Longo Francesco, Massaro Alessandro, Mauro Manuela, Allegra Mario, Arizza Vincenzo, Tesoriere Luisa, Restivo Ignazio
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, 90128 Palermo, Italy.
Antioxidants (Basel). 2025 Jun 11;14(6):713. doi: 10.3390/antiox14060713.
Current intra-articular therapies with hyaluronic acid (HA) provide symptomatic relief in joint diseases, but have limited efficacy in counteracting oxidative stress and inflammation, key drivers of cartilage degradation in rheumatoid arthritis (RA). To address this limitation, the potential of combining HA with the phytochemicals xanthohumol (XAN) and epigallocatechin-3-O-gallate (EGCG), known for their antioxidant and anti-inflammatory properties, was evaluated in a cellular model of RA (SW982 synoviocytes stimulated with interleukin-1β, IL-1β). The Chou-Talalay method demonstrated that their combination synergistically reduced reactive oxygen species (ROS) and nitric oxide (NO) levels. The "TRIPLE" combination (HA + XAN + EGCG) showed the lowest combination index and the highest dose reduction index. Compared to individual treatments, TRIPLE significantly decreased IL-1β-induced IL-6, IL-8, TNF-α, and MMP-3 levels, while increasing the levels of the anti-inflammatory cytokine IL-10. Western blot analysis revealed a marked reduction in iNOS, COX-2, and MMP-3 protein expression following TRIPLE treatment. Moreover, the combination inhibited IL-1β-induced phosphorylation of IκB and p65, thereby preventing NF-κB activation. These findings suggest that integrating XAN and EGCG into injectable HA formulations may represent a promising strategy to improve the management of joint inflammation in RA.
目前使用透明质酸(HA)的关节内治疗方法可缓解关节疾病的症状,但在对抗氧化应激和炎症方面效果有限,而氧化应激和炎症是类风湿性关节炎(RA)中软骨降解的关键驱动因素。为了解决这一局限性,在RA细胞模型(用白细胞介素-1β,IL-1β刺激的SW982滑膜细胞)中评估了将HA与具有抗氧化和抗炎特性的植物化学物质黄腐酚(XAN)和表没食子儿茶素-3-O-没食子酸酯(EGCG)联合使用的潜力。Chou-Talalay方法表明,它们的组合可协同降低活性氧(ROS)和一氧化氮(NO)水平。“三联”组合(HA + XAN + EGCG)显示出最低的组合指数和最高的剂量降低指数。与单独治疗相比,三联组合显著降低了IL-1β诱导的IL-6、IL-8、TNF-α和MMP-3水平,同时提高了抗炎细胞因子IL-10的水平。蛋白质印迹分析显示,三联治疗后iNOS、COX-2和MMP-3蛋白表达明显降低。此外,该组合抑制了IL-1β诱导的IκB和p65磷酸化,从而阻止了NF-κB的激活。这些发现表明,将XAN和EGCG整合到可注射的HA制剂中可能是改善RA关节炎症管理的一种有前景的策略。