Department of Synopsis of the Golden Chamber, School of Basic Medical Sciences, Heilongjiang University of Chinese Medicine, 24 Heping Road, Harbin, 150040, Heilongjiang, People's Republic of China.
Department of Ultrasound Medicine, First Affiliated Hospital, Heilongjiang University of Chinese Medicine, Harbin, 150040, Heilongjiang, People's Republic of China.
J Nat Med. 2021 Jan;75(1):37-47. doi: 10.1007/s11418-020-01440-7. Epub 2020 Aug 6.
Monosodium urate (MSU)-mediated inflammation is closely related to gouty arthritis (GA). Dioscin, an active ingredient, has been reported to possess anti-inflammatory property. Nevertheless, the role of dioscin in GA and the underlying mechanism have not been fully understood. In the present study, we investigated the anti-inflammatory effect of dioscin on MSU-induced GA through in vivo and in vitro experiments. Histopathological analysis showed that dioscin alleviated the severity of GA concomitant with the lowered uric acid and creatinine levels. Moreover, the increasing IL-1β, IL-6, and TNF-α levels induced by MSU were decreased via administration of dioscin in mice and human synoviocytes. Western blotting results suggested that dioscin inhibited the activation of NLRP3 through down-regulating the protein expressions of NLRP3, apoptosis-associated speck-like protein containing a caspase recruitment domain (ASC), cleaved-caspase-1, as well as IL-1β. In addition, TLR4, myeloid differentiation primary response gene 88 (MyD88), p-IKKβ, p-p65, and NF-κB p65 in nuclei levels were significantly reduced by dioscin. Importantly, dioscin remarkably lowered the NF-κB p65-DNA activity in MSU-treated mice utilizing electrophoretic mobility shift assay (EMSA) analysis. Taken together, dioscin had a protective effect against MSU-initiated inflammatory response via repressing the production of inflammatory cytokines and the activation of inflammasome NLRP3 and TLR4/NF-κB signaling pathway. The above findings revealed that dioscin could be a potential drug for the treatment of GA.
尿酸单钠(MSU)介导的炎症与痛风性关节炎(GA)密切相关。薯蓣皂苷元是一种活性成分,据报道具有抗炎作用。然而,薯蓣皂苷元在 GA 中的作用及其潜在机制尚未完全阐明。在本研究中,我们通过体内和体外实验研究了薯蓣皂苷元对 MSU 诱导的 GA 的抗炎作用。组织病理学分析表明,薯蓣皂苷元缓解了 GA 的严重程度,同时降低了尿酸和肌酐水平。此外,薯蓣皂苷元降低了 MSU 诱导的小鼠和人滑膜细胞中白细胞介素-1β(IL-1β)、白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)水平的升高。Western blot 结果表明,薯蓣皂苷元通过下调 NLRP3 蛋白表达、凋亡相关斑点样蛋白(ASC)、切割型半胱氨酸蛋白酶-1(caspase-1)和 IL-1β,抑制 NLRP3 的激活。此外,薯蓣皂苷元还显著降低了 MSU 处理的小鼠中 TLR4、髓样分化初级反应基因 88(MyD88)、磷酸化 IKKβ(p-IKKβ)、磷酸化 p65(p-p65)和核内 NF-κB p65 的水平。重要的是,电泳迁移率变动分析(EMSA)显示,薯蓣皂苷元显著降低了 MSU 处理的小鼠中 NF-κB p65-DNA 的活性。综上所述,薯蓣皂苷元通过抑制炎症细胞因子的产生和炎症小体 NLRP3 和 TLR4/NF-κB 信号通路的激活,对 MSU 引发的炎症反应具有保护作用。这些发现表明,薯蓣皂苷元可能是治疗 GA 的一种潜在药物。