Department of Pharmacology, Ribeirao Preto Medical School, University of Sao Paulo, 14049-900 Ribeirao Preto, Brazil.
Health Sciences Special Academic Unit, Federal University of Jatai, 75804-020 Jataí, Brazil.
Int J Mol Sci. 2021 Jun 7;22(11):6154. doi: 10.3390/ijms22116154.
High levels of aldosterone (Aldo) trigger oxidative stress and vascular dysfunction independent of effects on blood pressure. We sought to determine whether Aldo disrupts Nrf2 signaling, the main transcriptional factor involved in antioxidant responses that aggravate cell injury. Thoracic aorta from male C57Bl/6J mice and cultured human endothelial cells (EA.hy926) were stimulated with Aldo (100 nM) in the presence of tiron [reactive oxygen species (ROS) scavenger, eplerenone [mineralocorticoid receptor (MR) antagonist], and L-sulforaphane (SFN; Nrf2 activator). Thoracic aortas were also isolated from mice infused with Aldo (600 μg/kg per day) for 14 days. Aldo decreased endothelium-dependent vasorelaxation and increased ROS generation, effects prevented by tiron and MR blockade. Pharmacological activation of Nrf2 with SFN abrogated Aldo-induced vascular dysfunction and ROS generation. In EA.hy926 cells, Aldo increased ROS generation, which was prevented by eplerenone, tiron, and SFN. At short times, Aldo-induced ROS generation was linked to increased Nrf2 activation. However, after three hours, Aldo decreased the nuclear accumulation of Nrf2. Increased Keap1 protein expression, but not activation of p38 MAPK, was linked to Aldo-induced reduced Nrf2 activity. Arteries from Aldo-infused mice also exhibited decreased nuclear Nrf2 and increased Keap1 expression. Our findings suggest that Aldo reduces vascular Nrf2 transcriptional activity by Keap1-dependent mechanisms, contributing to mineralocorticoid-induced vascular dysfunction.
醛固酮(Aldo)水平升高会引发氧化应激和血管功能障碍,而与血压影响无关。我们试图确定 Aldo 是否会破坏 Nrf2 信号转导,Nrf2 是参与抗氧化反应的主要转录因子,而这些反应会加重细胞损伤。我们用 Aldo(100 nM)刺激雄性 C57Bl/6J 小鼠的胸主动脉和培养的人内皮细胞(EA.hy926),并在其中加入 tiron(活性氧(ROS)清除剂)、依普利酮(盐皮质激素受体(MR)拮抗剂)和 L-苏氨酸(SFN;Nrf2 激活剂)。我们还从接受 Aldo(每天 600 μg/kg)输注 14 天的小鼠中分离出胸主动脉。Aldo 降低了内皮依赖性血管舒张功能,增加了 ROS 的产生,这些作用可被 tiron 和 MR 阻断所预防。用 SFN 对 Nrf2 进行药理激活可消除 Aldo 诱导的血管功能障碍和 ROS 的产生。在 EA.hy926 细胞中,Aldo 增加了 ROS 的产生,而依普利酮、tiron 和 SFN 可预防这种增加。在短时间内,Aldo 诱导的 ROS 产生与 Nrf2 激活增加有关。然而,三小时后,Aldo 减少了 Nrf2 的核积累。Keap1 蛋白表达增加,但 p38 MAPK 未激活,与 Aldo 诱导的 Nrf2 活性降低有关。接受 Aldo 输注的小鼠的动脉也表现出核 Nrf2 减少和 Keap1 表达增加。我们的研究结果表明,Aldo 通过 Keap1 依赖性机制降低血管 Nrf2 的转录活性,导致盐皮质激素诱导的血管功能障碍。