Inhibition by phosphoramidon of Pseudomonas aeruginosa elastase injected intracorneally in rabbit eyes.

Abstract

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.

• Authors: E Kessler, A Spierer
• Journal: Current eye research (Curr Eye Res) Vol. 3 Issue 8 Pg. 1075-8 (Aug 1984) ISSN: 0271-3683 [Print] England
• PMID: 6435958 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Dipeptides
• Glycopeptides
• phosphorylleucylphenylalanine
• Pancreatic Elastase
• phosphoramidon

Topics

• Animals
• Chemical Phenomena
• Chemistry
• Cornea (drug effects, microbiology)
• Dipeptides (therapeutic use)
• Drug Evaluation, Preclinical
• Glycopeptides (administration & dosage, therapeutic use)
• Injections
• Keratitis (prevention & control)
• Pancreatic Elastase (administration & dosage, antagonists & inhibitors)
• Pseudomonas Infections (prevention & control)
• Pseudomonas aeruginosa (enzymology)
• Rabbits