Macrosphelide, a novel inhibitor of cell-cell adhesion molecule. I. Taxonomy, fermentation, isolation and biological activities.
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.
Hayashi
M
M
The Kitasato Institute, Tokyo, Japan.
Kim
Y P
YP
Hiraoka
H
H
Natori
M
M
Takamatsu
S
S
Kawakubo
T
T
Masuma
R
R
Komiyama
K
K
Omura
S
S
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*
D000900:Anti-Bacterial Agents; D006571:Heterocyclic Compounds; C097798:macrosphelide A; C097799:macrosphelide B