埃里亚宁：一种具有显著抗炎活性的直接 NLRP3 抑制剂。

Erianin: A Direct NLRP3 Inhibitor With Remarkable Anti-Inflammatory Activity.

机构信息

Department of Neurology, Huaian Hospital Affiliated to Xuzhou Medical University, Huaian, China.

The Key Laboratory of Targeted Intervention of Clinical Disease, Collaborative Innovation Center of Translational Medicine for Clinical Disease, Nanjing Medical University, Nanjing, China.

出版信息

Front Immunol. 2021 Oct 20;12:739953. doi: 10.3389/fimmu.2021.739953. eCollection 2021.

Erianin (Eri) is the extract of Lindl. The NLRP3 inflammasome is a multiprotein complex that plays key roles in a wide variety of chronic inflammation-driven human diseases. Nevertheless, little is known about the protection of Eri against NLRP3 inflammasome-related diseases. In this study, we demonstrated that Eri inhibited NLRP3 inflammasome activation and . Mechanistically, Eri directly interacted with NLRP3, leading to inhibition of NLRP3 inflammasome assembly. Eri associated with the Walker A motif in the NACHT domain and suppressed NLRP3 ATPase activity. In mouse models, Eri had therapeutic effects on peritonitis, gouty arthritis and type 2 diabetes, NLRP3. More importantly, Eri was active for synovial fluid cells and monocytes from patients with IAV infection and gout. Eri may serve as a potential novel therapeutic compound against NLRP3-driven diseases.

穿心莲内酯（Eri）是穿心莲的提取物。NLRP3 炎性小体是一种多蛋白复合物，在多种慢性炎症驱动的人类疾病中发挥关键作用。然而，对于穿心莲内酯对 NLRP3 炎性小体相关疾病的保护作用知之甚少。在这项研究中，我们表明穿心莲内酯抑制 NLRP3 炎性小体的激活。机制上，穿心莲内酯直接与 NLRP3 相互作用，导致 NLRP3 炎性小体组装的抑制。穿心莲内酯与 NACHT 结构域中的 Walker A 基序结合，并抑制 NLRP3 的 ATP 酶活性。在小鼠模型中，穿心莲内酯对腹膜炎、痛风性关节炎和 2 型糖尿病具有治疗作用，下调 NLRP3。更重要的是，穿心莲内酯对流感病毒感染和痛风患者的滑液细胞和单核细胞具有活性。穿心莲内酯可能成为一种针对 NLRP3 驱动疾病的潜在新型治疗化合物。