title: Embellistatin, a microtubule polymerization inhibitor, inhibits angiogenesis both in vitro and in vivo.
abstract: The efficient inhibition of angiogenesis is considered as a promising strategy for the treatment of angiogenesis-related diseases including cancer. Herein, we report that embellistatin, a bicyclic ketone compound known as a microtubule polymerization inhibitor, exhibits anti-angiogenic activity. Embellistatin inhibited in vitro angiogenesis of bovine aortic endothelial cells (BAECs) such as bFGF-induced invasion and tube formation as well as bFGF-induced mouse corneal angiogenesis in vivo. Notably, embellistatin exhibited stronger inhibition activity for the growth of BAECs than that of normal and cancer cell lines. Cell cycle analysis revealed that the compound arrests cell cycle at G2/M phase, which is associated with the increased expression of p21(WAF1) and p53 partly. These results demonstrate that embellistatin may serve the basis for the development of new anti-angiogenic agents.
authors.affiliation: Chemical Genomics Laboratory, Department of Biotechnology, College of Engineering, Yonsei University, 134 Shinchon-dong, Seodaemun-gu, Seoul 120-749, Republic of Korea.
authors.forename: Hye Jin
authors.initials: HJ
authors.lastname: Jung
authors.forename: Joong Sup
authors.initials: JS
authors.lastname: Shim
authors.forename: Hyang Burm
authors.initials: HB
authors.lastname: Lee
authors.forename: Chang-Jin
authors.initials: CJ
authors.lastname: Kim
authors.forename: Takashi
authors.initials: T
authors.lastname: Kuwano
authors.forename: Mayumi
authors.initials: M
authors.lastname: Ono
authors.forename: Ho Jeong
authors.initials: HJ
authors.lastname: Kwon
mesh_terms: D020533:Angiogenesis Inhibitors / Q000008:administration & dosage*; D000818:Animals; D002417:Cattle; D002460:Cell Line; D020256:Choroidal Neovascularization / Q000188:drug therapy* / Q000473:pathology*; D004305:Dose-Response Relationship, Drug; D006538:Heptanoic Acids / Q000008:administration & dosage*; D006801:Humans; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008870:Microtubules / Q000187:drug effects*; D009281:Naphthalenes / Q000008:administration & dosage*; D009389:Neovascularization, Pathologic / Q000473:pathology* / Q000517:prevention & control*; D018919:Neovascularization, Physiologic / Q000187:drug effects*; D016896:Treatment Outcome
chemical_list: D020533:Angiogenesis Inhibitors; D006538:Heptanoic Acids; D009281:Naphthalenes; C517529:embellistatin