Regulaxis SAS, Romainville, France.
ESE Conseil, Saint-Cloud, France.
PLoS One. 2020 Apr 14;15(4):e0231240. doi: 10.1371/journal.pone.0231240. eCollection 2020.
REG-O3 is a 24-aminoacid chimeric peptide combining a sequence derived from growth hormone (GH) and an analog of somatostatin (SST), molecules displaying cartilage repair and anti-inflammatory properties, respectively. This study aimed to investigate the disease-modifying osteoarthritis drug (DMOAD) potential of REG-O3 by analyzing its effect on pain, joint function and structure, upon injection into osteoarthritic rat knee joint.
Osteoarthritis was induced in the right knee of mature male Lewis rats (n = 12/group) by surgical transection of the anterior cruciate ligament (ACLT) combined with partial medial meniscectomy (pMMx). Treatments were administered intra-articularly from fourteen days after surgery through three consecutive injections one week apart. The effect of REG-O3, solubilized in a liposomal solution and injected at either 5, 25 or 50 μg/50 μL, was compared to liposomal (LIP), dexamethasone and hyaluronic acid (HA) solutions. The study endpoints were the pain/function measured once a week throughout the entire study, and the joint structure evaluated eight weeks after surgery using OARSI score.
ACLT/pMMx surgery induced a significant modification of weight bearing in all groups. When compared to liposomal solution, REG-O3 was able to significantly improve weight bearing as efficiently as dexamethasone and HA. REG-O3 (25 μg) was also able to significantly decrease OARSI histological global score as well as degeneration of both cartilage and matrix while the other treatments did not.
This study provides evidence of a remarkable protecting effect of REG-O3 on pain/knee joint function and cartilage/matrix degradation in ACLT/pMMx model of rat osteoarthritis. REG-O3 thus displays an interesting profile as a DMOAD.
REG-O3 是一种 24 个氨基酸的嵌合肽,结合了生长激素 (GH) 和生长抑素 (SST) 的类似物,分别具有软骨修复和抗炎特性。本研究旨在通过分析 REG-O3 对骨关节炎大鼠膝关节疼痛、关节功能和结构的影响,研究其作为治疗骨关节炎的药物 (DMOAD) 的潜力。
通过手术切断前交叉韧带 (ACLT) 并部分切除内侧半月板 (pMMx),在成熟雄性 Lewis 大鼠的右膝关节中诱导骨关节炎 (n = 12/组)。手术后 14 天开始关节内给药,连续给药 3 次,间隔 1 周。将 REG-O3 溶解在脂质体溶液中,以 5、25 或 50 μg/50 μL 的剂量注射,与脂质体 (LIP)、地塞米松和透明质酸 (HA) 溶液进行比较。研究终点是整个研究过程中每周测量一次的疼痛/功能,以及手术后 8 周使用 OARSI 评分评估关节结构。
ACLT/pMMx 手术后所有组的负重能力均发生显著改变。与脂质体溶液相比,REG-O3 能够像地塞米松和 HA 一样有效地改善负重能力。REG-O3(25 μg)还能显著降低 OARSI 组织学总体评分以及软骨和基质的退变,而其他治疗方法则没有。
本研究为 REG-O3 在 ACLT/pMMx 大鼠骨关节炎模型中对疼痛/膝关节功能和软骨/基质降解的显著保护作用提供了证据。因此,REG-O3 作为一种 DMOAD 具有很好的应用前景。