Department of Orthopedics, Northern Jiangsu People's Hospital Affiliated to Yangzhou University, Northern Jiangsu People's Hospital Affiliated to Nanjing University, Yangzhou, Jiangsu, China; Yancheng School of Clinical Medicine of Nanjing Medical University, Yancheng Third People's Hospital, Yancheng, Jiangsu, China.
Dalian Medical University, Dalian, Liaoning, China.
Eur J Pharmacol. 2022 Dec 5;936:175347. doi: 10.1016/j.ejphar.2022.175347. Epub 2022 Oct 29.
Osteoarthritis (OA) is primarily characterized by progressive degeneration and destruction of articular cartilage. Currently, there is no effective method to treat OA. The metabolic disturbance of cartilage extracellular matrix (ECM) and oxidative stress are critical to promote OA progression. Galangin (Gal) is a small molecule compound that pertains to flavonoids. To determine the protective effect and mechanism of Gal against OA progression, various experiments were performed in vitro and in vivo. In vitro, Gal promoted ECM production and attenuated ECM degradation in human OA chondrocytes. The expression of ECM components from human OA cartilage explants was also stimulated by Gal treatment. As demonstrated from the in vivo study, the intra-articular injection of Gal delayed OA progression in rat models. Moreover, RNA sequencing analysis showed that proline/arginine-rich end leucine repeat protein (PRELP) was a molecular target of Gal activity. Gal inhibited oxidative stress and attenuated ECM degradation by activating PRELP expression. The study demonstrated that Gal could attenuate ECM degradation and ameliorate OA progression, and PRELP may be a potential candidate drug of Gal for treating OA.
骨关节炎（OA）主要表现为关节软骨进行性退变和破坏。目前，OA 尚无有效的治疗方法。软骨细胞外基质（ECM）代谢紊乱和氧化应激对促进 OA 进展至关重要。高良姜素（Gal）是一种小分子化合物，属于黄酮类。为了确定 Gal 对 OA 进展的保护作用和机制，在体外和体内进行了各种实验。在体外，Gal 促进人 OA 软骨细胞 ECM 的产生并抑制 ECM 的降解。Gal 处理还刺激人 OA 软骨外植体中 ECM 成分的表达。从体内研究结果表明，关节内注射 Gal 可延缓大鼠模型 OA 的进展。此外，RNA 测序分析表明，脯氨酸/精氨酸丰富的末端亮氨酸重复蛋白（PRELP）是 Gal 活性的分子靶点。Gal 通过激活 PRELP 表达来抑制氧化应激和减轻 ECM 降解。该研究表明，Gal 可抑制 ECM 降解并改善 OA 进展，而 PRELP 可能是 Gal 治疗 OA 的潜在候选药物。
