title: [Antimicrobial Properties of Eremoxylarin A Produced by Ascomycete of Sordariomycetes in Submerged Culture].
abstract: The fungal strain INA 01108 producing antibiotic substances with broad spectrum of antibacterial activity was isolated from the natural environment. By the morphological characteristics and DNA analysis it was shown to belong to Ascomycetes of Sordariomycetes. In submerged culture the strain produced at least four antibiotics. The major component of them was identified as eremophilane-type sesquiterpene eremoxylarin A. Eremoxylarin A is effective in vitro against grampositive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin group glycopeptide antibiotics resistant Leuconostoc mesenteroides VKPM B-4177. The efficacy and toxicity of eremoxylarin A was determined on a murine staphylococcal sepsis model. The dose of 6.25 mg/kg provided 100% recovery and survival of the animals, while the dose of 3.12 mg/kg was close to the ED50. The chemical structure of eremoxylarin A allows to modify the antibiotic and such studies may be relevant to design a less toxic derivative without loss of the valuable antimicrobial properties.
authors.forename: O V
authors.initials: OV
authors.lastname: Efremenkova
authors.forename: B F
authors.initials: BF
authors.lastname: Vasiljeva
authors.forename: V A
authors.initials: VA
authors.lastname: Zenkova
authors.forename: A M
authors.initials: AM
authors.lastname: Korolev
authors.forename: Y N
authors.initials: YN
authors.lastname: Lusikov
authors.forename: T A
authors.initials: TA
authors.lastname: Efimenko
authors.forename: I A
authors.initials: IA
authors.lastname: Malanicheva
authors.forename: E P
authors.initials: EP
authors.lastname: Mirchink
authors.forename: E B
authors.initials: EB
authors.lastname: Isakova
authors.forename: E N
authors.initials: EN
authors.lastname: Bilanenko
authors.forename: O V
authors.initials: OV
authors.lastname: Kamzolkina
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000302:isolation & purification / Q000627:therapeutic use* / Q000633:toxicity; D001203:Ascomycota / Q000254:growth & development* / Q000378:metabolism / Q000648:ultrastructure; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D007934:Leuconostoc / Q000187:drug effects*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D051379:Mice; D008826:Microbial Sensitivity Tests; D000081223:Polycyclic Sesquiterpenes; D018805:Sepsis / Q000188:drug therapy* / Q000382:microbiology; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000627:therapeutic use* / Q000633:toxicity; D013203:Staphylococcal Infections / Q000188:drug therapy* / Q000382:microbiology
chemical_list: D000900:Anti-Bacterial Agents; D000081223:Polycyclic Sesquiterpenes; D012717:Sesquiterpenes; C018286:eremophilane compounds