Effects of Selenate on Adipocyte Differentiation and the Expression of Selenoproteins in 3T3-L1 Cells (3T3-L1세포에서 selenate의 처리가 세포의 분화와 selenoprotein의 발현에 미치는 영향)

  • Park, Seol Hui;Moon, Yang Soo
    • Journal of Life Science
    • /
    • v.24 no.10
    • /
    • pp.1085-1091
    • /
    • 2014
  • The purpose of this study was to determine the effect of selenate on adipocyte differentiation and to identify genes involved in the modulation of adipogenesis in 3T3-L1 cells. To test the effect of selenate on adipocyte differentiation, adipogenesis was induced in cells using various concentrations ($0-100{\mu}M$) of selenate. Various phases of adipogenesis were induced: postconfluent (PC), early phase (EP, d0-d2), postmitotic growth arrest (PM, d2-d4), and all period (AP). The PC cells exposed to selenate for 24 h displayed dose-dependent inhibition of intracellular lipid droplet accumulation on day 6 of adipogenesis. Two days of selenate treatment at EP or AP inhibited adipogenesis, with an approximately 20-80% reduction in lipid accumulation compared to that of a control (p<0.05). When preadipocytes were exposed to selenate during the PM period, the antiadipogenic effect of selenate was attenuated. Two types of selenoprotein genes (Seps1 and Sepp1) were up-regulated by the selenate treatment during mitotic clonal expansion, whereas these genes were down-regulated during PM growth arrest (p<0.05). The findings demonstrate the antiadipogenic function of selenate and the possible involvement of Sepp1 and Seps1 genes in selenate-inhibited adipogenesis in 3T3-L1 cells.

Studies on the Synthesis and Antibacterial Activity of PAS-Sulfonamide Derivatives (PAS-Sulfonamide 유도체의 합성 및 항균력에 관한 연구)

  • 이남순;임중기;원정희;유서홍
    • YAKHAK HOEJI
    • /
    • v.23 no.3_4
    • /
    • pp.159-166
    • /
    • 1979
  • Twelve derivatives of PAS-sulfonamide were synthesized and tested for their antibacterial activity against various bacterial strains. The derivatives XII and XIV showed relatively potent antibacterial activity to INAH-R strains and INAH-PAS-R strains and type XII to streptococcal strains; type IX and type VI to Pseudomonas aeruginosa.

  • PDF

랫드에서 D-galactosamine을 이용한 중기 발암성 검색법에서 natural killer 세포활성 및 c-myc 종양 단백질 발현에 관한 연구

  • 이영순;강경선;조재진;남기환
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1994.04a
    • /
    • pp.191-191
    • /
    • 1994
  • 본 연구는 D-galactosamine을 이용한 중기발암성 모델에서 세포성면역중의 하나인 natural killer (NK) 세포활성과 c-myc 종양단백의 발현을 알아보기 위하여 실시하였다. 수컷 6주령의 SPF SD랫드 50마리를 3개군으로 각 군당 20마리씩 나누어 배치하였다. 실험 0일에 제 1,2 군에서 DEN을 복강내로 체중 kg당 200mg 1회 투여하여 발암유발을 하였으며 대조군인 제 3군에는 saline을 투여하였다. 제 2주에 제 1군에는 강력한 발암촉진물질인 2-acetylaminofluorene (AAF)을 사료에 0.01% 투여하였으며, 제 2군은 미약한 발암촉진물질인 phenobarbital (PB)을 0.05%로 음수에 6주간 투여하였다 제 8, 15, 36주에 경시적으로 부검하였다. 제 8주에 부검시 GST-P$^{+}$ 병변이 잘 유도되어 전암병변의 유도가 잘 되었음을 확인하였다. 제 15주에 부검시 AAF를 투여한 군에서 glutathione S-transferase placental form (GST-p)에 대한 면역조직화학적 염색에서 AAF와 PB를 투여한 제 1군 및 제 2군의 간장에서는 주위조직과 한계가 명료한 GST-P$^{+}$ 증식성 결절과 병소를 관찰할 수 있었으나 기초 사료만을 투여한 제 3군은 어떠한 GST-P$^{+}$ 증식성 결절 및 병소를 관찰할 수 없었다. 랫드에서 natural killer세포는 사람이나 마우스에서 주로 자연살생능 (natural killing activity)을 보이는 LGL(lure granular lymphocyte)의 형태를 띄고 있었으며 LGL 이라고 부르는 것처럼 특징적으로 세포질 대 핵의 비율이 높고 azurophilic 과립을 세포질내에 함유하고 있으며 일반적으로 신장 형태의 핵을 가지고 있었다. 또한 세포의 크기는 small lymphocyte와 대식세포 (macrophage)의 중간 크기였다. 15주와 시험종료시 정상대조군인 제 3군의 랫드로 부터 분리한 NK 세포활성도 (% cytotoxicity)에 비하여 발암물질 투여군의 NK 활성도는 PB 투여군들의 NK활성도 보다 약간 낮았다. 랫드에서 c-myc 종양단백은 65KD 와 671KD 에서 band가 형성된 것이 관찰되었다. 시험 개시후 15주에 부검한 랫드의 간에서 c-myc 종양단백의 발현은 모든 처리군들이 대조군에 비하여 높게 발현되는. 것이 관찰되었으나 시험개시후 26주에 부검한 랫드의 간에서 c-myc 종양단백의 발현은 대조군에 비하여 차이가 거의 없었다. 따라서 랫드에서 화학적으로 유도한 간암발생 과정에서 NK 세포활성이 현저하게 억제되는 것으로 생각되며, c-myc 종양단백의 발현은 시험개시후 15주에 그 발현이 확실한 것으로 사료되어 진다.

  • PDF

Synthesis of Melandrin Derivatives (Melandrin 유도체의 합성)

  • Lim, Jung-Ki;Woo, Won-Sick;Lee, Kang-Ro;Ma, Eun-Sook
    • YAKHAK HOEJI
    • /
    • v.38 no.3
    • /
    • pp.281-285
    • /
    • 1994
  • Melandrin was isolated from the Melandrium firmum(Caryophyllaceae), its structure was N-(p-hydroxybenzoyl)-5-hydroxyanthranilic acid. Fourteen melandrin derivatives(I-XIV) were synthesized and according to MME calculation by the computer, optimized three dimensional structure of compounds was obtained. The space orientation of compounds was cis-form as a indomethacin.

  • PDF

Syntheses and Central Nervous Depressant Activities of Piperine Derivatives (II) Piperic Acid Amides (Piperine유도체의 합성 및 중추억제작용에 관한 연구(II) Piperic Acid Amide 유도체)

  • 은재순;임중기;김완주;우원식;이은방
    • YAKHAK HOEJI
    • /
    • v.27 no.4
    • /
    • pp.283-287
    • /
    • 1983
  • In order to search more active and less toxic central nervous depressants, piperic acid amides were synthesized by condensation of piperonal with crotonic acid amides. The bioassay results revealed that, among the compounds synthesized, the piperonic acid methylamide and ethylamide exhibited potent protective activity against strychnine-induced convulsion.

  • PDF

Syntheses and Central Nervous Depressant Activity of Piperine Derivatives(III) N-Piperoyl Amino Acids (Piperine유도체의 합성 및 중추억제작용에 관한 연구(III) N-Piperoylamino Acid 유도체)

  • 이한구;임중기;이은방;우원식
    • YAKHAK HOEJI
    • /
    • v.27 no.4
    • /
    • pp.289-293
    • /
    • 1983
  • Twelve new N-piperoyl amino acids were synthesized by acylation of amino acids with piperoylchloride in order to develop the new central nervous depressants. Silylation of the carboxylic group of amino acids not only precluded side reactions but-also facilitated acylation at room temperature without catalysts. The acute toxicity of all the synthesized compounds were lower than that of piperine itself, whereas they showed strong protective effect against the strychnine-induced mortality.

  • PDF

Development of Wind Turbine Simulator Using 3kW PMSG (3kW 영구 자석형 동기발전기를 이용한 풍력 터빈 시뮬레이터 개발)

  • Choi, Wonshik;Oh, Joongki;Park, Kihyun;Park, Hyunchul
    • 한국신재생에너지학회:학술대회논문집
    • /
    • 2010.11a
    • /
    • pp.182.1-182.1
    • /
    • 2010
  • 본 논문에서는 3kW 영구 자석형 동기발전기(PMSG)를 이용한 풍력 터빈 시뮬레이터 개발에 대해 기술하였다. 풍력발전 시스템은 블레이드를 포함한 회전부, 동력 전달부, 발전기, 전력변환기로 크게 나눌 수 있으며, 시뮬레이터는 유도 모터와 PMSG, 인버터-컨버터와 제어 시스템으로 이루어진다. 시뮬레이터를 운전하기 위해서는 특정 속도의 바람 모델을 적용하여 풍력 발전기의 회전부에 걸리게 되는 토크와 회전 속도 값이 요구된다. 풍력 터빈 모델로부터 계산값을 시뮬레이터에 맞게 스케일링하여 유도 모터를 구동 한다. 발전기측 컨버터는 MPPT(Maximum Power Point Tracking) 알고리즘을 통해 제어하고 계통측 인버터는 유효 전력과 무효 전력을 제어하도록 한다. PSIM과 MATLAB/SIMULINK를 이용하여 컴퓨터 시뮬레이션으로 그 결과를 증명하였다.

  • PDF

Syntheses and Central Nervous Depressant Activity of Piperine Derivatives(I) 3,4-methylenedioxycinnamic Acid Derivatives (Piperine 유도체의 합성 및 중추억제작용에 관한 연구(I) 3,4-Methylenedioxycinnamic Acid 유도체)

  • 임중기;이동웅;이진영;김연순;우원식;이은방
    • YAKHAK HOEJI
    • /
    • v.26 no.4
    • /
    • pp.189-196
    • /
    • 1982
  • Piperine was reported to have a potential central nervous system (CNS) depressant activity in mice. In order to search a more active and less toxic compound than piperine and to elucidate the active group of piperine, the aromatic amides (10 compeunds) and aromatic esters (10 cempounds) of 3, 4-methylenedioxycinnamic acid were synthesized and evaluated on CNS depressant activity in comparison with piperine. The pharmacological tests conducted are as follows; (1) Acute, toxicity, (2) Antagonism against strychnine induced conduced convulsion, (3) Antagonism against maximal electrobhock seizure, (4) Rotarod test, (5) Potentiation of hexobarbital sleeping time. It was observed that 3, 4-methylendioxycinanamic acid derivatives were less toxic than piperine, and showed no significant CNS depressant activities. These facts indicate that the piperoyl group might be concerned with the pharmacological activity of piperine.

  • PDF

Artificial Activation of Pig Oocytes Arrested at meiotic Metaphase II (제2감수분열 중기에서 발달정지된 돼지 난자의 인위적 난활성)

  • R. S. Prather;;Z. Mach ty
    • Korean Journal of Animal Reproduction
    • /
    • v.20 no.4
    • /
    • pp.395-412
    • /
    • 1997
  • Mammalian eggs are ovulated arrested at meiotic metaphase II until fertilization. Generally in mammals, fertilization results in a series of intracellular calcium oscillations that are mediated by inositol triphosphate (IP$^3$) or cyclic adenosine diphosphoribose (cADPr). The high levels of maturation promotion factor (MPF) within the cell decrease, pronuclei form, the cytoskeleton is reorganized and proteins are post-translationally modified. If all is normal, the newly formed embryo initiates the developmental program specific to that species. Artificial methods of producing these effects in pig oocytes are discussed. One potential mechanism mediated via a signal transduction pathway is present in pig oocytes. Stimulation of this pathway leads to the early events following fertilization, and electrical stimulation leads to apparently normal de v velopment to day 12. Further studies are needed to determine which mechanism(s) the sperm uses to initiate development.

  • PDF