title: Eponemycin, a novel antibiotic, is a highly powerful angiogenesis inhibitor.
abstract: Eponemycin, a novel antibiotic, was examined as to its anti-angiogenic activity in an in vivo assay system involving chorioallantoic membranes (CAMs) of growing chick embryos. Eponemycin powerfully inhibited angiogenesis in the CAMs. This powerful inhibition was dose-dependent, the inhibitory activity becoming detectable at a dose of 7.5 fmol/egg and the ID50 value being 250 fmol/egg, suggesting that eponemycin exhibits more potent anti-angiogenic activity than Ch 55, a synthetic retinoid, which had been the strongest angiogenesis inhibitor identified so far. To determine which event(s) in the angiogenesis process was affected by eponemycin, experiments were conducted using systems involving cultured vascular endothelial cells. Eponemycin effectively inhibited both the proliferation and migration of endothelial cells, indicating that the antibiotic affected these two important events during angiogenesis, resulting in effective inhibition of angiogenesis. These results strongly suggest that eponemycin could be a promising candidate as an angiogenesis inhibitor for the control of aberrant angiogenesis occurring in different diseases such as tumor development and diabetic retinopathy.
authors.affiliation: Division of Cancer Therapeutics, Tokyo Metropolitan Institute of Medical Science, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Oikawa
authors.forename: M
authors.initials: M
authors.lastname: Hasegawa
authors.forename: M
authors.initials: M
authors.lastname: Shimamura
authors.forename: H
authors.initials: H
authors.lastname: Ashino
authors.forename: S
authors.initials: S
authors.lastname: Murota
authors.forename: I
authors.initials: I
authors.lastname: Morita
mesh_terms: D000482:Allantois / Q000098:blood supply*; D000577:Amides / Q000302:isolation & purification / Q000494:pharmacology; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D002339:Carotid Arteries; D002455:Cell Division / Q000187:drug effects; D002465:Cell Movement / Q000187:drug effects; D002478:Cells, Cultured; D002642:Chick Embryo; D002823:Chorion / Q000098:blood supply*; D004305:Dose-Response Relationship, Drug; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects / Q000502:physiology*; D009389:Neovascularization, Pathologic / Q000517:prevention & control*; D012694:Serine / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D000577:Amides; D000903:Antibiotics, Antineoplastic; C063282:eponemycin; D012694:Serine