• 제목/요약/키워드: Agonistic

검색결과 91건 처리시간 0.031초

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

  • 하정희;박용기;강병수;이동웅
    • 생약학회지
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    • 제30권2호
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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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FRC에서 agonistic anti-LTβR antibody의 LTβR 자극은 MLCK 연관성 및 stress fiber 형성에 대한 강력한 억제 작용 (Lymphotoxin β Receptor Stimulation Is Linked to MLCK Activity and Suppresses Stress Fiber Formation in Agonistic Anti-LTβR Antibody-stimulated Fibroblastic Reticular Cells)

  • 김민환;이종환
    • 생명과학회지
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    • 제27권10호
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    • pp.1199-1206
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    • 2017
  • 종양괴사인자 수용체 일종인 Lymphotoxin ${\beta}$ receptor ($LT{\beta}R$)은 림프 구조와 기관 형성에 중요한 역학을 한다. 우리는 fibroblastic reticular cell (FRC)에서 agonistic $anti-LT{\beta}R$ antibody로 $LT{\beta}R$을 자극하면 stress fiber (SF)에 변화가 생긴다는 것을 알았다. MLCK와 ROCK는 세포에서 SF 형성 기여에 중요한 역할을 한다. 본 연구는 MLCK 저해에 초점을 맞추어 $LT{\beta}R$ 신호 전달은 SF 조절로 항섬유화 효과에 대하여 조사하였다. SF 변화에 대한 $LT{\beta}R$의 기능 조사를 위해 agonistic $anti-LT{\beta}R$ antibody로 처리된 FRC와 세포 추출물을 이용하여 immunoblot, fluorescence assay와 Rho-guanosine diphosphate (GDP)/guanosine triphosphate (GTP) exchange 활성 분석법으로 분석하였다. 세포막과 세포골격 연결자 ezrin은 agonistic $anti-LT{\beta}R$ antibody 처리된 FRC에서 완전히 탈인사화가 유도되었다. Actomysoisn에 의한 SF를 확인하였고 인산화 myosin light chain (p-MLC)인 함께 co-localization 되는 것도 확인하였다. ML7 처리된 FRC에서 agonistic $anti-LT{\beta}R$ antibody 처리된 세포에서 관찰되는 유사한 현상인 SF분해, 세포막 응축과 쇠퇴 현상이 나타났다. ROCK 활성저해는 액틴 골격 변화는 유도하였으나 부분적으로 SF가 세포에 남아 있었다. 반면, ML7에 의한 MLCK저해는 SF를 완전히 분해하였다. 또한, $LT{\beta}R$ 자극은 MLC 인산화를 완전히 억제하였지만, Rho-GDP/GTP exchange 활성변화에서는 감소는 되었으나 활성이 완전히 없어지지는 않았다. 결론적으로 이런 결과들은 FRC에서 $LT{\beta}R$신호전달을 통해 유도되는 SF 조절에는 MLCK가 보다 더 강력한 역할을 한다는 것을 제시하고 있다.

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

  • 이면재
    • 디지털융복합연구
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    • 제12권1호
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    • pp.555-561
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    • 2014
  • 게임에서 인공 지능은 주로 NPC(Non Player Character)와 적의 행동 패턴을 결정하거나 길 찾기에 사용된다. 이러한 인공 지능을 구현하는 경우에 FSM(Finite State Machine)과 플로킹(Flocking) 방법이 사용된다. FSM 방법에서는 상태 개수에 따라 NPC의 행동 개수에도 제한을 받는다. 상태 개수가 너무 적은 경우 플레이어들이 쉽게 NPC의 행동 패턴을 알 수 있으며 너무 많은 경우에는 구현이 복잡하게 된다. Flocking 방법에서는 리더의 결정에 따라 NPC들의 행동이 결정되기 때문에 NPC들의 이동 패턴이나 공격 방향을 쉽게 플레이어들이 알 수 있다. 본 논문에서는 이 문제를 개선하기 위하여 동물의 세력 투쟁 행동(공격, 위협, 의례적인 보여줌, 기피, 복종)들을 NPC에 적용하는 것을 제안하고 이를 Unity3D 엔진을 이용하여 구현한다. 이 논문은 실제감 있는 NPC 인공 지능 제작에 도움을 줄 수 있다.

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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    • 제12권4호
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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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    • 제11권4호
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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.

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

  • 김광백;문용은;박충식
    • 지능정보연구
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    • 제11권2호
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    • pp.81-103
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    • 2005
  • 신경계의 뉴런 구조는 흥분 뉴런과 억제 뉴런으로 구성되며 각각의 흥분 뉴런과 억제 뉴런은 주동근 뉴런(agonistic neuron)에 의해 활성화되며 길항근 뉴런(antagonist neuron)에 의해 비활성화 된다. 본 논문에서는 인간 신경계의 생리학적 뉴런 구조를 분석하여 퍼지 논리를 이용한 생리학적 퍼지 신경망을 제안한다. 제안된 구조는 주동근 뉴런에 의해 흥분 뉴런이 될 수 있는 뉴런들을 선택하여 흥분시켜 출력층으로 전달하고 나머지 뉴런들을 억제시켜 출력층에 전달시키지 않는다. 신경계를 기반으로 한 제안된 생리학적 퍼지 신경망의 학습구조는 입력층, 학습 데이터의 특징을 분류하는 중간층, 그리고 출력 층으로 구성된다. 제안된 퍼지 신경망의 학습 및 인식 성능을 평가하기 위해 정확성이 요구되는 의학의 한 분야인 기관지 편평암 영상 인식과 영상 인식의 주요 응용 분야인 차량번호판 인식에 적용하여 기존의 신경망과 성능을 비교 분석하였다. 실험 결과에서는 제안된 생리학적 퍼지 신경망이 기존의 신경망보다 학습 시간과 수렴성이 개선되었을 뿐만 아니라, 인식에 있어서도 우수한 성능이 있음을 확인하였다.

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

  • Yoshimura, Hiroyuki
    • 고려인삼학회:학술대회논문집
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    • 고려인삼학회 1987년도 Proceedings of Korea-Japan Panax Ginseng Symposium 1987 Seoul Korea
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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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생약의 Benzodiazepine 수용체 효능활성 검색 (II). -천마성분 및 유효분획의 활성- (Agonistic Activities to the Benzodiazepine Receptor by Extracts of Medicinal Plants(II). -Activities of component and Active Fraction from Gastrodia elata-)

  • 하정희;용철순;김정애;허근;이동웅
    • 생약학회지
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    • 제30권3호
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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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자돈의 이유일령이 이유자돈의 육성성적 및 행동에 미치는 영향 (Effects of Weaning Days on Feeding Performance and Behaviour of Piglets)

  • 이용준;송영한
    • 한국축산시설환경학회지
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    • 제6권2호
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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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생약의 Benzodiazepine 수용체 효능활성 검색(III) 생약복합제제 추출물 및 성분분획의 활성 (Agonistic Activities to the Benzodiazepine Receptor by Extracts of Medicinal Plants(III) Activities of Composite Druge and Component Fractions)

  • 이동웅;하정희;강병수;이갑득
    • 생명과학회지
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    • 제10권4호
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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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