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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1988-11-15
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pubmed:abstractText |
A lipid A-subunit analogue GLA-27, a 4-O-phosphono-D-glucosamine derivative carrying 3-O-tetradecanoyl and N-3-tetradecanoyloxytetradecanoyl groups, exhibited significant biological activities but no detectable pyrogenicity or local Shwarzman activity. In order to synthesize compounds combining GLA-27 with muramyl dipeptide (MDP), the OH group at the C6 position of GLA-27 was first succinylated. A compound which combined a succinylated GLA-27 (GLA-101) with 1-deoxy N-acetyl-muramyl-L-alanyl-D-isoglutamine methyl ester (1-deoxy MDP) via spacers of different carbon chain lengths of 5, 11 and 15, termed GLA-105, GLA-106 and GLA-107, respectively, and their biological activities were investigated. Intraperitoneal administration of combined preparations with spacers, GLA-105 and GLA-107, induced much higher phagocytic activity in peritoneal macrophages than GLA-27, GLA-101 and 1-deoxy MDP. The activity of GLA-106 did not increase by the combination. In induction of natural killer (NK) activity in peritoneal cells, GLA-105 and GLA-107 were significantly more active than 1-deoxy MDP but only comparable with GLA-27. GLA-101 showed stronger NK activity than GLA-27. The activity of GLA-106 was stronger than 1-deoxy MDP but weaker than GLA-27, GLA-105 and GLA-107. Mitogenic, interferon-inducing and tumor necrosis factor-inducing activities decreased by combining GLA-101 with 1-deoxy MDP. GLA-101, GLA-105 and GLA-107 strongly inhibited the formation of lesions on the tail of mice infected with Vaccinia virus. The activity was almost equivalent to that of GLA-27.(ABSTRACT TRUNCATED AT 250 WORDS)
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetylmuramyl-Alanyl-Isoglutamine,
http://linkedlifedata.com/resource/pubmed/chemical/Antiviral Agents,
http://linkedlifedata.com/resource/pubmed/chemical/GLA 27,
http://linkedlifedata.com/resource/pubmed/chemical/Interferons,
http://linkedlifedata.com/resource/pubmed/chemical/Lipid A,
http://linkedlifedata.com/resource/pubmed/chemical/Tumor Necrosis Factor-alpha
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pubmed:status |
MEDLINE
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pubmed:issn |
0192-0561
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
339-46
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:2459075-Acetylmuramyl-Alanyl-Isoglutamine,
pubmed-meshheading:2459075-Animals,
pubmed-meshheading:2459075-Antiviral Agents,
pubmed-meshheading:2459075-Female,
pubmed-meshheading:2459075-Immunity,
pubmed-meshheading:2459075-Immunity, Innate,
pubmed-meshheading:2459075-Interferons,
pubmed-meshheading:2459075-Killer Cells, Natural,
pubmed-meshheading:2459075-Lipid A,
pubmed-meshheading:2459075-Macrophage Activation,
pubmed-meshheading:2459075-Mice,
pubmed-meshheading:2459075-Structure-Activity Relationship,
pubmed-meshheading:2459075-Tumor Necrosis Factor-alpha
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pubmed:year |
1988
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pubmed:articleTitle |
Immunopharmacological activities of chemically synthesized lipid A-subunit analogue GLA-27 combined with muramyl dipeptide via spacers of different carbon chain length.
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pubmed:affiliation |
School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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