Dipartimento di Produzioni Animali, Biotecnologie Veterinarie, Qualità e Sicurezza degli Alimenti-Sezione di Fisiologia Veterinaria, Università degli Studi di Parma, Via del Taglio 10, 43126 Parma, Italy.
Invest New Drugs. 2012 Feb;30(1):186-90. doi: 10.1007/s10637-010-9550-z. Epub 2010 Oct 6.
Angiogenesis is normally a highly regulated process that occurs during development, reproduction, and wound repair. However, angiogenesis can also become a fundamental pathogenic process in cancer and several other diseases. To date, the synthesis of angiogenesis inhibitors has been researched in several ways also starting from bioactive plant compounds. In the present study, we tested both in an angiogenesis bioassay and in ovarian cell culture, the potential antiangiogenic effect of a natural-derived benzo[k,l]xanthene lignan (5). This unusual compound was synthesized through the biomimetic dimerization of CAPE (caffeic acid phenethyl ester), a bioactive component of honeybee propolis. The lignan showed a significant, dose-related inhibitory effect on new vessel growth in the angiogenesis bioassay and it inhibited Vascular Endothelial Growth Factor secretion in ovarian cell culture. Therefore, we indicate the natural-derived benzo[k,l]xanthene lignan 5 as a potential new angiogenesis inhibitor.
血管生成通常是一个高度受调控的过程，发生在发育、繁殖和伤口修复过程中。然而，血管生成也可能成为癌症和其他几种疾病的基本病理过程。迄今为止，已经通过多种方法研究了血管生成抑制剂的合成，也从生物活性植物化合物开始。在本研究中，我们在血管生成生物测定和卵巢细胞培养中都测试了天然衍生的苯并[k,l]呫吨木质素（5）的潜在抗血管生成作用。该不寻常的化合物是通过 CAPE（咖啡酸苯乙酯）的仿生二聚化合成的，CAPE 是蜂胶的一种生物活性成分。木质素在血管生成生物测定中对新血管生长表现出显著的、剂量相关的抑制作用，并抑制卵巢细胞培养中的血管内皮生长因子分泌。因此，我们将天然衍生的苯并[k,l]呫吨木质素 5 作为一种有潜力的新血管生成抑制剂。
