Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, Fort Worth, TX 76107, USA.
North Texas Eye Research Institute, University of North Texas Health Science Center, Fort Worth, TX 76107, USA.
Int J Mol Sci. 2023 Jul 17;24(14):11557. doi: 10.3390/ijms241411557.
Oxidative stress (OS)-induced mitochondrial damage is a risk factor for primary open-angle glaucoma (POAG). Mitochondria-targeted novel antioxidant therapies could unearth promising drug candidates for the management of POAG. Previously, our dual-acting hybrid molecule SA-2 with nitric oxide-donating and antioxidant activity reduced intraocular pressure and improved aqueous humor outflow in rodent eyes. Here, we examined the mechanistic role of SA-2 in trabecular meshwork (TM) cells in vitro and measured the activity of intracellular antioxidant enzymes during OS. Primary human TM cells isolated from normal (hNTM) or glaucomatous (hGTM) post-mortem donors and transformed glaucomatous TM cells (GTM-3) were used for in vitro assays. We examined the effect of SA-2 on oxygen consumption rate (OCR) and extracellular acidification rate (ECAR) in vitro using Seahorse Analyzer with or without the oxidant, tert-butyl hydroperoxide (TBHP) treatment. Concentrations of total antioxidant enzymes, catalase (CAT), malondialdehyde (MDA), and glutathione peroxidase (GPx) were measured. We observed significant protection of both hNTM and hGTM cells from TBHP-induced cell death by SA-2. Antioxidant enzymes were elevated in SA-2-treated cells compared to TBHP-treated cells. In addition, SA-2 demonstrated an increase in mitochondrial metabolic parameters. Altogether, SA-2 protected both normal and glaucomatous TM cells from OS via increasing mitochondrial energy parameters and the activity of antioxidant enzymes.
氧化应激 (OS) 诱导的线粒体损伤是原发性开角型青光眼 (POAG) 的一个风险因素。靶向线粒体的新型抗氧化治疗方法可能为 POAG 的治疗挖掘出有前途的药物候选物。此前,我们具有一氧化氮供体和抗氧化活性的双重作用杂合分子 SA-2 降低了啮齿动物眼内压并改善了房水流出。在这里,我们研究了 SA-2 在体外小梁网 (TM) 细胞中的作用机制,并在 OS 期间测量了细胞内抗氧化酶的活性。从正常 (hNTM) 或青光眼 (hGTM) 死后供体分离的原代人 TM 细胞和转化的青光眼 TM 细胞 (GTM-3) 用于体外测定。我们使用 Seahorse 分析仪在有或没有氧化剂叔丁基过氧化氢 (TBHP) 处理的情况下,检测了 SA-2 对体外耗氧量 (OCR) 和细胞外酸化率 (ECAR) 的影响。测量了总抗氧化酶、过氧化氢酶 (CAT)、丙二醛 (MDA) 和谷胱甘肽过氧化物酶 (GPx) 的浓度。我们观察到 SA-2 对 TBHP 诱导的 hNTM 和 hGTM 细胞死亡有明显的保护作用。与 TBHP 处理的细胞相比,SA-2 处理的细胞中的抗氧化酶升高。此外,SA-2 显示出线粒体代谢参数的增加。总之,SA-2 通过增加线粒体能量参数和抗氧化酶的活性来保护正常和青光眼 TM 细胞免受 OS 影响。