Selectivity in the potentiation of antibacterial activity of α-peptide/β-peptoid peptidomimetics and antimicrobial peptides by human blood plasma

摘要: Antimicrobial peptides (AMPs) are promising leads for novel antibiotics; however, their activity is often compromised under physiological conditions. The purpose of this study was to determine the α-peptide/β-peptoid peptidomimetics and AMPs against Escherichia coli Staphylococcus aureus in presence human blood-derived matrices immune effectors. minimum inhibitory concentration (MIC) two E. decreased by up one order magnitude when determined 50% blood plasma as compared MHB media. MIC a membrane-active AMP, LL-I/3, also decreased, whereas intracellularly acting were not potentiated plasma. Blood serum had no effect on neither matrix an S. aureus. Unexpectedly, concentrations albumin did influence activity. Plasma potentiation mediated LL-37 analogue, lysozyme or hydrogen peroxide; abolished complement system heat-inactivated. Time-course experiments indicated that due plasma-mediated effects bacterial cells prior activities peptidomimetics. unexpected enhancement antibacterial conditions significantly increases therapeutic potential these compounds.