Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.
Inflammation. 2017 Aug;40(4):1177-1190. doi: 10.1007/s10753-017-0561-1.
RANKL and RANK are potential contributors of inflammatory cascade in human and animal model of arthritis. The current study aims to investigate the effect of N-(2-hydroxyphenyl)acetamide (NA-2) on regulation of RANKL pathway in collagen-induced arthritis (CIA) model in rats. CIA was induced using bovine type II collagen in female Wistar rats. The clinical parameters, level of pro-inflammatory and oxidative stress markers were measured to determine the progression of the disease. The mRNA level of RANKL and RANK and downstream mediators of inflammation i.e. c-fos, c-jun, NF-κB and Akt were analysed in spleen tissue using real-time PCR. Immunohistochemical analysis of iNOS, pAkt and c-Fos was also done in spleen tissue. Treatment with NA-2 and indomethacin showed increase in body weight and significant reduction in paw volume and arthritic score (p < 0.0001). Marked reduction in the level of oxidative stress markers, NO, PO and GSH (p < 0.0001), and pro-inflammatory markers, IL-1β (p < 0.0001) and TNF-α (p < 0.01), was also observed. Likewise, NA-2 and indomethacin treatment also significantly suppressed the mRNA expression of RANKL, RANK, c-fos, c-jun, NF-κB (p < 0.0001) and Akt (p < 0.01) and protein expression of iNOS, pAkt and c-Fos (p < 0.0001) compared to the arthritic control group. Our findings suggest that NA-2 is an antiarthritic agent acting in a pleiotropic manner in CIA rats by not only reducing the clinical signs of arthritis, inflammatory cytokines and free radical production but also attenuating the RANK/RANKL signaling pathway.
RANKL 和 RANK 是人类和动物关节炎模型中炎症级联的潜在贡献者。本研究旨在探讨 N-(2-羟基苯基)乙酰胺 (NA-2) 对胶原诱导性关节炎 (CIA) 大鼠模型中 RANKL 通路的调节作用。使用牛 II 型胶原在雌性 Wistar 大鼠中诱导 CIA。测量临床参数、促炎和氧化应激标志物的水平,以确定疾病的进展。使用实时 PCR 分析脾组织中 RANKL 和 RANK 的 mRNA 水平以及炎症的下游介质,即 c-fos、c-jun、NF-κB 和 Akt。还对脾组织中的 iNOS、pAkt 和 c-Fos 进行了免疫组织化学分析。NA-2 和吲哚美辛治疗显示体重增加,爪体积和关节炎评分显著降低(p < 0.0001)。还观察到氧化应激标志物、NO、PO 和 GSH(p < 0.0001)和促炎标志物、IL-1β(p < 0.0001)和 TNF-α(p < 0.01)水平明显降低。同样,与关节炎对照组相比,NA-2 和吲哚美辛治疗也显著抑制了 RANKL、RANK、c-fos、c-jun、NF-κB(p < 0.0001)和 Akt(p < 0.01)的 mRNA 表达以及 iNOS、pAkt 和 c-Fos 的蛋白表达(p < 0.0001)。我们的研究结果表明,NA-2 是一种抗炎剂,通过不仅减少关节炎的临床症状、炎症细胞因子和自由基产生,而且还减弱 RANK/RANKL 信号通路,在 CIA 大鼠中发挥多效作用。