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首页> 外文期刊>Angiogenesis >Anti-angiogenic activity of sesterterpenes; natural product inhibitors of FGF-2-induced angiogenesis.
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Anti-angiogenic activity of sesterterpenes; natural product inhibitors of FGF-2-induced angiogenesis.

机译：酯类萜的抗血管生成活性; FGF-2诱导的血管生成的天然产物抑制剂。

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Angiogenesis, the growth of new blood vessels from the pre-existing vasculature is of physiological and pathological importance. We have investigated the anti-angiogenic potential of two naturally occurring sesterterpenes, leucosesterterpenone (compound 1) and leucosterlactone (compound 2) isolated from the Himalayan plant Leucosceptrum canum and identified as having biological activity in preliminary screening. Compound 1 inhibited fibroblast growth factor-2-induced proliferation, migration in a wounding assay, chemotaxis and tube formation with small vessel (human dermal) and large vessel (bovine aortic) endothelial cells while compound 2 was largely inactive. Both compounds were also active in an in vivo angiogenic model using the chick chorioallantoic membrane. Neither compounds showed inhibitory activity in the absence of fibroblast growth factor-2. We were able to demonstrate in a binding assay that compounds 1 and 2 bound to the fibroblast growth factor-2 receptor-1 with IC(50) values of 1.4 +/-0.956 and 132.47 +/- 7.90 muM, respectively, with a concomitant down regulation of phosphorylated ERK1/2 but did not bind to receptor-2. Compound 1 was less hydrophobic than compound 2 and this may contribute to its increased activity. Compound 1 is a new addition to the small number of inhibitors of fibroblast growth factor-2-induced angiogenesis. The compound was a specific inhibitor in that it had no effect on vascular endothelial growth factor or epithelial growth factor-induced angiogenesis. Since angiogenesis is essential for tumour development we conclude that these compounds may have potential as anti-tumour agents.
机译：血管生成，来自先前存在的脉管系统的新血管的生长具有生理和病理学重要性。我们已经研究了从喜马拉雅植物Leucosceptrum canum中分离得到的两种自然存在的酯基萜烯类化合物（亮氨酸酯基萜烯（化合物1）和亮氨酸内酯（化合物2））的抗血管生成潜力，并在初步筛选中被鉴定为具有生物活性。化合物1抑制成纤维细胞生长因子2诱导的增殖，伤口分析中的迁移，趋化性和小血管（人真皮）和大血管（牛主动脉）内皮细胞的管形成，而化合物2则大部分没有活性。两种化合物在使用鸡绒膜尿囊膜的体内血管生成模型中也具有活性。在没有成纤维细胞生长因子2的情况下，这两种化合物均未显示抑制活性。我们能够在结合试验中证明化合物1和2与成纤维​​细胞生长因子2受体1结合，其IC（50）值分别为1.4 +/- 0.956和132.47 +/- 7.90μM，同时下调磷酸化的ERK1 / 2，但不与受体2结合。化合物1的疏水性低于化合物2，这可能有助于其增加活性。化合物1是少数成纤维细胞生长因子2诱导的血管生成抑制剂的新添加。该化合物是特异性抑制剂，因为它对血管内皮生长因子或上皮生长因子诱导的血管生成没有影响。由于血管生成对于肿瘤发展至关重要，因此我们得出结论，这些化合物可能具有抗肿瘤作用。

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