Department of Bioengineering, Zunyi Medical University, Zhuhai Campus, Zhuhai, Guangdong 519041, China.
School of Life Sciences and Food Engineering, Hanshan Normal University, Chaozhou, Guangdong 521041, China.
J Nat Prod. 2021 Jun 25;84(6):1755-1762. doi: 10.1021/acs.jnatprod.1c00008. Epub 2021 May 24.
Angiogenesis is a complicated pathological process and plays an important role in modulating tumor development. Flavonoids, sharing the basic functional group with estrogen, have been utilized as chemopreventive agents to inhibit endothelial cell angiogenesis and also suppress tumor cell proliferation. Ononin, also referred to as formononetin-7-β-d-glucoside, is one of the bioactive chemicals found within many functional food or plants. The anticancer functions of ononin have been reported both and . However, the anti-angiogenetic properties of ononin have not been reported. The possible efficacies of ononin against angiogenesis was verified in cultured endothelial cells. Ononin suppressed vascular endothelial growth factor (VEGF)-induced HUVEC migration, invasion. and tube formation activity after 48 h. The apoptosis rate and specific markers, i.e., Bax/Bc-2 ratio, cleaved caspase 3/9 (Cl-caspase 3/9), and cytochrome c (Cyto c), were enhanced in the ononin-treated group. On the other hand, the protein expressions levels of hypoxia-inducible factor 1α (HIF-1α), mitogen-activated protein kinase kinase (MEK)/extracellular signal-regulated kinase (ERK), and vascular endothelial growth factor receptor 2 (VEGFR2) were restricted after ononin treatment for 2 days in VEGF-pretreated endothelial cells. In summary, ononin acts as a candidate for angiogenetic-related disease prevention and treatment.
血管生成是一个复杂的病理过程，在调节肿瘤发展中起着重要作用。黄酮类化合物与雌激素具有相同的基本官能团，已被用作化学预防剂来抑制内皮细胞血管生成，并抑制肿瘤细胞增殖。染料木黄酮，也称为芒柄花素-7-β-D-葡萄糖苷，是许多功能性食品或植物中发现的生物活性化学物质之一。染料木黄酮的抗癌功能已被 和 报道。然而，染料木黄酮的抗血管生成特性尚未被报道。在培养的内皮细胞中验证了染料木黄酮对血管生成的可能疗效。染料木黄酮抑制血管内皮生长因子（VEGF）诱导的 HUVEC 迁移、侵袭和管形成活性，作用 48 小时。在染料木黄酮处理组中，细胞凋亡率和特定标志物，即 Bax/Bc-2 比、裂解 caspase 3/9（Cl-caspase 3/9）和细胞色素 c（Cyto c）增加。另一方面，在 VEGF 预处理的内皮细胞中，用染料木黄酮处理 2 天后，缺氧诱导因子 1α（HIF-1α）、丝裂原活化蛋白激酶激酶（MEK）/细胞外信号调节激酶（ERK）和血管内皮生长因子受体 2（VEGFR2）的蛋白表达水平受到限制。总之，染料木黄酮可作为血管生成相关疾病预防和治疗的候选药物。
