Inhibition of the activity of human leukocyte elastase by lipids particularly oleic acid and retinoic acid.
The effect of various natural hydrophobic lipids on the in vitro and in vivo activity of human leukocyte elastase has been examined. In vitro studies using 2 different substrates indicated that fatty acids inhibit human leukocyte elastase activity, with maximum inhibition observed with oleic acid. Triolein, cholesterol, and beta-carotene caused little inhibition. The presence of a carboxyl group appears important since retinoic acid but not retinol also inhibited activity. In vivo studies of an emphysema model in mice indicated that intrapulmonary instillation of oleic or retinoic acid reduced lung injury caused by human leukocyte elastase. The possibility of using these compounds to diminish elastolytic damage in emphysema is raised.
Sklan
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Faculty of Agriculture, Hebrew University, Rehovot, Israel.
Rappaport
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Vered
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D000818:Animals; D006801:Humans; D066298:In Vitro Techniques; D019272:Leukocyte Elastase; D008168:Lung / Q000187:drug effects / Q000473:pathology; D051379:Mice; D019301:Oleic Acid; D009829:Oleic Acids / Q000494:pharmacology*; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors*; D011656:Pulmonary Emphysema / Q000473:pathology / Q000517:prevention & control; D014212:Tretinoin / Q000494:pharmacology*
D009829:Oleic Acids; D019301:Oleic Acid; D014212:Tretinoin; D010196:Pancreatic Elastase; D019272:Leukocyte Elastase