• Title/Summary/Keyword: 길항제

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The Roles of Excitatory Amino Acid System in the Organophosphate-induced Brain Damage (유기인제에 의한 뇌 손상에 있어서 흥분성 아미노산의 역할)

  • Ko, Bong-Woo;Park, Eun-Hae;Kim, Dong-Sik;Bang, Sung-Hyun;Jin, Joo-Yeon;Kim, Dae-Sung;Ju, Chang-Wan;Lee, Kyung-Kap;Cho, Moon-Jae;Kimcho, So-Mi;Lee, Bong-Hee;Riu, Key-Zung;Park, Min-Kyoung;Lee, Young-Jae
    • Applied Biological Chemistry
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    • v.44 no.3
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    • pp.148-152
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    • 2001
  • This study investigated the role of excitatory amino acid systems in the initiation of organophosphate-induced seizures and brain damages in rats through quantitative in vivo microdialysis. Microdialysates were collected from the hippocampus of rat brain, treated with diisopropylfluorophosphate (DFP; 2.67 mg/kg, s.c.) alone, and/or atropine sulfate (15 mg/kg, i.m.) and procyclidine (30 mg/kg, i.m.). The protective effects of atropine, a muscarinic blocker, and/or procyclidine, a N-methyl-D-aspartate and cholinergic antagonist, against DFP were examined. DFP treatment increased the levels of aspartate (Asp) and glutamate (Glu) significantly in the hippocampal persuate with the induction of seizures. Treatment of procyclidine could effectively block the increase of Asp and Glu levels. Atropine treatment showed no significant anticonvulsive effects against DFP-induced seizures. The increases of Asp and Glu levels by DFP were also completely blocked through the combined treatment of atropine and procyclidine. Histopathological findings on the hippocampus confirmed the above results. More effective protection was observed through the treatments of procyclidine alone or of both procyclidine and atropine than atropine alone against DFP-induced brain damage. Procyclidine was shown to be effective in DFP-induced seizures.

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Blockade of Thromboxane Influences Does Not Affect Renal Blood Flow Deficit in Anesthetized Diabetic Rats (마취된 당뇨 흰쥐의 신혈류량 감소에 관여하는 기전 : 내인성 쓰롬복산계의 무관성)

  • Ha, Hun-Joo;Dunham, Earl W.
    • The Korean Journal of Pharmacology
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    • v.24 no.2
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    • pp.221-232
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    • 1988
  • Studies were conducted to determine whether reduced renal blood flow (RBF) exhibited by rats with uncontrolled, streptozotocin (STZ)-induced diabetes is attributable to diabetes-associated, enhanced renal vasoconstrictor influence of endogenous thromboxane $(TX)A_2$. Rats which were injected with STZ after pretreatment with 3-O-methyl glucose (3OMG), an agent which prevents STZ-induced hyperglycemia, were also studied. Basal values of total RBF (RBF; ml $min^{-1}$ $gKw^{-1}$; electromagnetic flow probe), systemic arterial pressure (BP; mm Hg) and renal vascular resistance (RVR;BP $RBF^{-1})$in pentobarbital-anesthetized rats during a control period were $5.9{\pm}0.3$(P<0.1_{VS}. CR), $115{\pm}3$ and $20.3{\pm}1.0$(P<0.1_{VS}. CR) for STZR (n=15), and $8.4{\pm}0.4$, $123{\pm}3$ and $15.1{\pm}0.8$ for age-matched control rats (CR; n= 15), respectively. Basal values of RBF, BP and RVR in 3OMG pretreated STZR were identical to CR. In preparations shown capable of renal vasodilatation, OKY 1581 (1 mg/kg, i.v. followed by 0.4 mg/kg min infusion) abolished arachidonate-induced $(TX)A_2$ synthesis, but did not alter basal BP, RBF or RVR in either STZR or CR (n=4/group). Similarly, i.r.a. infusion of SQ29548 (100 ng/ml RBF) abolished renal vasoconstriction induced by a TX/prostaglandin endoperoxide mimic, U46619, but had no discern able affect on RVR in either STZR (n=8) or CR (n=8). The data indicates that $TXA_2$ does not participate in the elevated basal RVR of STZR which are associated with the diabetic state.

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Influence of Intracerebroventricular Yohimbine on the Renal Function of the Rabbit (가토 신장기능에 미치는 측뇌실내 Yohimbine의 영향)

  • Kook, Young-Johng;Kim, Kyung-Keun;Kim, Sei-Jong
    • The Korean Journal of Pharmacology
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    • v.21 no.2
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    • pp.119-127
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    • 1985
  • The renal function is under regulatory influence of the central nervous system, mainly through activation of sympathetic nerve to the kidney, and it was recently reported that clonidine, an agonist to ${\alpha}_2$-adrenoceptors, induces diuresis and natriuresis when injected directly into a lateral ventricle of the rabbit brain (i.c.v.). This study was undertaken, therefore, to obtain further information as to the role of the central ${\alpha}_2$-adrenoceptors in regulating renal function, by observing the effects of i.c.v. yohimbine, a specific antagonist of adrenoceptors of ${\alpha}_2$-type, on the rabbit renal function, and to elucidate the mechanism involved in it. With 10 ${\mu}g/kg$ i.c.v. of yohimbine sodium excretion transiently increased along with increasing tendency of urine flow, renal plasma flow and glomerular filtration rate. These responses decreased with increasing doses. With 100 and 300 ${\mu}g/kg$ i.c.v. marked antidiuresis and antinatriuresis as well as profound decreases of renal perfusion and glomerular filtration were noted. Systemic blood pressure transiently increased. In reserpinized rabbits, 100 ${\mu}g/kg$ yohimbine i.c.v. did not produce any significant changes in urine flow, sodium excretion as well as in renal hemodynamics. The pressor response was also abolished. In preparations in which one kidney was denervated and the other left intact as control, i.c.v. yohimbine elicited typical antidiuretic antinatriuretic response in the innervated control kidney, whereas the denervated experimental kidney responded with marked diuresis and increases in excretory rates of sodium and potassium and in osmolar clearance in spite of absence of increased filtration and perfusion . Systemic blood pressure responded as in the normal rabbits. These observations indicate that i.c.v. yohimbine affects renal function in dual ways in opposite directions, the first being the antidiuretic antinatriuretic effects which results from decreased renal perfusion and glomerular filtration due to sympathetic activation and which is predominantly expressed in the normal rabbits, and the second less apparent effect being the diuretic and natriuretic action which is not mediated by nerve pathway but brought about by some humoral mechanism and which is effected by decreased sodium reabsorption in the tubules, possibly of the proximal portion.

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Optimization of the cryopreserved condition for utilization of GPCR frozen cells (GPCR 냉동보관 세포의 활용을 위한 냉동조건의 최적화 연구)

  • Noh, Hyojin;Lee, Sunghou
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.16 no.2
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    • pp.1200-1206
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    • 2015
  • The major target for drug discovery, G-protein coupled receptor (GPCR) is involved in many physiological activities and related to various diseases and disorders. Among experimental techniques relating to the GPCR drug discovery process, various cell-based screening methods are influenced by cell conditions used in the overall process. Recently, the utilization of frozen cells is suggested in terms of reducing data variation and cost-effectiveness. The aim of this study is to evaluate various conditions in cell freezing such as temperature conditions and storage terms. The stable cell lines for calcium sensing receptor and urotensin receptor were established followed by storing cultured cells at $-80^{\circ}C$ up to 4 weeks. To compare with cell stored at liquid nitrogen, agonist and antagonist responses were recorded based on the luminescence detection by the calcium induced photoprotein activation. Cell signals were reduced as the storage period was increased without the changes in $EC_{50}$ and $IC_{50}$ values $EC_{50}:3.46{\pm}1.36mM$, $IC_{50}:0.49{\pm}0.15{\mu}M$). In case of cells stored in liquid nitrogen, cell responses were decreased comparing to those in live cells, however changes by storage periods and significant variations of $EC_{50}/IC_{50}$ values were not detected. The decrease of cell signals in various frozen cells may be due to the increase of cell damages. From these results, the best way for a long-term cryopreservation is the use of liquid nitrogen condition, and for the purpose of short-term storage within a month, $-80^{\circ}C$ storage condition can be possible to adopt. As a conclusion, the active implementation of frozen cells may contribute to decrease variations of experimental data during the initial cell-based screening process.

Sphingosine-1-Phosphate-Induced Migration and Differentiation of Human Mesenchymal Stem Cells to Smooth Muscle Cells (Sphingosine-1-phosphate에 의한 중간엽 줄기세포의 이동과 평활근세포로의 분화)

  • Song, Hae-Young;Shin, Sang-Hun;Kim, Min-Young;Kim, Jae-Ho
    • Journal of Life Science
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    • v.21 no.2
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    • pp.183-193
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    • 2011
  • Migration and differentiation of mesenchymal stem cells are crucial for tissue regeneration in response to injury. Sphingosine-1-phosphate (S1P) is a bioactive lipid that regulates a variety of biological processes, including proliferation, survival, differentiation and motility. In the present study, we determined the role of S1P in migration and differentiation of human bone marrow-derived mesenchymal stem cells (BMSCs). S1P stimulated migration of BMSCs in a dose- and time-dependent manner, and pre-incubation of the cells with pertussis toxin completely abrogated S1P-induced migration, suggesting involvement of Gi-coupled receptors in S1P-induced cell migration. S1P elicited elevation of intracellular concentration of $Ca^{2+}$ ($[Ca^{2+}]_i$) and pretreatment with VPC23019, an antagonist of $S1P_1/S1P_3$, blocked S1P-induced migration and increase of $[Ca^{2+}]_i$. Small interfering RNA-mediated knockdown of endogenous $S1P_1$ attenuated S1P-induced migration of BMSCs. Furthermore, S1P treatment induced expression of $\alpha$-smooth muscle actin ($\alpha$-SMA), a smooth muscle marker, and pretreatment with VPC23019 abrogated S1P-induced $\alpha$-SMA expression. S1P induced phosphorylation of p38 mitogen-activated protein kinase (MAPK), and pretreatment of cells with SB202190, an inhibitor of p38 MAPK, or adenoviral overexpression of a dominant-negative mutant of the p38 MAPK blocked S1P-induced cell migration and $\alpha$-SMA expression. Taken together, these results suggest that S1P stimulates migration and smooth muscle differentiation of BMSCs through an $S1P_1$-p38 MAPK-dependent mechanism.

Effect of Ginseng Saponins on the Biosynthesis of Prostaglandins (인삼 사포닌 성분이 프로스타글란딘류 생성에 미치는 영향)

  • 이선희;박찬웅
    • Journal of Ginseng Research
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    • v.13 no.2
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    • pp.202-210
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    • 1989
  • The effects of Ginseng saponins on the in vitro biosynthesis of prostaglandins were examined in order to identify the role of some Ginseng components on the regulation of arachidonic arid metabolism. The productions of prostaglandin $E_2$ (PG$E_2$), $F_2$ (PGF2), thromboxane $B_2$(TX$B_2$) and 6-ketoprostaglandin Fl (6-Keto-PGF1) from [3Hl-arachidonic acid were evaluatpf by radiochromatographic analysis with rabbit kidney microtome, human platelet homogenate and bovine aortic microsome. The amounts of the total prostaglandins produced by cyclooxygenase activity and malondialdehyde from arachidonic acid didn't show significant changes in the presence of Ginseng saponins. Both of panaxadiol and panaxatriol didn't affect the production of PG$E_2$ while the formations of PG$F_2$( and TX$B_2$( were nearkedly reduced and the production of prostacyclin was increased. The formation of TXBE was reduced by ginsenoside $Rb_2$, Rc, and Re, however the production of 6-Keto-PGF1 was increased dose dependently up to 1 mg/ml. Moreover, platelet aggregations induced by arachidonic acid and U46619 (9.11-methanepoxy PG$H_2$), TX$A_2$ mimetics, were also inhibited by three ginsenosides. The effect of G-Re on prostacyclin synthetase was inhibited by tranylcypromine, prostacyclin synthetase inhibitor. These results suggest that Ginseng saponins may not directly act on cyclooxygenase but affect on the divergent pathway from endoperoxide.

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A Study on Establishment of Quality Management System (ISO 9001 : 2000/ KS A9001 : 2001) based on ERP (ERP 기반의 품질경영시스템(ISO 9001 : 2000/ KS A 9001:2001) 구축에 관한 연구)

  • 김용직;강창욱
    • Proceedings of the Society of Korea Industrial and System Engineering Conference
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    • 2002.05a
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    • pp.413-419
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    • 2002
  • 본 연구의 목적은 품질경영시스템의 ISO 9000:2000/KS A 9000:2001 개정 규격 내용 및 요구사항을 살펴보는 한편, 우리나라 중소기업이 전환규격을 적용하는데 있어서 ERP PACKAGE를 이용하여 효과적인 품질경영시스템 구축 방안을 제시하기 위함이다. 본 연구에서는 업무 PROCESS와 품질 기록을 중심으로 ISO 9000:2000/KS A 9000:2001 개정 규격을 ERP PACKAGE에 접목하는 방법을 도출하였으며, 적용 사례로서 기계 제조업체의 구매업무를 중심으로 품질경영시스템 구축방안을 제시하였다. 본 연구의 결과는 다음과 같다. 첫째, 정형화된 업무 체계를 갖추어 업무 담당자간 혹은 부서간의 업무 마찰을 줄이고 여러부서에서 발생하는 업부 DATA를 중앙집중식으로 공유하여 동일한 DATA의 수집과 작성에 중복성을 최소화하는 등에서 업무의 효과가 있는 것을 볼 수 있다. 둘째, ERP PACKAGE를 이용한 품질경영시스템(ISO 9000:2000/KS A 9000:2001)의 효과적인 추진 방안은 다음과 같다 1) 전환 규격의 충분한 이해가 요구된다. 2) 현재의 업무 프로세스를 파악한 후 ERP PACKAGE에서 제공하는 개선된 업무프로세스를 적용하는 것이 필요하다. 3) 개선된 업무 프로세스의 실행 결과를 ERP PACKAGE 모듈에서 품질기록으로 유지한다. 4) 새로운 품질경영 정보 시스템을 업무 전반에 적용하기 위한 기업인프라 구축과 프로세스에 대한 지속적인 개선이 요구된다. 본 연구에서는 ISO 9000:2000/KS A 9000:2001 개정 규격요구사항을 이해하고 ERP PACKAGE를 이용하여 최초로 개정규격을 적용하거나, 전환규격으로 품질경영시스템을 구축 시 좀더 효과적이고 효율적인 품질경영시스템을 구축하는데 업무지침으로 활용될 수 있을 것이다.의 수와 생존율면에서 볼 때 가장 적합한 것으로 사료되었다./TEX>개월 투여하게 되면 HDL 콜레스테롤 양이 현저히 증가하였으며, 총 콜레스테롤 양, 동맥경화지표, 중성지방, 유리지방산, 과산화지방은 현 저히 감소하였다.- 결론 - 홍삼과 진세노사이드는 사람과 흰쥐에 있어 과지혈증을 호전시켰다. 실험적으로 과지혈증을 유발시킨 흰쥐에서, 혈중 아포단백질, 지방단백질 및 프로스타글란딘 상호성을 개선시켰다.었다.xA_{2}$ synthetase 억제제인 imidazole의 효과와 유사하였다. 4. G-Re는 $1{\times}10^{-5}g/ml$ 이하의 농도에서는 효과가 없으나 $1{\times}10^{-4}g/ml$ 이상의 농도에서 농도의존적으로 유의성 있는 $PGE_{2},\;PGF_{2}{\alpha},\;TXB_{2}$의 생성억제와 함께 6-keto-$PGF_{1}{\alpha}$ 증가를 보였다. 이는 prostacyclin synthetase를 자극하는 serotonin의 효과와 같은 작용으로서 prostacyclin synthetase 억제제인 tranylcypromine에 대하여 길항효과를 보였다. 5. $TxB_{2}$생성억제 작용을 나타내는 ginsenoside들의 효과를 뒷받침하기 위하여 인삼 saponin 성분을 전처치한 patelet rich plasma에서 혈소판 응집시험 결과, ADP로 유도된 혈소판 응집반응에는 모든 인삼 saponin 성분들이 효과가 없었으나 arachidonic acid로 유도된 혈소판 응집반응에는 $G-Rb_{2}$, G-Rc, G-Re의 순으로 농도 의존적인 억제현상을 보였다. 이상의 결과와 같이 인삼 saponin 성분들은

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Interaction Effects between Glyphosate and Some Other Herbicides on Cutgrass, Leersia oryzoides SW (겨풀(Leersia oryzoides SW.)에 대한 Glyphosate와 수종(數種) 제초제간(除草劑間)의상호작용(相互作用) 효과(效果))

  • Yim, I.B.;Guh, J.O.;Lee, K.H.
    • Korean Journal of Weed Science
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    • v.7 no.3
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    • pp.329-336
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    • 1987
  • Antagonistic interaction between glyphosate and some herbicides in effects of post-emergence application on cut grass and of pre-emergence application on some weed species including barnyardgrass was evaluated with pots in plastic house. By addition of oxyfluorfen to glyphosate, the weeding efficacy on cutgrass was visually evaluated as promotive in both weeding rate and efficacy. However, by alachlor, simazine, gluphosinate or quizalofop-ethyl showed delayed weeding rate, and by paraquat, the promotive in rate but lower in efficacy, respectively. Fresh weights of cutgrass at 30 days after the lower-rate application has generally indicated the lower weeding efficacy than that from glyphosate alone. Even at higher rate application, the addition of alachlor or simazine to glyphosate has still indicated the lower efficacies. As a result of interaction analysis by Colby method, no synergism was detected from any treatments, and the combinations of simazine or paraquat to glyphosate in lower mixing rate showed significant antagonism at 5% probability level of DMRT. On the annual weed species including barnyardgrass, the significant soil-residual weeding efficacies were recognized by addition of any rate of oxyfluorfen, alachlor, simazine and higher rate of quizalofop-ethyl to glyphosate, respectively.

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Control of Red Pepper Anthracnose Using Bacillus subtilis YGB36, a Plant Growth Promoting Rhizobacterium (식물생장촉진근권세균 Bacillus subtilis YGB36을 이용한 고추 탄저병의 생물학적 방제)

  • Lee, Yong Yoon;Lee, Younmi;Kim, Young Soo;Kim, Hyun Sup;Jeon, Yongho
    • Research in Plant Disease
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    • v.26 no.1
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    • pp.8-18
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    • 2020
  • Red pepper, one of the major economic crops in Korea, is being affected by anthracnose disease caused by Colletotrichum acutatum. To control this disease, an antagonistic bacterial strain, Bacillus subtilis YGB36 identified by 16S rDNA sequencing, physiological and biochemical analyses is used as a biological control agent. In vitro screening revealed that the strain YGB36 possess strong antifungal activity against the pathogen Cylindrocarpon destructans. The strain exhibited cellulase, protease, amylase, siderophore production and phosphate solubility. In vitro conidial germination of C. acutatum was most drastically inhibited by YGB36 cell suspensions (106 cfu/ml) or culture filtrate. Development of anthracnose symptoms was reduced on detached immature green pepper fruits by treatment with cell suspensions, and its control value was recorded as 65.7%. The YGB36 bacterial suspension treatment enhanced the germination rate of red pepper seeds and promoted root development and growth under greenhouse conditions. The in vitro screening of fungicide and insecticide sensitivity test against YGB36 revealed that the bacterial growth was not affected by any of the insecticides, and 11 fungicides out of 21 used. Collectively, our results clearly suggest that the strain YGB36 is considered as one of the potential biocontrol agents against anthracnose disease in red pepper.

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.