Inhibition of human neutrophil elastase by wheat ceramides

Synopsis Ceramides, composed of sphingosine N-acyl linked to fatty acids have become widely used in cosmetology. They play several physiological roles in the regulation of skin barrier function. Human neutrophil elastase (HNE) can be inhibited by long-chain fatty acids and their derivatives; it was therefore postulated that plant ceramides could be inhibitors of HNE. Ceramides were extracted from wheat, isolated and characterized. The main fatty acids were 16:0, 18:1, 18:2 and the sphingoid moiety was phytosphingosine. Concentrations necessary to reach 50% inhibition of HNE were, respectively, 33 and 41 mug ml(-1) for non-glycosyl ceramides (CER) and glycosyl ceramides (gly-CER) when using a synthetic specific substrate. Similar extents of inhibition were obtained using a physiological substrate, insoluble elastin. Ex vivo studies showed that CER protected human skin elastic fibres against HNE degradation. Ceramides, being natural non-toxic substances, besides their role in cosmetics, could be of pharmacological interest in dermal inflammatory disorders.