Rheumatoid arthritis (RA) is a chronic joint disorder, of which, excessive angiogenesis is the well-established factor contributing to synovitis and joint destruction. Ardisia crispa (Primulaceae) is a medicinal herb with evidenced anti-angiogenic properties, attributed to 2-methoxy-6-undecyl-1,4-benzoquinone (BQ) found in its roots. However, it is still unclear how BQ is able to inhibit angiogenesis in RA. Hence, we investigated the anti-arthritic potential of quinone-rich fraction (QRF) separated from Ardisia crispa roots hexane extract (ACRH) by targeting angiogenesis on collagen-induced arthritis (CIA) in rats. The QRF was priorly identified by quantifying the BQ content in the fraction using GC–MS. Male Sprague–Dawley rats (n = 6) were initially immunised with type II collagen (150 µg) subcutaneously at the base of the tail on day 0. QRF (3, 10, and 30 mg/kg/day) and celecoxib (5 mg/kg/day) were orally administered for 13 consecutive days starting from day 14 post-induction, except for the vehicle and arthritic controls. QRF at all dosages moderately ameliorated the arthritic scores, ankle swelling, and hind paw oedema with no significant (p > 0.05) modulation on the bodyweights and organ weights (i.e., liver, kidney, and spleen). Treatment with QRF at 3, 10, and 30 mg/kg, significantly (p < 0.05) attenuated VEGF-A, PI3K, AKT, NF-κB, p38, STAT3, and STAT5 proteins and markedly restored the increased synovial microvessel densities (MVD) to the normal level in arthritic rats in a dose-independent manner. In conclusion, QRF conferred the anti-arthritic effect via angiogenesis inhibition in vivo, credited to the BQ content and synergism, at least in part, by other phytoconstituents.

类风湿性关节炎 (RA) 是一种慢性关节疾病，其中过度的血管生成是导致滑膜炎和关节破坏的公认因素。Ardisiacrispa（报春科）是一种药草，具有明显的抗血管生成特性，归因于其根中发现的 2-甲氧基-6-十一烷基-1,4-苯醌 (BQ)。然而，目前尚不清楚 BQ 如何能够抑制 RA 中的血管生成。因此，我们研究了富醌部分（QRF）的抗关节炎电位从分离朱砂皱通过对大鼠胶原诱导的关节炎靶向血管生成（CIA）的根己烷提取（ACRH）。QRF 是通过使用 GC-MS 对馏分中的 BQ 含量进行定量来确定的。雄性 Sprague-Dawley 大鼠 ( n = 6) 最初在第 0 天用 II 型胶原蛋白 (150 µg) 在尾巴底部皮下免疫。 QRF（3、10 和 30 毫克/公斤/天）和塞来昔布（5 毫克/公斤/天）是从诱导后第 14 天开始，连续 13 天口服给药，载体和关节炎对照除外。所有剂量的 QRF 均适度改善关节炎评分、踝关节肿胀和后爪水肿， 对体重和器官重量（即肝、肾和脾）没有显着（p > 0.05）调节。用 3、10 和 30 mg/kg 的 QRF 处理显着（p < 0.05) 减弱 VEGF-A、PI3K、AKT、NF-κB、p38、STAT3 和 STAT5 蛋白，并以与剂量无关的方式使关节炎大鼠增加的滑膜微血管密度 (MVD) 显着恢复至正常水平。总之，QRF 通过体内血管生成抑制赋予抗关节炎作用，这归功于 BQ 含量和协同作用，至少部分是由其他植物成分引起的。