• Title/Summary/Keyword: Agonistic

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Agonistic Activities to the Benzodiazepine Receptor by Extracts of Medicinal Plants(I) -Screening of Some Sedative Plant Extracts- (생약의 Benzodiazepine 수용체 효현활성 검색(I) -수종의 신경안정 생약 추출물에 대한 활성 검색-)

  • Ha, Jeoung-Hee;Park, Yong-Ki;Kang, Byung-Soo;Lee, Dong-Ung
    • Korean Journal of Pharmacognosy
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    • v.30 no.2
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    • pp.211-215
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    • 1999
  • This study was aimed to evaluate an agonistic activity to benzodiazepine receptor of several medicinal plants, which have been used as sedatives in oriental medicine. Methanol extracts of medicinal plants which were used in this study inhibited the binding of $[^3H]Ro15-1788$, a selective benzodiazepine receptor antagonist to benzodiazepine receptor of rat cortices. Inhibitory activity of Cyperus rotundus was observed to be the highest among the tested medicinal plants. Methanol extracts of Cyperus rotundus and Zizypus jujuba inhibited a $[^3H]flunitrazepam$, a selective benzodiazepine receptor agonist, binding to benzodiazepine receptor. GABA significantly enhanced the inhibition of $[3H]flunitrazepam$ binding by Cyperus rotundus and Zizypus jujuba, and these positive GABA shifts supported the strong possibility of agonistic activity to benzodiazepine receptor. From these results, it may be concluded that the substance or substances with neurochemical properties characteristic of a benzodiazepine receptor agonist may be important components and contribute to the sedative property of these medicinal plants.

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Lymphotoxin β Receptor Stimulation Is Linked to MLCK Activity and Suppresses Stress Fiber Formation in Agonistic Anti-LTβR Antibody-stimulated Fibroblastic Reticular Cells (FRC에서 agonistic anti-LTβR antibody의 LTβR 자극은 MLCK 연관성 및 stress fiber 형성에 대한 강력한 억제 작용)

  • Kim, Min Hwan;Lee, Jong-Hwan
    • Journal of Life Science
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    • v.27 no.10
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    • pp.1199-1206
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    • 2017
  • The lymphotoxin ${\beta}$ receptor ($LT{\beta}R$), a member of the tumor necrosis factor receptor family, plays an important role in lymphoid tissue's architecture and organogenesis. We found that $LT{\beta}R$ stimulation induced changes in stress fibers (SFs) in fibroblastic reticular cells (FRCs). MLCK and ROCK play critical roles in the regulation of SF formation in cells. The present study was performed to investigate the antifibrotic effects on SF regulation of $LT{\beta}R$ signaling, with a focus on MLCK inhibition. The effect of $LT{\beta}R$ on the SF change was analyzed using immunoblot and fluorescence assays and agonistic $anti-LT{\beta}R$ antibody-treated FRCs. In addition, we checked the level of Rho-guanosine diphosphate (GDP)/guanosine triphosphate (GTP) exchange activity with FRC lysate. Phospho-ezrin proteins acting as membrane-cytoskeleton linkers completely de-phosphorylated in agonistic $anti-LT{\beta}R$ antibody-treated FRCs. The actin bundles rearranged into SFs, where phospho-myosin light chain (p-MLC) co-localized in FRCs. ML7-treated FRCs completely blocked SFs and showed retraction and shrinkage processes comparable to those observed in agonistic $anti-LT{\beta}R$ antibody-treated cells. Inhibition of ROCK activity induced changes in the actin cytoskeleton organization; however, some SFs remained in the cells, while they were completely disrupted by MLCK inhibition with ML7. We showed that the phosphorylation of MLC was completely abolished with $LT{\beta}R$ stimulation in FRCs. When $LT{\beta}R$ was stimulated with the agonistic $anti-LT{\beta}R$ antibody, the Rho-GDP/GTP exchange activity was reduced, however, the activity was not completely abolished. Collectively, the results illustrated that MLCK was potently responsible for the SF regulation triggered via $LT{\beta}R$ signaling in FRCs.

Implementation of NPC Artificial Intelligence Using Agonistic Behavior of Animals (동물의 세력 투쟁 행동을 이용한 게임 인공 지능 구현)

  • Lee, MyounJae
    • Journal of Digital Convergence
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    • v.12 no.1
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    • pp.555-561
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    • 2014
  • Artificial intelligence in the game is mainly used to determine patterns of behavior of NPC (Non Player Character) and the enemy, path finding. These artificial intelligence is implemented by FSM (Finite State Machine) or Flocking method. The number of NPC behavior in FSM method is limited by the number of FSM states. If the number of states is too small, then NPC player can know the behavior patterns easily. On the other hand, too many implementation cases make it complicated. The NPC behaviors in Flocking method are determined by the leader's decision. Therefore, players can know easily direction of movement patterns or attack pattern of NPCs. To overcome these problem, this paper proposes agonistic behaviors(attacks, threats, showing courtesy, avoidance, submission)in animals to apply for the NPC, and implements agonistic behaviors using Unity3D engine. This paper can help developing a real sense of the NPC artificial intelligence.

Cell Survival, Apoptosis and AMPK-COX-2 Signaling Pathway of Mammary Tumor Cells after Genistein Treatment Combined with Estrogen

  • Lee, Yun-Kyoung;Hwang, Jin-Taek;Kim, Young-Min;Park, Ock-Jin
    • Preventive Nutrition and Food Science
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    • v.12 no.4
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    • pp.197-201
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    • 2007
  • Genistein is an active component of legumes and other related food shown to be associated with prevention of degenerative diseases such as cancer through inducing signaling pathways. Treatment of genistein resulted in the induction of apoptosis in the cultured cancer cells. This induction of apoptosis was demonstrated by the Tunel assay in these cells. Unveiling the potential of genistein in cytotoxicity via apoptosis when it is treated with estrogen can predict the therapeutic capability of genistein in breast cancers in the presence of endogenous estrogen. We have found that apoptosis induced by genistein treatment in the presence of estrogen is agonistic or antagonistic depending on the concentrations and treatment periods applied in MCF-7 breast cancer cells. For the suppression of cell survival, 24 hr of treatment was required to induce a synergistic agonistic response between estrogen and genistein at low concentrations of genistein. After this period, the agonistic pattern of genistein to estrogen disappeared. The decrement of COX-2 expression in MCF-7 cells treated with genistein was accompanied with the activation of AMPK only at a high concentration of genistein. This association between AMPK activation and down-regulation of COX-2 by genistein was dampened in the presence of estrogen. It was also demonstrated that genistein and estrogen regulate cell survival and apoptosis by modulating p53 and caspase-3 in the opposite direction. These results suggest that genistein has the potential to control breast cancer development, and co-treatment with estrogen can cause agonistic or antagonistic action on breast cancer cell control.

The Anti-tumor Activity of Vitamin C via the Increase of Fas (CD95) and MHC I expression on Human Stomach Cancer Cell Line, SNU1

  • Yu, Yeon-Sil;Bae, Se-Yeon;Kim, Hye-Min;Kim, Ye-Jin;Chu, Nag-Bum;Chu, Nag-Kyun;Kang, Jae-Seung;Lee, Wang-Jae
    • IMMUNE NETWORK
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    • v.11 no.4
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    • pp.210-215
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    • 2011
  • It is already known that high concentration of vitamin C induces apoptosis on tumor cells. However, there is no report regarding the function of vitamin C on the modulation of immune susceptibility of cancer. Therefore, we investigated whether vitamin C can modulate immune susceptibility of tumor cells, especially on the induction of Fas-mediated apoptosis. First, the optimal concentration of vitamin C, which cannot induce damages on tumor cells for 36 hrs. We found that 2 mM of vitamin C did not show harmful effect. In addition, the optimal concentration of agonistic anti-Fas Abs for 18 hrs was examined. As a result, 400 ng/ml of agonistic anti-Fas Abs did not induce apoptosis on tumor cells. Next, we tried to find the effect of 2 mM of vitamin C on the modulation of the susceptibility to agonistic anti-Fas Abs. When tumor cells were cultured with 400 ng/ml of agonistic anti-Fas Abs for 18 hrs, after pre-treatment with 2 mM of vitamin C for 24 hrs, viability of cells was decreased. Interestingly, we found that the expression of Fas (CD95) and MHC class I was increased by the treatment of vitamin C. Taken together, vitamin C increases the susceptibility of tumor cells to anti-Fas Abs and the expression of Fas (CD95) and MHC class I on tumor cells.

Physiological Fuzzy Neural Networks for Image Recognition (영상 인식을 위한 생리학적 퍼지 신경망)

  • Kim, Kwang-Baek;Moon, Yong-Eun;Park, Choong-Shik
    • Journal of Intelligence and Information Systems
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    • v.11 no.2
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    • pp.81-103
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    • 2005
  • The Neuron structure in a nervous system consists of inhibitory neurons and excitory neurons. Both neurons are activated by agonistic neurons and inactivated by antagonist neurons. In this paper, we proposed a physiological fuzzy neural network by analyzing the physiological neuron structure in the nervous system. The proposed structure selectively activates the neurons which go through a state of excitement caused by agonistic neurons and also transmit the signal of these neurons to the output layers. The proposed physiological fuzzy neural networks based on the nervous system consists of a input player, and the hidden layer which classifies features of learning data, and output layer. The proposed fuzzy neural network is applied to recognize bronchial squamous cell carcinoma images and car plate images. The result of the experiments shows that the learning time, the convergence, and the recognition rate of the proposed physiological fuzzy neural networks outperform the conventional neural networks.

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Psychotropic Effects of Ginseng Saponine on Agonistic Behavior in Male and Female Mice

  • Yoshimura, Hiroyuki
    • Proceedings of the Ginseng society Conference
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    • 1987.06a
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    • pp.59-66
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    • 1987
  • Psychotropic actions of crude ginseng saponins(CGS), pure ginsenoslue Rbl(GS-bl) and gin- senoside Rgl(GS-gl) isolated from the root of Panax ginseng, were evaluated by determining their effects on agonistic behavior in male(Experiment 1) and female(Experiment 2) mice, using a biologically relevant method. The results of experiment 1 demonstrated that CGS and GS-bl significantly suppressed aggressive episodes (offensive sideways posture and attack bite) in a dose-dependent manner when the resident was drugged, whereas G5-gl was ineffective. However, when the intruder was treated with one of three ginseng saponins, agonistic behavior between resident and intruder males was not altered. In experiment 2, acute administration of CGS and G5-bl significantly suppressed maternal aggression, whereas GS-gl was ineffective. As compared with the vehicle-treated group, chronic treatment with CGS and GS-bl significantly suppressed maternal aggression, while GS-gl showed a tendency to increase the frequency of attack bite by females. These findings clearly indicate that the root of Panax ginseng contains psychoactive ingredient, which can suppress both intermale and maternal aggression in mice. We suggest that the present results have important implications for the clinical usefulness of ginseng saponins in psychiatric medicine.

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Agonistic Activities to the Benzodiazepine Receptor by Extracts of Medicinal Plants(II). -Activities of component and Active Fraction from Gastrodia elata- (생약의 Benzodiazepine 수용체 효능활성 검색 (II). -천마성분 및 유효분획의 활성-)

  • Ha, Jeoung-Hee;Yong, Chul-Soon;Kim, Jung-Ae;Huh, Keun;Lee, Dong-Ung
    • Korean Journal of Pharmacognosy
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    • v.30 no.3
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    • pp.284-289
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    • 1999
  • In order to find active ingradients having an agonistic activity to benzodiazepine receptor from Gastrodia elata Blume (Orchidaceae) which has been used as an anticonvulsant in oriental medicine, one component and some fractions were separated from the butanol extract of the rhizomes of this plant and evaluated for their activities on GABA/benzodiazepine receptor in vitro. As a result, one crude mixture (F4f) obtained from the most active fraction (F4) inhibited significantly the binding of $[^3H]Ro15-1788$, a selective benzodiazepine receptor antagonist, to benzodiazepine receptor of rat cortices. GABA significantly enhanced the inhibition of $[^3H]flunitrazepam$ binding by F4f, and this positive GABA shift supported the strong possibility of the agonistic activity of F4f to benzodiazepine receptor.

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Effects of Weaning Days on Feeding Performance and Behaviour of Piglets (자돈의 이유일령이 이유자돈의 육성성적 및 행동에 미치는 영향)

  • 이용준;송영한
    • Journal of Animal Environmental Science
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    • v.6 no.2
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    • pp.97-104
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    • 2000
  • This study was carried out to determine the effects of different weaning age on feeding performance and behaviour of piglets. Sixty crossbred(YLxD) litters of piglets were randomly alloted to be 15 pens with 4 piglets per pen and 5 pens per treatment by weaned at 14, 21, and 28 days. Pens were video-taped for 24 hours immediately at 7 weeks and 8 weeks of age. The piglets weaned at 14 and 21 days were significantly (P<0.05) much intake than piglets weaning at 28 days. The piglets weaning at 14 days were significantly lighter than piglets weaning at 14 and 21 days fro m2 weeks to 8 weeks age. However, feed conversion ration was significantly(P<0.05) improved according to late weaning days. Times spent engaged in Feeding, lying and walking were similar in piglets across weaning age. They also showed similar occurrence of drinking and agonistic behaviour at 7 weeks and 8 weeks of age. Piglets weaned at 14 days exhibited more belly-nosing behaviour at 7 weeks of age, but similar in piglets at 8 weeks of age across weaning age. We concluded that piglets performance influenced by weaning day, however time spent for feeding, lying and walking behaviour were no significance. Drinking, Agonistic and belly-nosing were not significantly different by weaning age.

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Agonistic Activities to the Benzodiazepine Receptor by Extracts of Medicinal Plants(III) Activities of Composite Druge and Component Fractions (생약의 Benzodiazepine 수용체 효능활성 검색(III) 생약복합제제 추출물 및 성분분획의 활성)

  • 이동웅;하정희;강병수;이갑득
    • Journal of Life Science
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    • v.10 no.4
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    • pp.374-379
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    • 2000
  • This study was attempted to evaluate an agonistic activity to benzodiazepine receptor of several medicinal pants, which have been used as sedatives in oriental medicine. The activities of the methanol extracts of composite preparation of oriental drugs were compared with those of the simple drugs, furthermore, the active fraction was found out from the simple preparation. Inhibitory effects of composite preparations, Cyperus rotundus/Acorus gramineus, Thuja orientalis/Euphoria longan, Thuja orientalis/Albizzia julibrissin, on the binding of ${[^3H]}$Ro15-1788, a selective benszodiazepine receptor antagonist to benzodiazepine receptor of rat cortices, were observed to be lower than those of corresponding simple preparations. These unexpected results suggest that some components of the composite druge may rather act as an obstacle, not to show the sinergistic effect. The methanol extracts of Cyperus rotundus having the highest activity were fractionated using polar and nonpolar solvents to give ethylacetate and hexane fractions, respectively. The ethylacetate fraction containing relatively polar components exhibited much higher activity than the hexane fraction, which consiste of nonpolar agonist, binding to benzodiazepine receptor. However, in the presence of GABA, this fraction inhibited ${[^3H]}$flunitrazepan binding, and these positive GABA shift supported the strong possibility of agonistic activity to benzodiazepine receptro. As a result, it may be concluded that the substance or substances with neurochemical properties as a benzodiazepine receptor agonist may contribute to the sedative property of Cyperus rotundus.

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