Xu Jin, Li Yan, Yao Shun, Jin Xiuxiu, Yang Mingzhu, Guo Qingge, Qiu Ruiqi, Lei Bo
Zhengzhou University People's Hospital, Henan Provincial People's Hospital, Zhengzhou 450003, China.
Academy of Medical Sciences, Zhengzhou University, Zhengzhou 450052, China.
Biomedicines. 2024 Sep 4;12(9):2020. doi: 10.3390/biomedicines12092020.
Increased or altered mitochondrial ROS production in the retinal ganglion cells is regarded as the chief culprit of the disease-causing Leber's hereditary optic neuropathy (LHON). SkQ1 is a rechargeable mitochondria-targeted antioxidant with high specificity and efficiency. SkQ1 has already been used to treat LHON patients, and a phase 2a randomized clinical trial of SkQ1 has demonstrated improvements in eyesight. However, the underlying mechanism of SkQ1 in LHON remains unclear. This study aimed to assess the effects and molecular mechanism of SkQ1 in the preservation of mitochondrial function using skin fibroblasts derived from LHON patients. Our study found that SkQ1 could reduce ROS production and stabilize the mitochondrial membrane. Mechanistically, through network pharmacology and molecular docking, we identified the key targets of SkQ1 as SOD2 and PINK1, which play crucial roles in redox and mitophagy. SkQ1 interacted with PINK1 and downregulated its expression to balance mitochondrial homeostasis. Collectively, the findings of our study reveal that by regulating PINK1/PRKN-mediated mitophagy, SkQ1 preserves mitochondrial function in LHON fibroblasts. The data indicate that SkQ1 may be a novel therapeutic intervention to prevent the progression of LHON.
视网膜神经节细胞中线粒体活性氧生成增加或改变被认为是导致Leber遗传性视神经病变(LHON)的主要原因。SkQ1是一种具有高特异性和高效性的可充电线粒体靶向抗氧化剂。SkQ1已被用于治疗LHON患者,并且SkQ1的一项2a期随机临床试验已证明视力有所改善。然而,SkQ1在LHON中的潜在机制仍不清楚。本研究旨在使用来自LHON患者的皮肤成纤维细胞评估SkQ1在维持线粒体功能方面的作用和分子机制。我们的研究发现SkQ1可以减少活性氧生成并稳定线粒体膜。从机制上讲,通过网络药理学和分子对接,我们确定SkQ1的关键靶点为SOD2和PINK1,它们在氧化还原和线粒体自噬中起关键作用。SkQ1与PINK1相互作用并下调其表达以平衡线粒体稳态。总体而言,我们的研究结果表明,通过调节PINK1/PRKN介导的线粒体自噬,SkQ1可维持LHON成纤维细胞中的线粒体功能。数据表明SkQ1可能是一种预防LHON进展的新型治疗干预措施。