University of Padua and Fondazione Istituto di Ricerca Pediatrica Città della Speranza (IRP), Padua, Italy.
University of Padua, Padua, Italy.
Arthritis Rheumatol. 2024 Feb;76(2):279-284. doi: 10.1002/art.42697. Epub 2023 Dec 21.
Calcium pyrophosphate (CPP) crystal deposition in the joints is associated with a heterogeneous set of debilitating syndromes characterized by inflammation and pain, for which no effective therapies are currently available. Because we found that the mitochondrial enzyme monoamine oxidase B (MAO-B) plays a fundamental role in promoting inflammatory pathways, this study aims at assessing the efficacy of two clinical-grade inhibitors (iMAO-Bs) in preclinical models of this disease to pave the way for a novel treatment.
We tested our hypothesis in two murine models of CPP-induced arthritis, by measuring cytokine and chemokine levels, along with immune cell recruitment. iMAO-Bs (rasagiline and safinamide) were administered either before or after crystal injection. To elucidate the molecular mechanism, we challenged in vitro primed macrophages with CPP crystals and assessed the impact of iMAO-Bs in dampening proinflammatory cytokines and in preserving mitochondrial function.
Both in preventive and therapeutic in vivo protocols, iMAO-Bs blunted the release of proinflammatory cytokines (interleukin [IL]-6 and IL1-β) and chemokines (CXCL10, CXCL1, CCL2 and CCL5) (n > 6 mice/group). Importantly, they also significantly reduced ankle swelling (50.3% vs 17.1%; P < 0.001 and 23.1%; P = 0.005 for rasagiline and safinamide, respectively). Mechanistically, iMAO-Bs dampened the burst of reactive oxygen species and the mitochondrial dysfunction triggered by CPP crystals in isolated macrophages. Moreover, iMAO-Bs blunted cytokine secretion and NLRP3 inflammasome activation through inhibition of the NF-κB and STAT3 pathways.
iMAO-Bs dampen inflammation in murine models of crystal-induced arthropathy, thereby uncovering MAO-B as a promising target to treat these diseases.
焦磷酸钙(CPP)晶体在关节中的沉积与一组以炎症和疼痛为特征的衰弱综合征有关,目前尚无有效的治疗方法。因为我们发现线粒体酶单胺氧化酶 B(MAO-B)在促进炎症途径方面起着至关重要的作用,所以本研究旨在评估两种临床级抑制剂(iMAO-Bs)在这种疾病的临床前模型中的疗效,为一种新的治疗方法铺平道路。
我们通过测量细胞因子和趋化因子水平以及免疫细胞募集,在两种 CPP 诱导的关节炎的小鼠模型中测试了我们的假设。iMAO-Bs(rasagiline 和 safinamide)在晶体注射前或后给予。为了阐明分子机制,我们用 CPP 晶体挑战体外预刺激的巨噬细胞,并评估 iMAO-Bs 对抑制促炎细胞因子和维持线粒体功能的影响。
在预防和治疗性的体内方案中,iMAO-Bs 减弱了促炎细胞因子(白细胞介素 [IL]-6 和 IL1-β)和趋化因子(CXCL10、CXCL1、CCL2 和 CCL5)的释放(每组>6 只小鼠)。重要的是,它们还显著降低了踝关节肿胀(rasagiline 和 safinamide 分别为 50.3%比 17.1%;P<0.001 和 23.1%;P=0.005)。从机制上讲,iMAO-Bs 抑制了 CPP 晶体在分离的巨噬细胞中引发的活性氧爆发和线粒体功能障碍。此外,iMAO-Bs 通过抑制 NF-κB 和 STAT3 途径,抑制细胞因子分泌和 NLRP3 炎性体激活。
iMAO-Bs 抑制了晶体诱导的关节炎的小鼠模型中的炎症,从而揭示 MAO-B 是治疗这些疾病的一个有希望的靶点。