Department of Physiology and Pathophysiology, School of Basic Medical Sciences, Center for Reproductive Medicine, Third Hospital, Peking University, Beijing, China.
Center of Basic Medical Research, Institute of Medical Innovation and Research, Peking University Third Hospital, Beijing, China.
Nat Commun. 2024 Jun 4;15(1):4755. doi: 10.1038/s41467-024-48954-2.
Non-alcoholic steatohepatitis (NASH) is a severe type of the non-alcoholic fatty liver disease (NAFLD). NASH is a growing global health concern due to its increasing morbidity, lack of well-defined biomarkers and lack of clinically effective treatments. Using metabolomic analysis, the most significantly changed active lipid sphingosine d18:1 [So(d18:1)] is selected from NASH patients. So(d18:1) inhibits macrophage HIF-2α as a direct inhibitor and promotes the inflammatory factors secretion. Male macrophage-specific HIF-2α knockout and overexpression mice verified the protective effect of HIF-2α on NASH progression. Importantly, the HIF-2α stabilizer FG-4592 alleviates liver inflammation and fibrosis in NASH, which indicated that macrophage HIF-2α is a potential drug target for NASH treatment. Overall, this study confirms that So(d18:1) promotes NASH and clarifies that So(d18:1) inhibits the transcriptional activity of HIF-2α in liver macrophages by suppressing the interaction of HIF-2α with ARNT, suggesting that macrophage HIF-2α may be a potential target for the treatment of NASH.
非酒精性脂肪性肝炎(NASH)是一种严重的非酒精性脂肪性肝病(NAFLD)。由于发病率不断上升、缺乏明确的生物标志物以及缺乏临床有效的治疗方法,NASH 成为了一个日益严重的全球健康问题。通过代谢组学分析,从 NASH 患者中选择出变化最显著的活性脂质神经酰胺 d18:1[So(d18:1)]。So(d18:1)作为一种直接抑制剂抑制巨噬细胞 HIF-2α,促进炎症因子的分泌。雄性巨噬细胞特异性 HIF-2α 敲除和过表达小鼠验证了 HIF-2α对 NASH 进展的保护作用。重要的是,HIF-2α 稳定剂 FG-4592 可减轻 NASH 中的肝炎症和纤维化,这表明巨噬细胞 HIF-2α 可能是 NASH 治疗的潜在药物靶点。总的来说,这项研究证实了 So(d18:1)促进了 NASH 的发生,并阐明了 So(d18:1)通过抑制 HIF-2α与 ARNT 的相互作用抑制了肝巨噬细胞中 HIF-2α 的转录活性,提示巨噬细胞 HIF-2α 可能是治疗 NASH 的潜在靶点。