Synthesis and biological evaluation of novel lipid A antagonists.
A mimetic of Lipid A with a beta-N(OMe) glycosidic linkage, four linear C-14 hydrophobic chains and without phosphate groups has been prepared together with its beta-O-linked analogue. Both these molecules were active in inhibiting the inflammatory action of Escherichia coli lipid A on MT2 macrophages in a dose-dependent manner, while they were completely devoid of inflammatory activity.
Peri
Francesco
F
Department of Biotechnology and Biosciences, University of Milano-Bicocca, P.zza della Scienza 2, 20126 Milan, Italy. francesco.peri@unimib.it
Marinzi
Chiara
C
Barath
Marek
M
Granucci
Francesca
F
Urbano
Matteo
M
Nicotra
Francesco
F
D002240:Carbohydrate Sequence; D002241:Carbohydrates / Q000138:chemical synthesis* / Q000494:pharmacology*; D008050:Lipid A / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D018716:Molecular Mimicry; D008969:Molecular Sequence Data; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
D002241:Carbohydrates; D008050:Lipid A