Department of Pharmacology, School of Medicine, Chung Shan Medical University, No. 110, Sec. 1, Jianguo N. Rd., Taichung, 402, Taiwan, ROC.
Department of Pharmacy, Chung Shan Medical University Hospital, Taichung, Taiwan.
Arch Toxicol. 2024 Jul;98(7):2247-2259. doi: 10.1007/s00204-024-03751-0. Epub 2024 Apr 18.
3-Bromofluoranthene (3-BrFlu) is the secondary metabolite of fluoranthene, which is classified as a polycyclic aromatic hydrocarbon, through bromination and exists in the fine particulate matter of air pollutants. Endothelial dysfunction plays a critical role in the pathogenesis of cardiovascular and vascular diseases. Little is known about the molecular mechanism of 3-BrFlu on endothelial dysfunction in vivo and in vitro assay. In the present study, 3-BrFlu included concentration-dependent changes in ectopic angiogenesis of the sub-intestinal vein and dilation of the dorsal aorta in zebrafish. Disruption of vascular endothelial integrity and up-regulation of vascular endothelial permeability were also induced by 3-BrFlu in a concentration-dependent manner through pro-inflammatory responses in vascular endothelial cells, namely, SVEC4-10 cells. Generation of pro-inflammatory mediator PGE2 was induced by 3-BrFlu through COX2 expression. Expression of COX2 and generation of pro-inflammatory cytokines, including TNFα and IL-6, were induced by 3-BrFlu through phosphorylation of NF-κB p65, which was mediated by phosphorylation of MAPK, including p38 MAPK, ERK and JNK. Furthermore, generation of intracellular ROS was induced by 3-BrFlu, which is associated with the down-regulated activities of the antioxidant enzyme (AOE), including SOD and catalase. We also found that 3-BrFlu up-regulated expression of the AOE and HO-1 induced by 3-BrFlu through Nrf-2 expression. However, the 3-BrFlu-induced upregulation of AOE and HO-1 expression could not be revised the responses of vascular endothelial dysfunction. In conclusion, 3-BrFlu is a hazardous substance that results in vascular endothelial dysfunction through the MAPK-mediated-NFκB pro-inflammatory pathway and intracellular ROS generation.
3-溴荧蒽(3-BrFlu)是荧蒽的次生代谢物,属于多环芳烃,通过溴化作用存在于空气污染物的细颗粒物中。内皮功能障碍在心血管和血管疾病的发病机制中起着关键作用。目前,对于 3-BrFlu 对体内和体外内皮功能障碍的分子机制知之甚少。在本研究中,3-BrFlu 导致斑马鱼的肠道下静脉异位血管生成和背主动脉扩张呈浓度依赖性变化。通过血管内皮细胞的促炎反应,3-BrFlu 还以浓度依赖性方式破坏血管内皮完整性并上调血管内皮通透性,即 SVEC4-10 细胞。通过 COX2 表达,3-BrFlu 诱导促炎介质 PGE2 的产生。通过 MAPK(包括 p38 MAPK、ERK 和 JNK)介导的 NF-κB p65 的磷酸化,3-BrFlu 诱导 COX2 和促炎细胞因子 TNFα 和 IL-6 的表达。此外,3-BrFlu 诱导细胞内 ROS 的产生,这与抗氧化酶(AOE)的活性下调有关,包括 SOD 和过氧化氢酶。我们还发现,3-BrFlu 通过 Nrf-2 表达上调 3-BrFlu 诱导的 AOE 和 HO-1 的表达。然而,3-BrFlu 诱导的 AOE 和 HO-1 表达的上调并不能修正血管内皮功能障碍的反应。总之,3-BrFlu 是一种有害物质,通过 MAPK 介导的 NFκB 促炎途径和细胞内 ROS 的产生导致血管内皮功能障碍。