Wang Qing, Zhuang Di, Feng Wenchang, Ma Bitao, Qin Liping, Jin Lilun
Department of Traditional Chinese Medicine, Xinhua Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200092, China.
Saudi Pharm J. 2020 Dec;28(12):1499-1506. doi: 10.1016/j.jsps.2020.09.016. Epub 2020 Sep 25.
Osteoarthritis (OA) is a disease characterized by degeneration of the joint complex due to cartilage destruction. Fraxetin, a widely used and studied coumarin compound extracted from a traditional Chinese herb (Qin Pi), has shown anti-inflammatory and antioxidant properties, but its effects on OA have not been studied. In the present study, western blotting, immunofluorescence, and terminal deoxynucleotidyl transferase (TdT) dUTP nick-end labeling (TUNEL) were used to evaluate the effects of fraxetin on IL-1β-induced apoptotic activity, inflammatory responses, and catabolism in rat chondrocytes. The results showed that fraxetin prevented IL-1β-induced apoptosis of chondrocytes and inhibited inflammatory mediator release by regulating the Toll-like receptor 4 (TLR4)/myeloid differentiation primary response 88 (MyD88)/nuclear factor (NF)-κB pathway in chondrocytes. Additionally, fraxetin suppressed the upregulation of matrix metalloproteinase 13 (MMP13) and degradation of collagen II in the extracellular matrix (ECM). Moreover, the effects of fraxetin were assessed in a monosodium iodoacetate (MIA)-induced rat model of OA using hematoxylin and eosin (H&E) and Safranin O-fast green staining and magnetic resonance imaging (MRI). The results showed that fraxetin protected the cartilage against destruction. In conclusion, fraxetin could be a potential therapeutic for OA.
骨关节炎（OA）是一种由于软骨破坏导致关节复合体退变的疾病。秦皮乙素是一种从传统中药（秦皮）中提取的、已被广泛使用和研究的香豆素化合物，具有抗炎和抗氧化特性，但其对骨关节炎的影响尚未得到研究。在本研究中，采用蛋白质免疫印迹法、免疫荧光法和末端脱氧核苷酸转移酶（TdT）介导的dUTP缺口末端标记法（TUNEL）来评估秦皮乙素对白细胞介素-1β（IL-1β）诱导的大鼠软骨细胞凋亡活性、炎症反应和分解代谢的影响。结果表明，秦皮乙素可通过调节软骨细胞中Toll样受体4（TLR4）/髓样分化因子88（MyD88）/核因子（NF）-κB信号通路，防止IL-1β诱导的软骨细胞凋亡，并抑制炎症介质释放。此外，秦皮乙素可抑制细胞外基质（ECM）中基质金属蛋白酶13（MMP13）的上调和Ⅱ型胶原蛋白的降解。此外，使用苏木精-伊红（H&E）染色、番红O-固绿染色和磁共振成像（MRI），在碘乙酸钠（MIA）诱导的大鼠骨关节炎模型中评估了秦皮乙素的作用。结果表明，秦皮乙素可保护软骨免受破坏。总之，秦皮乙素可能是一种治疗骨关节炎的潜在药物。
