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Studies of MR 889, a new synthetic proteinase inhibitor
M Luisetti1, P D Piccioni, M Donnini
1Istituto di Tisiologia e Malattie Respiratorie dell'Università, IRCCS Policlinico San Matteo, Pavia, Italy.
Abstract:
We investigated the proteinase inhibitory activity of MR 889, a thiolactic acid derivative. It is able to in vitro inhibit at low concentration (10(-5),10(-6)M) the activity of porcine pancreatic elastase, human neutrophil elastase and bovine chymotrypsin. In addition, MR 889 is able to inhibit the residual activity of alpha 2-macroglobulin-trapped human neutrophil elastase, paralleling the efficacy of phenylmethylsufonylfluoride. Finally, MR 889 has been shown to in vitro reduce the burden of elastase- and chymotrypsin-like activity found in sputum sol-phases of patients admitted for chronic bronchitis exacerbation.