title: Synthesis, anti-MRSA, and anti-VRE activity of hemin conjugates with amino acids and branched peptides.
abstract: The increasing prevalence of antibiotic-resistant bacterial strains has necessitated the synthesis of novel antibacterial agents. It was previously shown that naturally occurring metalloporphyrin hemin possesses dark antibacterial activity against Gram-positive bacteria. To improve hemin antibacterial activity, we synthesized a number of hemin conjugates with amino acids and branched peptides. Arginine-containing hemin conjugates demonstrated high antibacterial activity against Gram-positive bacteria including methicillin- and vancomycin-resistant strains in vitro. Most of the synthesized conjugates showed low toxicity against human erythrocytes and leukocytes.
authors.affiliation: Department of Biotechnology and Organic synthesis, Moscow State University of Fine Chemical Technology, Vernadskogo prosp., 86, 119571, Moscow, Russia.
authors.forename: Sergei A
authors.initials: SA
authors.lastname: Okorochenkov
authors.forename: Galina A
authors.initials: GA
authors.lastname: Zheltukhina
authors.forename: Elena P
authors.initials: EP
authors.lastname: Mirchink
authors.forename: Elena B
authors.initials: EB
authors.lastname: Isakova
authors.forename: Alexey V
authors.initials: AV
authors.lastname: Feofanov
authors.forename: Vladimir E
authors.initials: VE
authors.lastname: Nebolsin
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016983:Enterococcus / Q000187:drug effects*; D006427:Hemin / Q000737:chemistry*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D020713:Vancomycin Resistance
chemical_list: D000900:Anti-Bacterial Agents; D006427:Hemin
keywords: antibacterial activity; branched peptides; hemin; methicillin-resistant Staphylococcus aureus; vancomycin-resistant Enterococcus faecium