• Title/Summary/Keyword: Analogs

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Platelet Anti-aggregating Activities of Higenamine Analogs (Higenamine 유도체들의 혈소판응집 억제작용)

  • 윤혜숙;백승환;이종란
    • YAKHAK HOEJI
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    • v.30 no.5
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    • pp.245-252
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    • 1986
  • Various structural analogs of higenamine, 1-(4'-hydroxylbenzyl)-6,7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline, were synthesized and their inhibitory activities against platelet aggregation induced by either arachidonic acid, ADP or collagen. Among the twenty-five compounds tested, inhibitory activity is favored by the 3, 4-dihydroisoquinoline system with the methyl bridge between the two aromatic rings replaced by either ethyl or ethenyl group. N-Methyl quaternization decreased the inhibitory activities. * 이논문의 내용중 편집상의 오류가 있습니다. 그에대한 정오표는 v.31, n.1의 45p.에 있습니다.

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A Novel Photonuclease; Bromofluoroacetophenone Analogs

  • Jeon, Raok
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.81-81
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    • 2001
  • The photoinducible DNA cleaving activities of bromofluoroacetophenones as a novel photonuclease were investigated. The photolytic behavior and DNA cleaving acitivity of fluorine derivative were compared with those of non-fluorine substituted compound, 4'-bromoacetophenones. Although the DNA cleaving activities of fluorine analogs were similar with those of 4'-bromoacetophenones, ο-bromo-$\rho$-fluoro derivatives gave the better DNA cleaving activities than $\rho$-bromo-ο-fluoro derivatives did.

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Anti-thrombotic Effects of Analogs of Protocatechuic Acid and Gallic Acid (Protocatechuic acid 및 Gallic acid 유도체들의 항 혈전작용)

  • 윤혜숙;강삼식;김문희;정기화
    • YAKHAK HOEJI
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    • v.37 no.5
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    • pp.453-457
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    • 1993
  • Platelet anti-aggregating activities were tested with analogs of protocatechuic acid and gallic acid. Six of them which showed comparable inhibitory effects with aspirin against collagen induced platelet aggregation were selected and their anti-thrombotic effects were evaluated in the mouse thrombosis model and compared with those of aspirin and paeonol. At the dose of 50 mg/kg, p.o., ethyl gailate(13) treated group showed higher % of recovery within 6 min of thrombotic challenge and lower mortality within 5 min than aspirin treated group.

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Specificity of Auxin Action on Ethylene Production in Corn Coleoptile Segments (옥수수(Zea mays L.) 자엽초 절편에서 에틸렌 생성에 대한 오옥신의 작용 특성)

  • 윤인선
    • Journal of Plant Biology
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    • v.34 no.4
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    • pp.325-330
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    • 1991
  • The ability of several auxin analogs to induce ethylene production was tested in the corn coleoptile. The synthetic auxins 1-naphthaleneacetic acid (1-NAA) and 2, 4-dichlorophenoxyacetic acid (2, 4-D) had strong stimulatory effects on ethylene induction surpassing that of IAA. Both 2-naphthalaneacetic acid (2-NAA) and 2, 6-dichlorophenoxy acetic acid (2, 6-D), structural analogs of these auxins, respectively, were found to be inactive. Treatment with NPA, a strong inhibitor of polar auxin transport, led to drastic increase in IAA-induced ethylene production while it has bo effect on ethylene production induced by 1-NAA. A positive correlative existed between intracellular auxin level and ethylene production.

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Desired Textures of Food Analogs and Methods of Measuring Their Textural Properties (대용 식품의 텍스츄어 특성 및 그의 측정 방법)

  • Bourne, Malcolm C.
    • Korean Journal of Food Science and Technology
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    • v.7 no.3
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    • pp.168-180
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    • 1975
  • Analogs and extenders should have mouthfeel and chewing characteristics that are similar to the food they are replacing or extending. Instrumental methods can measure some of the physical properties that constitute 'texture' but only sensory methods can provide a complete description and quantification of the textural properties of a food. Instrumental methods and sensory methods for measuring texture are reviewed.

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Wogonin and Its Analogs

  • Jang, Jin-Hee;Sin, Kwan-Seog;Park, Hae-Il
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.175.4-176
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    • 2003
  • Our long-term research goals involve the SARs study and the synthetic procedure development of wogonin and its analogs. We investigated efficient synthetic pathways of wogonin and its bioisosteres in a large quantity to decipher the structural requirements for anti-inflammatory activities. We plan to serially delete or modify the 5,7-dihydroxyl groups of wogonin to observe the effects of the hydroxyl groups on anti-inflammatory activity. Also we modofied the 8- methoxy group on a ring since it is known to be necessary for biological activity. (omitted)

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Transglutaminase-Catalysed Formation of Coenzymatically Active Immobilized NAD+ (효소법에 의한 NAD+의 $\beta$-casein에의 고정화)

  • 윤세억;박선영김명곤김강현
    • KSBB Journal
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    • v.4 no.3
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    • pp.229-234
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    • 1989
  • NAD+ analogs, 8-( 6-aminohexyl) aminonicotinamide adenine dinucleotide and N6-[(6- aminohewl)-carbamoylmethyl]- NAD+, were imobilized on bovine caseins by the action of hansglutaminase. It appears that NAD+ analogs bind with $\alpha$S1-and $\beta$-caseins through formation of the r-glutamylamine bond between the amino groups attached to the hexyl chains in NAD+ analogs and the glutaminyl residues in caseins. The NAD+ analogs immobilized on the caseins were enzymatically reducible by alcohol dehydrogenase. $\beta$-Casein was more useful carrier than the $\alpha$S1-casein and 8-substituted NAD+ analog was more effective than N6-substituted one in immobilization. Michaelis constant of 8-substituted NAD+ analog immobilized on $\beta$-casein in alcohol dehydrogenase reaction was similar to that of free from of NAD+ and that of NAD+ analog. Immobilized NAD+ was much more stable at alkaline pH than free NAD+ and its analog while maximum velocity was reduced to 31% of the free NAD+ analog. The coenzyme casein conjugated was recovered almost completely in casein precipitated by calcium.

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Development of a Highly Active Fluorescence-Based Detector for Yeast G Protein-Coupled Receptor Ste2p

  • Hong, Jin Woo;Ahn, Hee Jun;Baek, Jee Su;Hong, Eun young;Jin, Dong Hoon;Khang, Yong Ho;Hong, Nam Joo
    • Journal of Microbiology and Biotechnology
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    • v.28 no.10
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    • pp.1589-1603
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    • 2018
  • Twenty analogs of $[Orn^6,D-Ala^9]{\alpha}-factor$ were synthesized and assayed for their biological activities: seven analogs of $[Orn^6,X^9]{\alpha}-factor$, seven analogs of $[X^6,D-Ala^9]{\alpha}-factor$, five analogs of $[X^5,X^6,D-Ala^9]{\alpha}-factor$, and native ${\alpha}-factor$ (X = amino acids). Their biological activities (halo, gene induction, and affinity) were measured using S. cerevisiae Y7925 and LM102 and compared with those of native ${\alpha}-factor$ (100%). G protein-coupled receptor was expressed in strain LM102 containing pESC-LEU-STE2 vector. $[Dap^6,D-Ala^9]{\alpha}-factor$ with weak halo activity (10%) showed the highest receptor affinity (> 230%) and the highest gene induction activity (167%). $[Arg^6,D-Ala^9]{\alpha}-factor$ showed the highest halo activity (2,000%). The number of active binding sites per cell (about 20,000 for strain LM102) was determined using a newly-designed fluorescence-based detector, $[Arg^6,D-Ala^9]{\alpha}-factor-Edan$, with high sensitivity (12,500-fold higher than the absorption-based detector $[Orn^6]{\alpha}-factor-[Cys]_3$).

Effect of Glucose, Its Analogs and Some Amino Acids on Pre-steady State Kinetics of ATP Hydrolysis by PM-ATPase of Pathogenic Yeast (Candida albicans)

  • Bushra, Rashid;Nikhat, Manzoor;M., Amin;Luqman A., Khan
    • Animal cells and systems
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    • v.8 no.4
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    • pp.307-312
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    • 2004
  • Fast kinetics of transient pH changes and difference spectrum formation have been investigated following mixing of ADP/ATP with partially purified plasma membrane PM-ATPase of the pathogenic yeast Candida albicans in the presence of five nutrients: glucose, glutamic acid, proline, lysine, and arginine and two analogs of glucose: 2-deoxy D-glucose and xylose. Average $H^+$- absorption to release ratio, indicative of population of ATPase undergoing complete hydrolytic cycle, was found to be 0.27 for control. This ratio varied between 0.25 (proline) to 0.36 (arginine) for all other compounds tested, except for glucose. In the presence of glucose, $H^+$- absorption to release ratio was exceptionally high (0.92). While no UV difference spectrum was observed with ADP, mixing of ATP with ATPase led to a large conformational change. Exposure to different nutrients restricted the magnitude of the conformational change; the analogs of glucose were found to be ineffective. This suppression was maximal in the case of glucose (80%); with other nutrients, the magnitude of suppression ranged from 40-50%. Rate of $H^+$- absorption, which is indicative of E~P complex dissociation, showed positive correlation with suppression of conformational change only in the case of glucose and no other nutrient/analog. Mode of interaction of glucose with plasma membrane $H^+$-ATPase thus appears to be strikingly distinct compared to that of other nutrients/analogs tested. The results obtained lead us to propose a model for explaining glucose stimulation of plasma membrane $H^+$-ATPase activity.