Luo Yulin, Li Mengting, You Jingcan, Jiang Jun, Zeng Min, Luo Mao
Basic Medicine Research Innovation Center for Cardiometabolic Diseases, Clinical Trial Research Center, Ministry of Education, The Affiliated Traditional Chinese Medicine Hospital, Southwest Medical University, Luzhou, Sichuan, China.
Laboratory for Cardiovascular Pharmacology, Department of Pharmacology, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan, China.
Mol Biol Rep. 2025 Apr 29;52(1):437. doi: 10.1007/s11033-025-10532-0.
The phenotypic switch of vascular smooth muscle cells (VSMCs), characterized by the tissue-specific expression of certain microRNAs (miRNAs), is a critical factor in the development of diabetic vascular diseases. Metformin, a widely prescribed anti-diabetic medication for type 2 diabetes treatment, activates the adenosine monophosphate-activated protein kinase (AMPK) pathway and exerts a protective effect on vascular endothelium. Although the regulatory effects of metformin on the switch of the vascular smooth muscle cell phenotype have been identified, the specific role of miRNAs in this process remains unclear. We identified a specific miR-1 in response to metformin treatment and determined its effects on both miR-1 and its targets. Subsequently, we investigated the influence of these factors on the metformin-induced phenotype switch in vascular smooth muscle cells, specifically focusing on proliferation and migration, as well as activation of the AMPK/Transforming Growth Factor (TGF-β) axis. This was achieved using various methodologies, including bioinformatics analysis, quantitative real-time polymerase chain reaction (qRT-PCR), Western blot analysis, wound scratch assays, and Cell Counting Kit-8 assays. Our findings showed that metformin upregulated miR-1, which directly targets cyclin D1 (CCND1) in VSMCs. Metformin was observed to enhance the expression of contractile phenotype proteins, including α-smooth muscle actin (α-SMA) and smooth muscle myosin heavy chain (SMMHC), while simultaneously reducing the expression of proliferative phenotype proteins such as CCND1 and proliferating cell nuclear antigen (PCNA). The inhibition of miR-1 was found to reverse the effects of metformin on the phenotypic switch of VSMCs. This occurs partly through the AMPK/TGF-β signaling pathway and inhibits the migration and proliferation of VSMCs.
血管平滑肌细胞(VSMCs)的表型转换以某些微小RNA(miRNAs)的组织特异性表达为特征,是糖尿病血管疾病发展的关键因素。二甲双胍是一种广泛用于治疗2型糖尿病的抗糖尿病药物,它激活腺苷单磷酸激活蛋白激酶(AMPK)途径并对血管内皮发挥保护作用。尽管已经确定了二甲双胍对血管平滑肌细胞表型转换的调节作用,但miRNAs在这一过程中的具体作用仍不清楚。我们鉴定出一种对二甲双胍治疗有反应的特异性miR-1,并确定了其对miR-1及其靶标的影响。随后,我们研究了这些因素对二甲双胍诱导的血管平滑肌细胞表型转换的影响,特别关注增殖和迁移以及AMPK/转化生长因子(TGF-β)轴的激活。这是通过各种方法实现的,包括生物信息学分析、定量实时聚合酶链反应(qRT-PCR)、蛋白质免疫印迹分析、划痕试验和细胞计数试剂盒-8试验。我们的研究结果表明,二甲双胍上调miR-1,miR-1直接靶向血管平滑肌细胞中的细胞周期蛋白D1(CCND1)。观察到二甲双胍增强了收缩表型蛋白的表达,包括α-平滑肌肌动蛋白(α-SMA)和平滑肌肌球蛋白重链(SMMHC),同时降低了增殖表型蛋白如CCND1和增殖细胞核抗原(PCNA)的表达。发现抑制miR-1可逆转二甲双胍对血管平滑肌细胞表型转换的影响。这部分是通过AMPK/TGF-β信号通路发生的,并抑制血管平滑肌细胞的迁移和增殖。