Affiliated Eye Hospital of Nanchang University, Jiangxi Research Institute of Ophthalmology and Visual Science, Nanchang, China.
Affiliated Eye Hospital of Nanchang University, Jiangxi Research Institute of Ophthalmology and Visual Science, Nanchang, China; Queen Mary School of Nanchang University, Nanchang, China.
Eur J Pharmacol. 2020 Oct 5;884:173369. doi: 10.1016/j.ejphar.2020.173369. Epub 2020 Jul 24.
Glaucoma is a progressive optic neuropathy that has become the most common cause of irreversible blindness worldwide. Studies have shown that the protein mammalian target of rapamycin (mTOR) is a serine/threonine kinase that plays a central role in regulating numerous functions, such as growth, proliferation, cytoskeletal organization, metabolism, and autophagy. Clinical trials have shown that Rho-associated protein kinase (ROCK) inhibitors reduced intraocular pressure (IOP) in patients with glaucoma and ocular hypertension (OHT). In this study, we explored whether rapamycin (RAPA) eye drops can reduce IOP and protect retinal ganglion cells (RGCs). Our results indicated that in rats treated with RAPA, the drug was detected in the aqueous humor (AH), and the IOP was reduced. This may be related to the inhibition of RhoA protein activation by RAPA and regulation of the actin cytoskeleton in trabecular meshwork (TM) cells. In addition, the retinal thickness and the survival rate of RGCs were significantly reduced in the OHT group compared with the control group. These changes in the OHT group were significantly improved after treatment with RAPA. This may be because RAPA inhibited the activation of glial cells and the release of proinflammatory factors, thereby attenuating further damage to the retina and RGCs. Taken together, the results of this study demonstrated that RAPA not only reduced IOP but also protected RGCs, suggesting that RAPA is likely to be an effective strategy for the treatment of glaucoma.
青光眼是一种进行性视神经病变,已成为全球最常见的不可逆性失明原因。研究表明,哺乳动物雷帕霉素靶蛋白(mTOR)是一种丝氨酸/苏氨酸激酶,在调节多种功能中发挥核心作用,如生长、增殖、细胞骨架组织、代谢和自噬。临床试验表明,Rho 相关蛋白激酶(ROCK)抑制剂可降低青光眼和高眼压(OHT)患者的眼内压(IOP)。在这项研究中,我们探讨了雷帕霉素(RAPA)滴眼剂是否可以降低 IOP 并保护视网膜神经节细胞(RGCs)。我们的结果表明,在接受 RAPA 治疗的大鼠中,药物在房水中被检测到,IOP 降低。这可能与 RAPA 抑制 RhoA 蛋白激活和调节小梁网(TM)细胞中的肌动蛋白细胞骨架有关。此外,与对照组相比,OHT 组的视网膜厚度和 RGCs 的存活率明显降低。在接受 RAPA 治疗后,OHT 组的这些变化得到了显著改善。这可能是因为 RAPA 抑制了神经胶质细胞的激活和促炎因子的释放,从而减轻了对视网膜和 RGCs 的进一步损伤。综上所述,本研究结果表明,RAPA 不仅降低了 IOP,还保护了 RGCs,提示 RAPA 可能是治疗青光眼的有效策略。