• Title/Summary/Keyword: 길항저해제

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Action of Opiates on LHRH Release in vitro and Adenylate Cyelase Activity by Rat Hypothalamus (시상하부의 is vitro LHRH 분비와 adenylase cyclase 활성에 미치는 opiate의 작용)

  • 김경진;이병주조완규
    • The Korean Journal of Zoology
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    • v.30 no.4
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    • pp.341-350
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    • 1987
  • LHRH분비와 환denylate cyclase활성에 미치는 PGE2, Opioid, 그리고 Ca2+의 영향을 흰쥐의 시상하부 조직을 사용하여 조사하였다. K+(30mM)에 의한 LHR광분비촉진은 Ca2+의존적인데 반하여, PGE2에 의해 촉진되는 LHR노 분비는 세포의 Ca2+농도에 의존하지 않았다. PGE2에 의한 LHR기 분비와 CAMP합성은 PGE2농도(1$\times$10-7M-1$\times$10-4M)에 비례하여 촉진되었으며, $\beta$-endorphin (1x10-3M)은 PGEa에 의한 LHRH 분비촉진과 CAMP합성을 공히 억제하였다. 오피오이드 수용체의 길항제인 Naloxone(Ix10-"M)은 $\beta$-endorphin에 의한 저해효과를 극복시켜서, LHR광 분비와 CAMP합성은 각각 회복되었으나, CAMP합성은 부분적인 회복을 보인 반면에, LHRH분비는 PGE2에 의한 촉진효과보다도 더 활성화되었다. 결론적으로 LHRH분비에 미치는 오퍼오이드의 억제작용은 PGE2-cAMP의 세포내 전달과정을 저해함으로써 유발되는것으로 추정 된다.정 된다.

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T0901317 as an Inhibitor of Transcriptional Activation of Constitutive Androstane Receptor (CAR) (Constitutive androstane receptor (CAR)의 전사활성 저해제로서의 T0901317)

  • Kim, Hyun-Ha;Seol, Won-Gi
    • Journal of Life Science
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    • v.21 no.4
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    • pp.481-485
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    • 2011
  • T0901317 is a potent synthetic ligand for liver X receptor (LXR, NR1H2/3), a member of the nuclear receptor superfamily that functions as a transcription factor. However, T0901317 has been also reported to modulate the activity at least four other nuclear receptors (NRs), acting as agonists for farnesoid X receptor (FXR, NR1H4) and pregnane X receptor (PXR, NR1I2) and as antagonists for androgen receptor (AR, NR3C4) and retinoid-related orphan receptor-${\alpha}$ (ROR-${\alpha}$, NR1F1). We report here that T0901317 can also function as an inhibitor for constitutive androstane receptor (CAR, NR1I3). Since CAR is a major player of xenobiotic and cholesterol metabolism in the liver, along with PXR, FXR and LXR, which are reported to be regulated by T0901317, this further complicates the interpretation of potential results with T0901317 in liver cells.

Comparison of Herbicidal Action between Pyrazosulfuron - ethyl and Imazaquin (Pyrazosulfuron - ethyl과 Imazaquin의 살초작용 비교)

  • Hwang, I.T.;Choi, J.S.;Kim, J.S.;Cho, K.Y
    • Korean Journal of Weed Science
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    • v.16 no.4
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    • pp.317-326
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    • 1996
  • To know whether pyrazosulfuron-ethyl(PYR) and imazaquin(IMA), known as a acetolactate synthase(ALS) inhibitors, have a same herbicidal action pattern in rice(Oryza sativa) or barnyardgrass (Echinochloa crus-galli), an inhibition pattern and a response characteristics in combination with dymron or butachlor were investigated. In contrast to the phytotoxicity of rice treated with IMA, the one treated with PYR was completely tended to be recovered after 25 days after treatment. Safening effect of dymron against PYR was effectively developed to transplanted-rice, while such an effect was not shown in combination with IMA. In combination with PYR and butachlor, antagonistic effect was observed in both simultaneous or sequential treatment on bamyardgrass, however, additive effect was rather shown in combination with IMA and its activity was dominantly dependent on the first applied compound. $I_{50}$ of PYR and IMA on the ALS extracted from barnyardgrass was $4{\times}10^{-7}$M and $2.8{\times}10^{-6})$M, respectively. Butachlor did not affect their activities on ALS in vitro. These results suggest that PYR and IMA might have a different action each other in the pathway to a final herbicidal activity even though their primary action site is ALS.

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Studies on Effect and its Mechanism of Herbicide Mixture of Cyhalofop-butyl, pyribenzoxim and Pyrazosulfuron-ethyl - II. Effect of Herbicide Mixture on the Activity of ALS, Content of Free Amino Acids and Fatty Acids (Cyhalofop-butyl, Pyribenzoxim 및 Pyrazosulfuron-ethyl의 상호작용효과(相互作用效果) 및 상호작용(相互作用) 기작(機作)에 관(關)하여 - 제(第) 2 보(報) 혼합제초제(混合除草劑) 처리(處理)가 acetolactate synthase 활성(活性) 및 유리(遊離) 아미노산함량(含量)과 지방산함량(脂肪酸含量)에 미치는 영향(影響))

  • Wu, Ming-Gen;Kim, Kil-Ung;Shin, Dong-Hyun
    • Korean Journal of Weed Science
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    • v.18 no.3
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    • pp.197-204
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    • 1998
  • This study was conducted to determine the activity of ALS, content of endogenous free amino acids and fatty acids affected by herbicide mixture of cyhalofop-butyl, pyribenzoxim and pyrazosulfuron-ethyl. $I_{50}$ values (concentration required for 50% inhibition of ALS activity) of pyribenzoxim herbicide on the activity of ALS in Echinochloa crus-galli and Cyperus serotinus in vitro were recorded at 4${\times}$100 nM and 5${\times}$10 nM, respectively, while $I_{50}$ values of pyrazosulfuron against E crus-galli and C. serotinus were 4.5${\times}$10 nM and 4${\times}$10 nM, respectively, and the mixture of two herbicides showed additive effect on ALS activity at the low application rate, and independent effect at the high application rates of two herbicides. The inhibition rates of the three herbicides mixture treatment on the three branch-chain amino acids such as valine, leucine and isoleucine were 74.6%, 66.6% and 57.9% in C. serotinus and 36.6% 51.1% and 48.1% in E. crus-galli, respectively. A little bit higher inhibitory effect on the three branch-chain amino acids in C. serotinus and E. crus-galli seedlings was observed in two herbicide mixture of pyribenzoxim with pyrazosulfuron than three herbicide mixture of cyhalofop with pyribenzoxim and pyrazosulfuron. The interaction among three herbicides showed non-antagonism on the amounts of endogenous free amino acids.

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Whitening Efficacy Study of Natural Compounds-Peptide Derivatives via cAMP Signaling Pathway (cAMP 신호전달과정을 통한 신규 천연유래물질 펩타이드 유도체의 미백 효능 연구)

  • Lee, Hye-Suk;Shin, Kyong-Hoon;Ryu, Geun-Seok;Jee, Kyung-Yup;Cho, In-Shik;Kim, Han-Young
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.37 no.3
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    • pp.275-282
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    • 2011
  • Novel whitening agents were prepared using peptide-Natural origin compound derivatives. The peptide could be an antagonist of MC1R and Natural origin compound were well-known material as a Tyrosinase inhibitor. We also suggest the new assay method which could evaluate the Antagonistic effectiveness to MC1R using cAMP signaling pathway. 24 candidates were synthesized and 11 peptide derivatives were selected by cAMP assay method. To evaluate cAMP assay, the selected peptide derivatives were assayed to evaluate their melanogensis inhibitory activity. At this work, we could know that the sequences which include -RW- have a melanogensis inhibitory activity, and cAMP assy could use as a evaluating method of MC1R antagonist. But, to evaluate the whitening activity of some material, cross-checking with melanin inhibitory assay method was recommended.

Lysophosphatidic Acid Stimulates SKOV-3 Cell Migration through the Generation of Reactive Oxygen Species via the mTORC2/Akt1/NOX Signaling Axis (리소포스타티드산은 SKOV-3 난소암세포의 mTORC2/Akt1/NOX 신호전달 기전을 통해 활성산소를 형성하고 이를 통해 세포의 이동을 촉진)

  • Eun Kyoung Kim;Seo Yeon Jin;Jung Min Ha;Sun Sik Bae
    • Journal of Life Science
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    • v.33 no.2
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    • pp.129-137
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    • 2023
  • Reactive oxygen species (ROS) play an essential role in a variety of cellular physiological phenomena. The present study assessed the signaling axis that mediates the lysophosphatidic acid (LPA)-induced migration of SKOV-3 cells. Insulin-like growth factor-1 (IGF-1) stimulated SKOV-3 cell migration in a time- and dose-dependent manner. Similarly, LPA stimulated SKOV-3 cell migration and the phosphorylation of Akt in a time- and dose-dependent manner. The pharmacological inhibition of LPA receptors (LPA1/LPA3) significantly suppressed LPA-induced SKOV-3 cell migration. However, IGF-1-induced SKOV-3 cell migration was not affected by the inhibition of LPA1 and LPA3. Pharmacological inhibition of phosphoinositide 3-kinase (PI3K) or Rho-associated kinase (ROCK) significantly suppressed LPA-induced migration, whereas the inhibition of MAPK kinase (MEK) had no effect. Inhibition of PI3K or ROCK completely suppressed LPA-induced ROS generation, and suppression of nicotinamide adenine dinucleotide phosphate oxidase (NOX) or chelation of ROS by N-acetylcysteine (NAC) blocked LPA-induced SKOV-3 cell migration. LPA-induced ROS generation was suppressed by silencing Rictor or Akt1 but not Raptor or Akt2. Silencing Rictor or Akt1 significantly suppressed LPA-induced SKOV-3 cell migration, whereas silencing Raptor or Akt2 had no effect. Finally, the overexpression of the constitutively active form Akt1 (CA-Akt1) significantly enhanced the LPA-induced migration of SKOV-3 cells. Given these results, we suggest that LPA stimulates SKOV-3 cell migration by ROS generation, which is mediated by the mTORC2/Akt1/NOX signaling axis.

Physiological Effects of TOPE, a Photo - independent Diphenylether, on Higher Plants (비광요구형 디페닐에테르계 TOPE 의 생리적 작용에 관한 연구)

  • Kim, J.S.;Cho, K.Y.;Pyon, J.Y.
    • Korean Journal of Weed Science
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    • v.16 no.2
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    • pp.160-170
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    • 1996
  • Several physiological responses were investigated in plants treated with TOPE as a preliminary step to know its action site. Unlike photo-dependent diphenylethers, herbicidal activity of TOPE appeared slowly and its typical symptoms were both burning of leaf blades and abnormal division of meristem in grasses, Similarly, both leakage of cell electrolytes and the curling of cotyledon margin were also shown in cucumber(Cucumis sativus L.). Biosynthesis of chlorophyll in etiolated cucumber cotyledon was not inhibited directly by treatment of TOPE at low light intensity(5.5${\mu}$ mol $m^{-2}s^{-1}$ PAR) and protoporphyrin IX was not also accumulated. The contents of phytoene, phytofluene and ${\beta}$-carotene were abnormaly increased. Photosynthesis was inhibited only at high concentration. Mitochondrial respiration was inhibited at high concentration but rather increased significantly at 10${\mu}$M of TOPE. However, respiration inhibitors did not alleviate the two symptoms of TOPE in cucumber cotyledon. In the same experiments, using inhibitors of protein or nucleic acid biosynthesis, only one of the two symptoms was alleviated by chloramphenicol and cycloheximide. In contrast, both symptoms were alleviated by actinomycin-D and hydroxyurea, suggesting that nucleic acid metabolism might be preferentially related to the mode of action of TOPE. DNA, RNA and protein contents were accumulated in both cucumber cotyledon and rice (Oryza sativa L.) routs treated with TOPE, and the DNA of them was increased at first. Thus, it is conjectured that TOPE increase nucleic acid metabolism directly or indirectly, and then disturb various metabolic pathways causing abnormal physiological and morphological effects followed by final death.

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Purification and Characterization of Chitinase from Antagonistic Bacteria Pseudomonas sp. 3098. (생물방제균 Pseudomonas sp. 3098이 생산하는 Chitinase의 정제 및 특성)

  • 이종태;김동환;도재호;김상달
    • Microbiology and Biotechnology Letters
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    • v.26 no.6
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    • pp.515-522
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    • 1998
  • Plant root rotting fungi, Fusarium solani are suppressed their growth by the chitinase which is produced from the antagonistic soil bacteria. The chitinase producable antagonistic bacterium Pseudomonas sp. 3098 was selected as a powerful biocontrol agent of F. solani from ginseng rhizosphere. The antagonistic Pseudomonas sp. 3098 was able to produce a large amount of extracellular chitinase which is key enzyme in the decomposition of fusarial hypal walls. The chitinase was purified from cultural filtrate of Pseudomonas sp. 3098 by the procedure of ammonium sulfate precipitation, anion exchange chromatography, gel filtration on Bio-Gel P-100, and 1st and 2nd hydroxyapatite chromatography. The molecular mass of the purified enzyme was ca. 45 kDa on SDS-FAGE. The optimal pH and temperature for the activity of purified chitinase were 5.0 and 45$^{\circ}C$, respectively. The enzyme was stable in pH range of 5.0 to 9.0 up to 5$0^{\circ}C$ The enzyme was significantly inhibited by metal compounds such as FeCl$_2$, AgNO$_3$ and HgCl$_2$, and was slightly inhibited by p-CMB, iodoacetic acid, urea, 2,4-DNP and EDTA. The enzyme had ability of digestion on colloidal chitin and chitin from shrimp shell, but could not digest chitosan and chitin from crab shell. Km value of the enzyme was 0.11% on colloidal chitin, and the maximum hydrolysis rate of the enzyme was 34% on colloidal chitin.

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Activation of the M1 Muscarinic Acetylcholine Receptor Induces GluA2 Internalization in the Hippocampus (쥐 해마에서 M1 무스카린 아세틸콜린 수용체의 활성에 의한 GluA2 세포내이입 연구)

  • Ryu, Keun Oh;Seok, Heon
    • Journal of Life Science
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    • v.25 no.10
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    • pp.1103-1109
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    • 2015
  • Cholinergic innervation of the hippocampus is known to be correlated with learning and memory. The cholinergic agonist carbachol (CCh) modulate synaptic plasticity and produced long-term synaptic depression (LTD) in the hippocampus. However, the exact mechanisms by which the cholinergic system modifies synaptic functions in the hippocampus have yet to be determined. This study introduces an acetylcholine receptor-mediated LTD that requires internalization of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA) receptors on the postsynaptic surface and their intracellular mechanism in the hippocampus. In the present study, we showed that the application of the cholinergic agonist CCh reduced the surface expression of GluA2 on synapses and that this reduction was prevented by the M1 muscarinic acetylcholine receptor antagonist pirenzepine in primary hippocampal neurons. The interaction between GluA2 and the glutamate receptor-interacting protein 1 (GRIP1) was disrupted in a hippocampal slice from a rat upon CCh simulation. Under the same conditions, the binding of GluA2 to adaptin-α, a protein involved in clathrin-mediated endocytosis, was enhanced. The current data suggest that the activation of LTD, mediated by the acetylcholine receptor, requires the internalization of the GluA2 subunits of AMPA receptors and that this may be controlled by the disruption of GRIP1 in the PDZ ligand domain of GluA2. Therefore, we can hypothesize that one mechanism underlying the LTD mediated by the M1 mAChR is the internalization of the GluA2 AMPAR subunits from the plasma membrane in the hippocampal cholinergic system.

Suppression Effect of Gray Mold and Late Blight on Tomato Plants by Rhamnolipid B (Rhamnolipid B에 의한 토마토 잿빛곰팡이병과 역병의 억제효과)

  • Ahn, Ji-Ye;Park, Myung-Soo;Kim, Seul-Ki;Choi, Gyung-Ja;Jang, Kyoung-Soo;Choi, Yong-Ho;Choi, Jae-Eul;Kim, In-Seon;Kim, Jin-Cheol
    • Research in Plant Disease
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    • v.15 no.3
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    • pp.222-229
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    • 2009
  • A Pseudomonas strain SG3 producing biosurfactant and showing antifungal and insecticidal activities was isolated from agricultural soil severely contaminated with machine oils. The antagonistic bacterium inhibited mycelial growth of all of the tested fungal pathogens. The fermentation broth of SG3 also effectively suppressed the development of various plant diseases including rice blast, tomato gray mold, tomato late blight, wheat leaf rust, barley powdery mildew and red pepper anthracnose. An antifungal substance was isolated from the fermentation broth of SG3 by ethyl acetate partitioning, silica gel column chromatography and preparative HPLC under the guide of bioassay. The chemical structure of the antifungal substance was determined to be rhamnolipid B by mass and NMR spectral analyses. The antifungal biosurfactant showed a potent in vivo antifungal activity against gray mold and late blight on tomato plants. In addition, rhamnolipid B inhibited mycelial growth of B. cinerea causing tomato gray mold and zoospore germination and mycelial growth of P. infestans causing tomato late blight. Pseudomonas sp. SG3 producing rhamnolipid B could be used as a new biocontrol agent for the control of plant diseases occurring on tomato plants.