title: Nanostructure formation enhances the activity of LPS-neutralizing peptides.
abstract: Peptides that interact with lipopolysaccharide (LPS) can provide the basis for the development of new antisepsis agents. In this work, several LPS-neutralizing acyl peptides derived from LALF, BPI, and SAP were prepared, structurally characterized, and biologically evaluated. In all cases, peptides with long acyl chains showed greater LPS-neutralizing activities than the original acetylated peptides. Structural analysis of these peptides revealed that N-acylation with long acyl chains promotes the formation of micellar or fibril-like nanostructures, thus proving a correlation between anti-LPS activity and nanostructure formation. The results of this study provide useful structural insight for the future design of new acyl peptides that strongly bind LPS and therefore act as antisepsis drugs. Furthermore, this nanostructure-biological activity correlation can be translated into other therapeutic areas.
authors.affiliation: Institute for Research in Biomedicine, Barcelona Science Park, 08028 Barcelona, Spain.
authors.forename: Carlos
authors.initials: C
authors.lastname: Mas-Moruno
authors.forename: Laura
authors.initials: L
authors.lastname: Cascales
authors.forename: Luis J
authors.initials: LJ
authors.lastname: Cruz
authors.forename: Puig
authors.initials: P
authors.lastname: Mora
authors.forename: Enrique
authors.initials: E
authors.lastname: Pérez-Payá
authors.forename: Fernando
authors.initials: F
authors.lastname: Albericio
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006737:Horseshoe Crabs / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D008070:Lipopolysaccharides / Q000737:chemistry*; D051379:Mice; D008823:Micelles; D046529:Microscopy, Electron, Transmission / Q000379:methods; D053758:Nanoparticles / Q000737:chemistry*; D036103:Nanotechnology / Q000379:methods*; D010455:Peptides / Q000737:chemistry*; D018805:Sepsis / Q000188:drug therapy; D015398:Signal Transduction
chemical_list: D008070:Lipopolysaccharides; D008823:Micelles; D010455:Peptides