title: Macrosphelide, a novel inhibitor of cell-cell adhesion molecule. I. Taxonomy, fermentation, isolation and biological activities.
abstract: Potent anti-adherent activity was detected in fermentation extracts of microbial strain FO-5050. Active compounds designated macrosphelide A and B were isolated and the structure was determined to be 16-membered macrolide antibiotics possessing three ester bonds in the ring structure. Macrosphelide A dose-dependently inhibited the adhesion of HL-60 cells to LPS-activated HUVEC monolayer (IC50, 3.5 microM); macrophelide B also inhibited HL-60 adhesion but to a lesser extent (IL50, 36 microM). Macrosphelide A did not show any antimicrobial and cytocidal activities at the concentration of 1000 micrograms/ml and 100 micrograms/ml, respectively.
authors.affiliation: The Kitasato Institute, Tokyo, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Hayashi
authors.forename: Y P
authors.initials: YP
authors.lastname: Kim
authors.forename: H
authors.initials: H
authors.lastname: Hiraoka
authors.forename: M
authors.initials: M
authors.lastname: Natori
authors.forename: S
authors.initials: S
authors.lastname: Takamatsu
authors.forename: T
authors.initials: T
authors.lastname: Kawakubo
authors.forename: R
authors.initials: R
authors.lastname: Masuma
authors.forename: K
authors.initials: K
authors.lastname: Komiyama
authors.forename: S
authors.initials: S
authors.lastname: Omura
mesh_terms: D000900:Anti-Bacterial Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002448:Cell Adhesion / Q000187:drug effects*; D002460:Cell Line; D005285:Fermentation; D018922:HL-60 Cells; D006571:Heterocyclic Compounds / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D008826:Microbial Sensitivity Tests; D003904:Mitosporic Fungi / Q000145:classification / Q000378:metabolism*
chemical_list: D000900:Anti-Bacterial Agents; D006571:Heterocyclic Compounds; C097798:macrosphelide A; C097799:macrosphelide B