The effect of furoyl saccharin, a novel non-peptidic acylating protease inhibitor, on experimental emphysema in the hamster.
Furoyl saccharin was evaluated for its ability to prevent the development of emphysematous lesions produced in hamsters by the exposure to aerosolized papain (3% for 3 h). Pretreatment with intratracheal furoyl saccharin (at the doses of 0.3, 1, 3 mg) reduced the appearance of papain-induced emphysema as evaluated by both physiologic (static compliance) and histologic (mean linear intercept and internal surface area of the lungs) methods. Inhibition was dose-related with maximal reduction of changes in static compliance (74%), mean linear intercept (84%) and internal surface area (65%) observed after a dose of 3 mg. This is the first time that a non-peptide acylating inhibitor of serine proteases is reported to be affective in preventing the development of experimental emphysema.
D000818:Animals; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D008297:Male; D008647:Mesocricetus; D010206:Papain; D011480:Protease Inhibitors / Q000627:therapeutic use*; D011656:Pulmonary Emphysema / Q000139:chemically induced / Q000517:prevention & control*; D012439:Saccharin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000627:therapeutic use
D011480:Protease Inhibitors; C045682:furoyl saccharin; D010206:Papain; D012439:Saccharin