Kim Jun-Sik, Jun Jae Hyun, Lee Jeongmi, Park Sunyoung, Kim Eunae, Hwang Su Jung, Moon Heesu, Baek Seung Hyun, Kim Hark Kyun, Park Jinsu, Cho Yoonsuk, Han Jihoon, Kim Chanhee, Kim Jongho, Yang Hyun-Mo, Lee Changsik, Chung Yeonseok, Lee Hyo-Jong, Jo Dong-Gyu
School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea; Department of Pharmacology, CKD Research Institute, Chong Kun Dang Pharmaceutical Co., Yongin 16995, Republic of Korea.
Metabolism. 2025 Mar;164:156108. doi: 10.1016/j.metabol.2024.156108. Epub 2024 Dec 15.
Diabetic retinopathy (DR), a major blindness cause in developed countries, is intricately linked to diabetes management and its duration. Here, we demonstrate that HDAC6 mediates NLRP3 inflammasome activation under diabetic conditions, leading to retinal inflammation and degeneration.
This study demonstrated the therapeutic effects of HDAC6 genetic ablation, pharmacological inhibition, and HDAC6-deficient bone marrow transplantation in a diabetes model induced by streptozotocin and a high-fat diet. The therapeutic potential was evaluated from a metabolic perspective, including ocular pathologies such as retinal lesions, neovascularization, and vascular leakage.
We discovered that inhibition or genetic ablation of HDAC6 markedly alleviates DR symptoms by dampening NLRP3 inflammasome activation and mitigating retinal damage. Moreover, bone marrow transplantation from HDAC6-deficient mice into wild-type counterparts reversed DR symptoms, underscoring the significance of HDAC6 in systemic immune regulation. The study introduces a novel HDAC6 inhibitor, noted for superior bioavailability and blood-retinal barrier permeability, further highlights the therapeutic promise of targeting HDAC6 in DR.
Our findings not only underscore the crucial role of HDAC6 in the immune regulatory mechanisms underlying DR pathogenesis through NLRP3 inflammasome activation but also position HDAC6 inhibition as a promising strategy for addressing diabetic complications beyond DR.
糖尿病视网膜病变(DR)是发达国家导致失明的主要原因,与糖尿病管理及其病程密切相关。在此,我们证明组蛋白去乙酰化酶6(HDAC6)在糖尿病条件下介导NLRP3炎性小体激活,导致视网膜炎症和变性。
本研究证明了HDAC6基因敲除、药物抑制以及HDAC6缺陷型骨髓移植在链脲佐菌素和高脂饮食诱导的糖尿病模型中的治疗效果。从代谢角度评估治疗潜力,包括视网膜病变、新生血管形成和血管渗漏等眼部病理变化。
我们发现抑制或基因敲除HDAC6可通过抑制NLRP3炎性小体激活和减轻视网膜损伤,显著缓解DR症状。此外,将HDAC6缺陷型小鼠的骨髓移植到野生型小鼠体内可逆转DR症状,强调了HDAC6在全身免疫调节中的重要性。该研究引入了一种新型HDAC6抑制剂,其具有卓越的生物利用度和血视网膜屏障通透性,进一步突出了靶向HDAC6治疗DR的前景。
我们的研究结果不仅强调了HDAC6通过NLRP3炎性小体激活在DR发病机制的免疫调节机制中的关键作用,还将HDAC6抑制定位为解决DR以外糖尿病并发症的一种有前景的策略。