Tailoring elastase inhibition with synthetic peptides

Chronic wounds are the result of excessive amounts of tissue destructive proteases such as human neutrophil elastase (HNE). The high levels of this enzyme found on those types of wounds inactivate the endogenous inhibitor barrier thus, the search for new HNE inhibitors is required.This work presents two new HNE inhibitor peptides, which were synthesized based on the reactive-site loop of the Bowman–Birk inhibitor protein. The results obtained indicated that these new peptides are competitive inhibitors for HNE and, the inhibitory activity can be modulated by modifications introduced at the N- and C-terminal of the peptides. Furthermore, these peptides were also able to inhibit elastase from a human wound exudate while showing no cytotoxicity against human skin fibroblasts in vitro, greatly supporting their potential application in chronic wound treatment.

Graphical abstractFigure optionsDownload full-size imageDownload high-quality image (202 K)Download as PowerPoint slideResearch highlights► New Bowman-Birk based peptides were designed. ► The peptides increased the inhibition of Human Elastase. ► Human Elastase found on chronic wounds is greatly inhibited by the designed peptides. ► The peptides are no cytotoxic to human skin fibroblasts cells.