Natural Products Research Institute, College of Pharmacy, Seoul National University, Gwanak-gu, Seoul 151-742, Republic of Korea.
Int J Oncol. 2013 Aug;43(2):600-10. doi: 10.3892/ijo.2013.1959. Epub 2013 May 24.
Magnolol, a neolignan from the traditional medicinal plant Magnolia obovata, has been shown to possess neuroprotective, anti-inflammatory, anticancer and anti-angiogenic activities. However, the precise mechanism of the anti-angiogenic activity of magnolol remains to be elucidated. In the present study, the anti-angiogenic effect of magnolol was evaluated in mouse embryonic stem (mES)/embryoid body (EB)-derived endothelial-like cells. The endothelial-like cells were obtained by differentiation from mES/EB cells. Magnolol (20 µM) significantly suppressed the transcriptional and translational expression of platelet endothelial cell adhesion molecule (PECAM), an endothelial biomarker, in mES/EB-derived endothelial-like cells. To further understand the molecular mechanism of the suppression of PECAM expression, signaling pathways were analyzed in the mES/EB-derived endothelial-like cells. Magnolol induced the generation of reactive oxygen species (ROS) by mitochondria, a process that was associated with the induction of apoptosis as determined by positive Annexin V staining and the activation of cleaved caspase-3. The involvement of ROS generation by magnolol was confirmed by treatment with an antioxidant, N-acetyl-cysteine (NAC). NAC inhibited the magnolol-mediated induction of ROS generation and suppression of PECAM expression. In addition, magnolol suppressed the activation of MAPKs (ERK, JNK and p38) and the PI3K/AKT/mTOR signaling pathway in mES/EB-derived endothelial-like cells. Taken together, these findings demonstrate for the first time that the anti-angiogenic activity of magnolol may be associated with ROS-mediated apoptosis and the suppression of the PI3K/AKT/mTOR signaling pathway in mES/EB-derived endothelial-like cells.
厚朴酚是一种来自传统药用植物厚朴的新木脂素,已被证明具有神经保护、抗炎、抗癌和抗血管生成活性。然而,厚朴酚抗血管生成活性的确切机制仍有待阐明。在本研究中,评估了厚朴酚在小鼠胚胎干细胞(mES)/胚胎体(EB)衍生的内皮样细胞中的抗血管生成作用。内皮样细胞通过 mES/EB 细胞的分化获得。厚朴酚(20µM)显著抑制 mES/EB 衍生的内皮样细胞中血小板内皮细胞黏附分子(PECAM)的转录和翻译表达,PECAM 是一种内皮生物标志物。为了进一步了解抑制 PECAM 表达的分子机制,分析了 mES/EB 衍生的内皮样细胞中的信号通路。厚朴酚通过线粒体诱导活性氧(ROS)的产生,这一过程与通过阳性 Annexin V 染色和切割的 caspase-3 的激活来确定的细胞凋亡的诱导相关。通过用抗氧化剂 N-乙酰半胱氨酸(NAC)处理来证实厚朴酚诱导的 ROS 产生。NAC 抑制了厚朴酚介导的 ROS 生成和 PECAM 表达的抑制。此外,厚朴酚抑制了 mES/EB 衍生的内皮样细胞中 MAPKs(ERK、JNK 和 p38)和 PI3K/AKT/mTOR 信号通路的激活。总之,这些发现首次表明,厚朴酚的抗血管生成活性可能与 ROS 介导的凋亡和抑制 mES/EB 衍生的内皮样细胞中的 PI3K/AKT/mTOR 信号通路有关。