• 제목/요약/키워드: $LTD_4$ antagonists

검색결과 4건 처리시간 0.018초

구조-활성간 연구를 통한 LTD4 antagonists의 개발 (Development of $LTD_4$ antagonists using QSAR)

  • 오민아;고동수;박관하;이승호;이혜승;임융호
    • Applied Biological Chemistry
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    • 제41권6호
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    • pp.477-482
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    • 1998
  • 새로운 Leukotriene $D_4$ antagonists를 찾기 위해 구조-활성간 연구를 수행하였다. 이미 알려진 chalcone 유도체의 구조와 생물학적 활성 자료를 이용하여 구조-활성간 계산을 수행한 결과 새로운 화합물을 발견하였고, 이를 합성하여 효과를 측정한 결과를 보고하고자 한다.

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The Alteration of Cytokine Expression and Goblet Cell Response by Cyclosporin A and Histamine Receptor Antagonists in C3H/HeN Mice Infected with Echinostoma hortense

  • Jo, Yong-Hee;Kim, In-Sik;Lee, Kyu-Jae;Kim, Jeong-Lye;Lee, Young-Mi;Cho, Kyung-Jin;Ryang, Yong-Suk
    • 대한의생명과학회지
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    • 제12권4호
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    • pp.329-335
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    • 2006
  • Echinostoma hortense (E. hortense) is an intestinal trematode with the highest infection rate in South Korea. However, the immune response against E. hortense infection has not been explained well. In the present study, we investigated the effect of treatment with cyclosporin A (CsA) and histamine receptor antagonists on the cytokine expression and mucosal goblet cells in E. hortense-infected C3H/HeN mice. The alteration of cytokine mRNA expression ($TNF-{\alpha},\;IL-l{\beta},\;IL-4\;and\;IL-5$), intestinal worm recovery rate and goblet cell responses were measured weekly from 0 to 5 weeks post-infection (P.I.) in the control and the following three drug-treated groups: CsA, hydroxyzine and cimetidine. Compared with the control group, the expression of $TNF-{\alpha}$, IL-4 and IL-5 mRNAs decreased in the CsA- and hydroxyzine-treated groups, but only IL-4 mRNA expression did in the cimetidine-treated group. Worm recovery rate was significantly increased in the drug-treated groups. Mucosal goblet cells and their mucin response significantly decreased in the CsA-treated group (P<0.01), but significantly increased in the cimetidine- (P<0.05) and hydroxyzine- (P<0.01) treated groups. These data suggest that CsA treatment inhibits production of Th1- and Th2-type cytokines which are necessary for the worm expulsion. Histamine receptor increases goblet cells and their mucin activation, although it remains to be elucidated whether it directly affects the worm expulsion period of E. hortense in C3H/HeN mice.

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Differential Induction of PepTLP Expression via Complex Regulatory System against Fungal Infection, Wound, and Jasmonic Acid Treatment during Pre-and Post-Ripening of Nonclimacteric Pepper Fruit

  • Jeon, Woong-Bae;Kim, Kwang-Sang;Lee, Hyun-Hwa;Cheong, Soo-Jin;Cho, Song-Mi;Kim, Sun-Min;Pyo, Byoung-Sik;Kim, Ynung-Soon;Oh, Boung-Jun
    • The Plant Pathology Journal
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    • 제20권4호
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    • pp.258-263
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    • 2004
  • Ripe fruit of pepper (Capsicum annuum) showed resistance to Colletotrichum gloeoporioides, but unripe fruit was susceptible. We previously isolated the PepTLP gene that induced in both unripe and ripe fruit by fungal infection and wound, and only in ripe fruit by jasmonic acid (JA) treatment. To examine further regulation of PepTLP, the action of specific agonist and antagonists of known signaling effector on the .PepTLP expression by fungal infection, wound, and JA was investigated. A similar dephosphorylation event negatively activated all the PepTLP expression in the ripe fruit by fungal infection, wound, and JA. The induction of PepTLP expression by wound is differentially regulated via phosphorylation and dephosphorylation step during pre- and post-ripening, respectively. In addition, the induction of PepTLP expression in the ripe fruit by wound and JA is differentially regulated via dephosphorylation and phosphorylation step, respectively. Only both wound and JA treatment has synergistic effect on the PepTLP expression in the unripe fruit. Both SA and JA treatments on the unripe fruit, and both wound or JA and SA on the ripe fruit could not do any effect on the expression of PepTLP. These results suggest that the induction of PepTLP expression is differentially regulated via complex regulatory system against fungal infection, wound, and JA treatment during pre- and post-ripening of pepper fruit.

Rhamnose-rich and fucose-rich oligo- and polysaccharides (RROP-s and FROPs), agonists and antagonists of cell-membrane receptors as new active principles against skin aging.

  • Robert, L.;Robert, A.M.;Gesztes, J.L.;Luppi, E.
    • 대한화장품학회:학술대회논문집
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    • 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
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    • pp.352-373
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    • 2003
  • Rhamnose-rich (RROP-s) and fucose-rich (FROP-s) oligo-and polysaccharides were prepared and extensively characterised by physical and chemical procedures [1,2] and compared to L-fucose. Their biological properties were then studied on human skin fibroblast cell cultures, human skin explant cultures and on hairless rat skin, using a variety of cell-biological, biochemical and computerised morphometrical procedures. Among the most important properties we could establish, the following are of particular interest for the tretment and prevention of age-dependent modifications of human skin (loss of skin-tissue, cells and matrix, wrinkle formation and others) : stimulation of cell proliferation (by $^3$[H]-thymidine incorporation and the MTT test), scavenging of reactive oxygen species (ROS) using several different procedures, and protease (MMP-2 and MMP-9) down-regulation. A topical preparation, using RROP-s and FROP-s, and/or L-fucose, was shown to increase cell proliferation, dermal matrix synthesis, efficient scavenging of ROS-s and to increase also the thickness of dermal tissue when applied for 4 weeks on hairless rat skin, accompanied by the densification of collagen bundles as well as by an increase of elastin synthesis. Using fluorescent labeled FROPs, it could be shown that these oligosaccharides react with cell-membrane receptors and especially with the elastin-laminin-receptor and the fucose-mannose receptor, but they penetrate also in the cell nucleus, suggesting the possibility of a direct action on the regulation of gene expression. When applied to the human skin of a team of voluntary women encompassing all age-groups, the efficiency of FROP-containing preparation could be confirmed using indentometry and computerised evaluation of skin micro-relief, as well as evaluation of periorbital wrinkles. It appears therefore that these preparations correspond to all the requirements of active anti-aging principles.

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