Analysis of the lipopolysaccharide-induced cytostatic activity of macrophages, by the use of synthetic models.
Informations on the structural features implicated in the macrophage-dependent cytostatic activity of "lipid A" preparations were obtained by the use of 15 synthetic glycolipids. Four structural requirements were identified: the presence of a reducing glucosamine unit; the presence of a free hydroxyl group on amide-linked 3-hydroxytetradecanoic acids, and the absence of free hydroxyl groups at positions 3 and 6 of the glucosamine. The monosaccharide resembling the reducing unit of the "lipid A backbone," which fulfills these criteria, had the highest cytostatic activity, whereas the compound possessing the substitution pattern of the nonreducing moiety was inactive.
D000818:Animals; D002455:Cell Division; D003602:Cytotoxicity, Immunologic / Q000187:drug effects*; D004187:Disaccharides / Q000494:pharmacology; D004731:Endotoxins / Q000494:pharmacology; D006017:Glycolipids / Q000494:pharmacology*; D008050:Lipid A / Q000494:pharmacology; D008070:Lipopolysaccharides / Q000494:pharmacology*; D008264:Macrophages / Q000276:immunology*; D008297:Male; D012515:Mast-Cell Sarcoma / Q000473:pathology; D051379:Mice; D008809:Mice, Inbred C3H; D008954:Models, Biological; D009005:Monosaccharides / Q000494:pharmacology; D011112:Polymyxin B / Q000494:pharmacology; D010566:Virulence Factors, Bordetella / Q000494:pharmacology
D004187:Disaccharides; D004731:Endotoxins; D006017:Glycolipids; D008050:Lipid A; D008070:Lipopolysaccharides; D009005:Monosaccharides; D010566:Virulence Factors, Bordetella; D011112:Polymyxin B