Inhibition by phosphoramidon of Pseudomonas aeruginosa elastase injected intracorneally in rabbit eyes.
Phosphoramidon (N-(alpha-L-rhamnopyranosyloxyhydroxyphosphinyl)-L-leucyl-L-trypto phan) is a powerful inhibitor of Pseudomonas aeruginosa elastase. The addition of this compound to an elastase solution injected intrastromally in rabbit eyes protected the corneas from the damage of the enzyme for a period of 12 hours. Phosphoramidon is comparable in this respect to the inhibitor 2-mercaptoacetyl-L-phenylalanyl-L-leucine, but is considerably more effective than its analog phosphoryl-L-leucyl-L-phenylalanine (P-Leu-Phe). It is suggested that the rhamnopyranosyl moiety, present in phosphoramidon but not in P-Leu-Phe, is responsible for the difference in the intracorneal activity of the two phosphoramidates. Phosphoramidon as well as the mercaptoacetyl derivative might prove beneficial in the treatment of Pseudomonas aeruginosa corneal infections.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D003315:Cornea / Q000187:drug effects / Q000382:microbiology; D004151:Dipeptides / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D006020:Glycopeptides / Q000008:administration & dosage / Q000627:therapeutic use*; D007267:Injections; D007634:Keratitis / Q000517:prevention & control*; D010196:Pancreatic Elastase / Q000008:administration & dosage / Q000037:antagonists & inhibitors*; D011552:Pseudomonas Infections / Q000517:prevention & control*; D011550:Pseudomonas aeruginosa / Q000201:enzymology*; D011817:Rabbits
D004151:Dipeptides; D006020:Glycopeptides; C033601:phosphorylleucylphenylalanine; D010196:Pancreatic Elastase; C008890:phosphoramidon