title: Isolation and characterization of NAI-802, a new lantibiotic produced by two different Actinoplanes strains.
abstract: Lantibiotics are biologically active peptides produced by Gram-positive bacteria. Starting from fermentation broth extracts preselected from a high-throughput screening program for discovering cell-wall inhibitors, we successfully isolated a new lantibiotic produced by Actinoplanes sp., designated as NAI-802. MS and NMR analysis together with explorative chemistry established that NAI-802 consists of 21 amino acids, 19 of which are identical to those present in the class II lantibiotic actagardine. Interestingly, NAI-802 carries one extra alanine and one extra arginine at the N- and C-termini, respectively. As expected from the overall higher positive charge, NAI-802 was slightly more active than actagardine against staphylococci and streptococci. Further improvement of its antibacterial activity was achieved by adding one additional positive charge through conversion of the C-terminal carboxylate into the corresponding basic amide. NAI-802 thus represents a novel promising candidate for treating Gram-positive infections caused by multidrug-resistant pathogens.
authors.affiliation: NAICONS Scrl, Milano, Italy.
authors.forename: Matteo
authors.initials: M
authors.lastname: Simone
authors.forename: Paolo
authors.initials: P
authors.lastname: Monciardini
authors.forename: Eleonora
authors.initials: E
authors.lastname: Gaspari
authors.forename: Stefano
authors.initials: S
authors.lastname: Donadio
authors.forename: Sonia I
authors.initials: SI
authors.lastname: Maffioli
mesh_terms: D000192:Actinomycetales / Q000378:metabolism*; D000900:Anti-Bacterial Agents / Q000096:biosynthesis* / Q000737:chemistry / Q000494:pharmacology*; D001430:Bacteriocins / Q000096:biosynthesis* / Q000737:chemistry / Q000494:pharmacology*; D005285:Fermentation; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy; D008826:Microbial Sensitivity Tests; D013210:Staphylococcus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D001430:Bacteriocins; C581107:NAI-802