Zhao Fangqing, Niu Xuan, Song Ge, Wang Lijie, Fu Yisheng, Li Shuwen, Gu Xinxin, Wang Qingkun, Luo Jiao
School of Public Health, Qingdao University, 308 Ningxia Road, Qingdao, 266071, Shandong, China.
J Transl Med. 2025 Jul 22;23(1):810. doi: 10.1186/s12967-025-06880-x.
Liver fibrosis is a progressive pathological process primarily driven by the transdifferentiation of hepatic stellate cells (HSCs) into myofibroblast-like cells which secrete excessive extracellular matrix (ECM). Although microRNAs (miRNAs) have emerged as key regulators of fibrogenesis, the therapeutic potential and mechanistic specificity of miR-214-3p (miR-214) in liver fibrosis remain insufficiently defined.
An adeno-associated virus (AAV)-based system was used to achieve either whole-liver or HSC-specific overexpression of miR-214 (via GFAP promoter) in a mouse model of alcohol-associated liver fibrosis induced by Lieber-DeCarli ethanol diet combined with low-dose CCl₄ injection. Liver fibrosis, steatosis, and inflammation were evaluated by biochemical assays, histology, immunostaining, and gene expression analyses. In vitro, stable miR-214 overexpression and knockdown in LX-2 cells were performed to assess effects on HSC proliferation, transdifferentiation, and ECM gene expression. MECP2 was identified as a direct functional target of miR-214 by bioinformatics and luciferase reporter assays.
miR-214 expression was significantly downregulated during HSC activation in vitro and in fibrotic livers. Whole-liver overexpression of miR-214 alleviated liver fibrosis but caused undesirable steatosis and inflammation. Notably, HSC-specific miR-214 overexpression ameliorated liver fibrosis without inducing these adverse effects. Functionally, miR-214 inhibited HSC proliferation and ECM gene expression, while its inhibition promoted this process. Mechanistically, miR-214 exerts its anti-fibrosis function at least in part by directing targeting MECP2, a critical regulator for HSC activation.
These findings not only identify miR-214 as a promising antifibrotic agent, but also highlight the translational advantage of cell-specific miRNA delivery. HSC-targeted miR-214 gene therapy may offer a promising and safer approach for treating liver fibrosis.
肝纤维化是一种进行性病理过程,主要由肝星状细胞(HSC)转分化为分泌过量细胞外基质(ECM)的肌成纤维细胞样细胞所驱动。尽管微小RNA(miRNA)已成为纤维化形成的关键调节因子,但miR-214-3p(miR-214)在肝纤维化中的治疗潜力和机制特异性仍未得到充分阐明。
在由Lieber-DeCarli乙醇饮食联合低剂量四氯化碳注射诱导的酒精性肝纤维化小鼠模型中,使用基于腺相关病毒(AAV)的系统通过胶质纤维酸性蛋白(GFAP)启动子实现miR-214在全肝或HSC特异性过表达。通过生化分析、组织学、免疫染色和基因表达分析评估肝纤维化、脂肪变性和炎症。在体外,在LX-2细胞中进行miR-214的稳定过表达和敲低,以评估对HSC增殖、转分化和ECM基因表达的影响。通过生物信息学和荧光素酶报告基因检测确定甲基化CpG结合蛋白2(MECP2)为miR-214的直接功能靶点。
在体外HSC激活过程中以及在纤维化肝脏中,miR-214表达显著下调。miR-214的全肝过表达减轻了肝纤维化,但导致了不良的脂肪变性和炎症。值得注意的是,HSC特异性miR-214过表达改善了肝纤维化而未诱导这些不良反应。在功能上,miR-214抑制HSC增殖和ECM基因表达,而其抑制则促进了这一过程。在机制上,miR-214至少部分通过直接靶向MECP2发挥其抗纤维化功能,MECP2是HSC激活的关键调节因子。
这些发现不仅将miR-214确定为一种有前景的抗纤维化药物,还突出了细胞特异性miRNA递送的转化优势。靶向HSC的miR-214基因治疗可能为治疗肝纤维化提供一种有前景且更安全的方法。