Sun Tong, Yu Haiyang, Zhang Dingning, Zhang Dan, Li Danni, Fu Jianhua
Department of Pediatrics, Shengjing Hospital of China Medical University, Shenyang, Liaoning, China.
Department of Neurology, Shengjing Hospital of China Medical University, Shenyang, Liaoning, China.
Redox Biol. 2025 May;82:103586. doi: 10.1016/j.redox.2025.103586. Epub 2025 Mar 6.
Many studies have reported the important role of glucagon-like peptide-1 receptor (GLP-1R) in regulating glucose homeostasis. However, in addition to the pancreas, GLP-1R is distributed in organs such as the lungs. A few researches have reported the mechanism of action of GLP-1R in acute and chronic lung diseases. Nevertheless, its effect on lung development remains unclear. In this research, we aimed to explore the role of GLP-1R in regulating lung development and its potential mechanisms in in vivo and in vitro bronchopulmonary dysplasia (BPD) models.
Neonatal Sprague-Dawley rats were divided into hyperoxia (FIO2 = 0.85) and control (FIO2 = 0.21) groups. Lung tissues were extracted at 3, 7, 10, and 14 postnatal days and subjected to hematoxylin and eosin staining for histopathological and morphological observation. Single-cell RNA sequencing was performed to explore the role of GLP-1R in lung development. Western blotting was conducted to assess the expression of GLP-1R, dynamin-related protein 1 (DRP1), and glycolysis-associated enzymes, including phosphofructokinase (PFKM), hexokinase 2 (HK2), and lactate dehydrogenase A (LDHA), in the lung tissues, primary alveolar type II (ATII) cells, and RLE-6TN cells. Double immunofluorescence staining was performed to confirm the co-localization of GLP-1R, DRP1, and ATII cells. A Seahorse XF96 metabolic extracellular flux analyzer was used to perform real-time analyses of extracellular acidification rate and oxygen consumption rate in ATII cells isolated from lung tissues and RLE-6TN cells. The adenosine triphosphate (ATP) concentrations in ATII and RLE-6TN cells were measured using an ATP kit. Mitochondria were stained with MitoTracker and observed using HiS-SIM. GLP-1R gene levels in lung tissues, primary ATII cells, and RLE-6TN cells were tested using RT-qPCR. We used MeRIP-qPCR to determine the m6A modification level of GLP-1R mRNA in RLE-6TN cells. A reporter gene was used to verify the modification site and key methyltransferases.
We observed that GLP-1R signaling regulates lung development and plays a key role in ATII cells, particularly after birth. Hyperoxia inhibits GLP-1R protein and gene expression in ATII cells and accelerates BPD development. ATP production decreased and glycolysis levels increased in ATII cells under hyperoxia. Activation of GLP-1R signaling promotes ATP production and downregulates glycolysis by regulating DRP1 induced mitochondria fission. In RLE-6TN cells, we verified that the m6A modification level of GLP-1R mRNA decreased; the modification site was tested by MeRIP-qPCR and was primarily induced by the methyltransferase-like 14 (METTL14).
GLP-1R is primarily expressed in ATII cells of neonatal rats and can promote lung development during the early postnatal period. The GLP-1R signaling pathway modulates mitochondrial fission and glucose metabolism in ATII cells under hyperoxia. Hyperoxia can inhibit the activation of GLP-1R by inhibiting m6A methylation during BPD pathogenesis.
许多研究报道了胰高血糖素样肽-1受体(GLP-1R)在调节葡萄糖稳态中的重要作用。然而,除胰腺外,GLP-1R还分布于肺等器官。少数研究报道了GLP-1R在急慢性肺部疾病中的作用机制。然而,其对肺发育的影响仍不清楚。在本研究中,我们旨在探讨GLP-1R在体内和体外支气管肺发育不良(BPD)模型中调节肺发育的作用及其潜在机制。
将新生Sprague-Dawley大鼠分为高氧组(FIO2 = 0.85)和对照组(FIO2 = 0.21)。在出生后第3、7、10和14天提取肺组织,进行苏木精和伊红染色,用于组织病理学和形态学观察。进行单细胞RNA测序,以探讨GLP-1R在肺发育中的作用。进行蛋白质免疫印迹法,以评估肺组织、原代II型肺泡上皮(ATII)细胞和RLE-6TN细胞中GLP-1R、动力相关蛋白1(DRP1)以及糖酵解相关酶(包括磷酸果糖激酶(PFKM)、己糖激酶2(HK2)和乳酸脱氢酶A(LDHA))的表达。进行双重免疫荧光染色,以确认GLP-1R、DRP1和ATII细胞的共定位。使用海马XF96代谢细胞外通量分析仪对从肺组织和RLE-6TN细胞中分离出的ATII细胞的细胞外酸化率和氧消耗率进行实时分析。使用ATP试剂盒测量ATII和RLE-6TN细胞中的三磷酸腺苷(ATP)浓度。用MitoTracker对线粒体进行染色,并使用HiS-SIM进行观察。使用RT-qPCR检测肺组织、原代ATII细胞和RLE-6TN细胞中GLP-基因水平。我们使用MeRIP-qPCR来确定RLE-6TN细胞中GLP-1R mRNA的m6A修饰水平。使用报告基因验证修饰位点和关键甲基转移酶。
我们观察到GLP-1R信号通路调节肺发育,并在ATII细胞中起关键作用,尤其是在出生后。高氧抑制ATII细胞中GLP-1R蛋白和基因表达,并加速BPD的发展。在高氧条件下,ATII细胞中的ATP生成减少且糖酵解水平增加。GLP-1R信号通路的激活通过调节DRP1诱导的线粒体分裂来促进ATP生成并下调糖酵解。在RLE-6TN细胞中,我们验证了GLP-1R mRNA的m6A修饰水平降低;通过MeRIP-qPCR检测修饰位点,主要由甲基转移酶样14(METTL14)诱导。
GLP-1R主要在新生大鼠的ATII细胞中表达,并可在出生后早期促进肺发育。在高氧条件下,GLP-1R信号通路调节ATII细胞中的线粒体分裂和葡萄糖代谢。在BPD发病机制中,高氧可通过抑制m6A甲基化来抑制GLP-1R的激活。