Anti-inflammatory lipocortin-derived peptides.
Peptide Ac2-26, drawn from the sequence of human lipocortin 1, inhibited the release of elastase activity from cytoplasmic granules of human neutrophils, and neutrophil adhesion to monolayers of endothelial cells, in a concentration-dependent manner (approximate IC50 of 100 micrograms/ml, 33 microM). The effect of peptide Ac2-26 was not restricted to a specific neutrophil activator, being effective against formyl-Met-Leu-Phe (FMLP), leukotriene B4 (LTB4) and platelet-activating factor (PAF). Peptide Ac2-26 did not alter FMLP binding to its receptor. These in vitro observations complement in vivo data obtained with this peptide and may enable a better understanding of its pharmacology and, perhaps, that of of lipocortin 1 too.
Perretti
M
M
Department of Biochemical Pharmacology, William Harvey Research Institute, London, United Kingdom.
Flower
R J
RJ
D000595:Amino Acid Sequence; D000818:Animals; D017302:Annexins / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000097:blood; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
D017302:Annexins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D010455:Peptides; D009240:N-Formylmethionine Leucyl-Phenylalanine