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rdf:type |
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lifeskim:mentions |
umls-concept:C0021467,
umls-concept:C0021469,
umls-concept:C0205369,
umls-concept:C0205409,
umls-concept:C0231491,
umls-concept:C0330232,
umls-concept:C1280500,
umls-concept:C1419053,
umls-concept:C1515655,
umls-concept:C1533691,
umls-concept:C1880022
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pubmed:issue |
3
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pubmed:dateCreated |
1985-3-27
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pubmed:abstractText |
Platelet-activating factor (PAF) is a potent lipid mediator of inflammation and asthma. Using a receptor preparation of rabbit platelet membranes, we identified a novel antagonist of PAF in the methylene chloride extract of a Chinese herbal plant, haifenteng (Piper futokadsura). The active antagonist, kadsurenone, was isolated and characterized in several in vitro and in vivo assays. It is a specific and competitive inhibitor of PAF binding to its receptor with a Ki of 5.8 X 10(-8) M vs. a Ki of 6.3 X 10(-9) M for PAF itself. It inhibits PAF-induced aggregation of rabbit platelets and human neutrophils at 2.4-24 microM, without showing any PAF agonistic activity. It potently inhibits PAF-induced degranulation of human neutrophils at 2.5-50 microM, also without any agonist activity. Kadsurenone is active orally at 25-50 mg/kg of body weight in blocking PAF-induced cutaneous permeability in the guinea pig. It also inhibits PAF-induced increases of hematocrit and circulating N-acetylglucosaminidase in the rat at greater than 10 mg/kg i.p. in a dose-dependent manner. Kadsurenone does not interfere with the function of several pharmacological mediators and receptors tested. Its structural specificity is evidenced by the poor PAF-antagonistic activities of three related structures isolated from the same haifenteng extract.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-1015835,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-121258,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-4179068,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-4396896,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-489536,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6309563,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6313047,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6315819,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6408071,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6427378,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6581831,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6652376,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6654882,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-6692502,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-7070056,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-7085259,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-7087685,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-7126622,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-7401945,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2983307-909582
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0027-8424
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
82
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
672-6
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:2983307-Angiosperms,
pubmed-meshheading:2983307-Animals,
pubmed-meshheading:2983307-Benzofurans,
pubmed-meshheading:2983307-Benzopyrans,
pubmed-meshheading:2983307-Capillary Permeability,
pubmed-meshheading:2983307-Guinea Pigs,
pubmed-meshheading:2983307-Humans,
pubmed-meshheading:2983307-Lignans,
pubmed-meshheading:2983307-Mathematics,
pubmed-meshheading:2983307-Neutrophils,
pubmed-meshheading:2983307-Platelet Activating Factor,
pubmed-meshheading:2983307-Platelet Aggregation,
pubmed-meshheading:2983307-Platelet Membrane Glycoproteins,
pubmed-meshheading:2983307-Rabbits,
pubmed-meshheading:2983307-Receptors, Cell Surface,
pubmed-meshheading:2983307-Receptors, G-Protein-Coupled
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pubmed:year |
1985
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pubmed:articleTitle |
Characterization of a platelet-activating factor receptor antagonist isolated from haifenteng (Piper futokadsura): specific inhibition of in vitro and in vivo platelet-activating factor-induced effects.
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pubmed:publicationType |
Journal Article
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