title: Mechanistic studies and biological activity of bioxalomycin alpha 2, a novel antibiotic produced by Streptomyces viridodiastaticus subsp. "litoralis" LL-31F508.
abstract: The bioxalomycins, a novel complex of broad-spectrum antibiotics, were isolated from fermentations of Streptomyces viridodiastaticus subsp. "litoralis" LL-31F508. Bioxalomycin alpha 2, the major component of this complex, exhibited antibacterial activity. The MICs ranged from < or = 0.002 to 0.008 micrograms/ml for gram-positive organisms and from 0.50 to 4 micrograms/ml for gram-negative organisms. Bioxalomycin alpha 2 was found to be bactericidal and to inhibit bacterial DNA synthesis preferentially. Bioxalomycin alpha 2 protected mice from a lethal challenge with Staphylococcus aureus Smith. The 50% effective dose of bioxalomycin alpha 2 administered orally was 10 times greater than that when the drug was given subcutaneously or intravenously. These data suggest a stability or bioavailability problem when the compound is administered orally.
authors.affiliation: Natural Products Research Section, American Cyanamid Company, Pearl River, New York 10965.
authors.forename: M P
authors.initials: MP
authors.lastname: Singh
authors.forename: P J
authors.initials: PJ
authors.lastname: Petersen
authors.forename: N V
authors.initials: NV
authors.lastname: Jacobus
authors.forename: W M
authors.initials: WM
authors.lastname: Maiese
authors.forename: M
authors.initials: M
authors.lastname: Greenstein
authors.forename: D A
authors.initials: DA
authors.lastname: Steinberg
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000096:biosynthesis; D004269:DNA, Bacterial / Q000096:biosynthesis; D005260:Female; D006873:Hydroquinones / Q000494:pharmacology*; D051379:Mice; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000494:pharmacology*; D012329:RNA, Bacterial / Q000096:biosynthesis; D013203:Staphylococcal Infections / Q000188:drug therapy; D013302:Streptomyces / Q000378:metabolism*
chemical_list: D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D004269:DNA, Bacterial; D006873:Hydroquinones; D010080:Oxazoles; D012329:RNA, Bacterial; C090719:bioxalomycin alpha(2)