Kim Jin, Moon Seo Yun, Kang Ho Geun, Kim Hee Jong, Choi Jun Sub, Lee Steven Hyun Seung, Park Keerang, Won So-Yoon
Institute of New Drug Development Research, CdmoGen Co., Ltd, Seoul, 05855, Republic of Korea.
CdmoGen Co., Ltd, Cheongju, 28577, Republic of Korea.
Sci Rep. 2025 Mar 19;15(1):9517. doi: 10.1038/s41598-025-93993-4.
Age-related macular degeneration (AMD) is a prevalent retinal disorder that leads to central vision loss, mainly due to chronic inflammation. Tumor necrosis factor-alpha (TNF-α) is a critical mediator of inflammatory responses within the retinal environment. This study has investigated TNF-α's influence on inflammatory cytokine production and endothelial barrier integrity in human microglial (HMC3) and endothelial (HUVEC) cells. We found that TNF-α significantly elevated the expression and secretion of interleukin-6 (IL-6) and interleukin-1β (IL-1β) in HMC3 cells and disrupted endothelial tight junctions in HUVECs, as evidenced by weakened ZO-1 staining and compromised barrier function. To mitigate these effects and further investigate the in vitro mechanism of actions in CRG-01's in vivo therapeutic efficacy of anti-inflammation, we employed AAV2-shmTOR, CRG-01, as the candidate for therapeutic vector targeting the mammalian target of the rapamycin (mTOR) pathway. TNF-α-induced IL-6, IL-1β, and NF-κB signaling in HMC3 cells were significantly reduced by AAV2-shmTOR treatment, which may present a promising avenue for the fight against AMD. It also effectively preserved endothelial tight junction integrity in TNF-α-treated HUVECs, providing reassurance about its effectiveness. Furthermore, the supernatant medium collected from AAV2-shmTOR-treated HMC3 cells decreased oxidative stress, protein oxidation, and cytotoxicity in ARPE retinal pigment epithelial cells. These results strongly suggested that CRG-01, the candidate therapeutic vector of AAV2-shmTOR, may have a therapeutic potential to treat AMD-related retinal inflammation.
年龄相关性黄斑变性(AMD)是一种常见的视网膜疾病,主要由于慢性炎症导致中心视力丧失。肿瘤坏死因子-α(TNF-α)是视网膜环境中炎症反应的关键介质。本研究调查了TNF-α对人小胶质细胞(HMC3)和内皮细胞(HUVEC)中炎症细胞因子产生和内皮屏障完整性的影响。我们发现,TNF-α显著提高了HMC3细胞中白细胞介素-6(IL-6)和白细胞介素-1β(IL-1β)的表达和分泌,并破坏了HUVECs中的内皮紧密连接,这通过ZO-1染色减弱和屏障功能受损得以证明。为了减轻这些影响并进一步研究CRG-01体内抗炎治疗效果的体外作用机制,我们采用AAV2-shmTOR,即CRG-01,作为靶向雷帕霉素哺乳动物靶点(mTOR)途径的治疗载体候选物。AAV2-shmTOR处理显著降低了TNF-α诱导的HMC3细胞中的IL-6、IL-1β和NF-κB信号传导,这可能为对抗AMD提供一个有前景的途径。它还有效保持了TNF-α处理的HUVECs中的内皮紧密连接完整性,证明了其有效性。此外,从AAV2-shmTOR处理的HMC3细胞收集的上清培养基降低了ARPE视网膜色素上皮细胞中的氧化应激、蛋白质氧化和细胞毒性。这些结果强烈表明,AAV2-shmTOR的候选治疗载体CRG-01可能具有治疗AMD相关视网膜炎症的潜力。