Venlafaxine is a serotonin-norepinephrine reuptake inhibitor used to treat depression. Previous studies demonstrated its anti-nociceptive and anti-inflammatory activities through the suppression of pro-inflammatory cytokines. Present research aimed to explore its anti-arthritic potential. Different in-vitro assays including egg albumin, bovine serum albumin denaturation and human red blood cell (RBC) membrane stabilization assays along with in-vivo models of formaldehyde and complete Freund’s adjuvant-induced arthritis were used to study its anti-arthritic effect. Venlafaxine inhibited egg albumin and bovine serum albumin denaturation and preserve the integrity of red blood cells membrane in concentration-dependent manner. In formaldehyde-induced arthritis venlafaxine significantly (p < 0.001) reduced the paw edema on treatment for 10 days. Chronic administration of venlafaxine for 28 days in Freund’s adjuvant-induced arthritis model decreased the paw volume (p < 0.001), arthritic index (p < 0.01), flexion pain score (p < 0.05), mobility score (p < 0.05), and improved the stance score (p < 0.05). Venlafaxine also significantly declined the rheumatoid factor (p < 0.01) and C-reactive protein (p < 0.05) levels and increased the RBC count (p < 0.01) and Hb value (p < 0.001). Upon PCR analysis venlafaxine remarkably turndown the mRNA expression of TNF-α, IL-6, IL-1β, and COX-2. Taken together it is inferred from current findings that venlafaxine possesses the significant anti-arthritic activity and could be a potential therapeutic option for the treatment of rheumatoid arthritis.

文拉法辛是一种用于治疗抑郁症的血清素-去甲肾上腺素再摄取抑制剂。以前的研究通过抑制促炎细胞因子证明了其抗伤害和抗炎活性。目前的研究旨在探索其抗关节炎的潜力。使用不同的体外测定法，包括卵白蛋白、牛血清白蛋白变性和人红细胞 (RBC) 膜稳定性测定法以及甲醛和完全弗氏佐剂诱导的关节炎的体内模型来研究其抗关节炎作用。文拉法辛以浓度依赖性方式抑制卵白蛋白和牛血清白蛋白变性并保持红细胞膜的完整性。在甲醛引起的关节炎文拉法辛显着（p < 0.001) 治疗 10 天后爪水肿减轻。在弗氏佐剂性关节炎模型中长期服用文拉法辛 28 天后，爪体积（p  < 0.001）、关节炎指数（p  < 0.01）、屈曲疼痛评分（p  < 0.05）、活动度评分（p  < 0.05）和提高了姿态得分 ( p  < 0.05)。文拉法辛还显着降低类风湿因子 ( p  < 0.01) 和 C 反应蛋白 ( p  < 0.05) 水平，并增加红细胞计数 ( p  < 0.01) 和 Hb 值 ( p < 0.001)。PCR 分析文拉法辛显着降低了 TNF-α、IL-6、IL-1β 和 COX-2 的 mRNA 表达。综上所述，从目前的研究结果推断，文拉法辛具有显着的抗关节炎活性，可能是治疗类风湿性关节炎的潜在治疗选择。