Prevention of some types of inflammatory damage using AA 231-1, a fluorinated beta-lactam.
The leukocyte elastase inhibitory activity of AA 231-1, a suicide substrate, was investigated in the presence of elastin, a natural substrate of elastase, and its efficiency to reduce the degradation of basement membrane and haemorrhage induced by elastase was analysed. Elastin only moderately decreased the inhibitory efficiency of AA 231-1. The digestion by human leukocyte elastase (HLE) of glomerular basement membrane prepared from pig kidney was prevented in the presence of AA 231-1. Intradermal microvascular haemorrhage was also significantly inhibited by AA 231-1. These results suggest that AA 231-1 may be a valuable candidate as an anti-inflammatory agent.
Reboud-Ravaux
M
M
Laboratory of Molecular Enzymology, Jacques Monod Institute, University of Paris VII, France.
Vergely
I
I
Maillard
J
J
Favreau
C
C
Kobaiter
R
R
Joyeau
R
R
Wakselman
M
M
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001384:Azetidines / Q000494:pharmacology; D001485:Basement Membrane / Q000187:drug effects; D004549:Elastin / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007678:Kidney Glomerulus / Q000187:drug effects; D007962:Leukocytes / Q000201:enzymology; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D013552:Swine; D047090:beta-Lactams
D000900:Anti-Bacterial Agents; D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001384:Azetidines; D047090:beta-Lactams; C067251:N-(2-chloromethylphenyl)-3,3-difluoroazetidin-2-one; D004549:Elastin; D010196:Pancreatic Elastase