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.
Steroids. 2012 Nov;77(13):1502-9. doi: 10.1016/j.steroids.2012.08.011. Epub 2012 Sep 4.
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.
植物激素油菜素甾体（BRs）及其衍生物胆甾烷酮的抗血管生成活性在人脐静脉内皮细胞（HUVEC）和人微血管内皮细胞（HMEC-1）中进行了研究。在 21 种测试的天然 BR 中，24-表油菜素内酯和 28-高同型 castasterone 抑制了 HUVEC 细胞的迁移。7 种测试的 BR 显著减少了管的数量。合成类似物胆甾烷酮在体外抑制血管生成的效果比天然 BR 更有效。由于 BRs 与人类固醇相似，我们还研究了 BRs 与人类甾体受体的相互作用。合成 BRs 胆甾烷酮对雌激素受体-α（ERα）、雌激素受体-β 和雄激素受体表现出激动作用。在天然 BR 中，发现 24-表油菜素内酯是雌激素受体-α（ERα）的弱拮抗剂。我们的研究结果首次提供了证据表明，一大类 BRs 可以抑制原代内皮细胞的体外血管生成。BRs 构成了一类新的人类甾体受体激活剂或抑制剂，具有抑制血管生成的能力。
