title: Brassinosteroids inhibit in vitro angiogenesis in human endothelial cells.
abstract: Antiangiogenic activity of the brassinosteroid plant hormones (BRs) and their derivative cholestanon was investigated in human umbilical vein endothelial cells (HUVEC) and in human microvascular endothelial cells (HMEC-1). 24-Epibrassinolide and 28-homocastasterone from group of 21 tested natural BRs inhibited migration of HUVEC cells. Seven tested BRs decreased the number of tubes significantly. Synthetic analogue cholestanon inhibited angiogenesis in vitro more effectively than natural BRs. Because of the similarity of BRs to human steroids, we have also studied interactions of BRs with human steroid receptors. Synthetic BRs cholestanon showed agonistic effects on estrogen-receptor-α, estrogen-receptor-β and androgen receptor. Of the natural BRs, 24-epibrassinolide was found to be a weak antagonist of estrogen-receptor-α (ERα). Our results provide the first evidence that large group of BRs can inhibit in vitro angiogenesis of primary endothelial cells. BRs constitute a novel group of human steroid receptor activators or inhibitors with capacity to inhibit angiogenesis.
authors.affiliation: Centre of Region Haná for Biotechnological and Agricultural Research, Department of Growth Regulators, Faculty of Science, Palacký University, Šlechtitelů 11, 783 71 Olomouc, Czech Republic.
authors.forename: Lucie
authors.initials: L
authors.lastname: Rárová
authors.forename: Stefan
authors.initials: S
authors.lastname: Zahler
authors.forename: Johanna
authors.initials: J
authors.lastname: Liebl
authors.forename: Vladimír
authors.initials: V
authors.lastname: Kryštof
authors.forename: David
authors.initials: D
authors.lastname: Sedlák
authors.forename: Petr
authors.initials: P
authors.lastname: Bartůněk
authors.forename: Ladislav
authors.initials: L
authors.lastname: Kohout
authors.forename: Miroslav
authors.initials: M
authors.lastname: Strnad
mesh_terms: D020533:Angiogenesis Inhibitors / Q000378:metabolism / Q000494:pharmacology*; D060406:Brassinosteroids / Q000378:metabolism / Q000494:pharmacology*; D047628:Estrogen Receptor alpha / Q000378:metabolism; D047629:Estrogen Receptor beta / Q000378:metabolism; D061307:Human Umbilical Vein Endothelial Cells / Q000187:drug effects* / Q000378:metabolism*; D006801:Humans; D018919:Neovascularization, Physiologic / Q000187:drug effects*
chemical_list: D020533:Angiogenesis Inhibitors; D060406:Brassinosteroids; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta