Department of Orthopaedics, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China.
The Second School of Medicine, Wenzhou Medical University, Wenzhou, China.
J Cell Mol Med. 2021 Jan;25(1):499-509. doi: 10.1111/jcmm.16104. Epub 2020 Nov 19.
Osteoarthritis (OA), a prevalent degenerative arthritis disease, principle characterized by the destruction of cartilage and associated with the inflammatory response. Maltol, a product formed during the processing of red ginseng (Panax ginseng, CA Meyer), has been reported to have the potential effect of anti-inflammatory. However, its specific mechanisms are not demonstrated. We investigated the protective effect of maltol in the progression of OA both in vitro and in vivo experiments. Human chondrocytes were pre-treated with maltol (0, 20, 40, 60 μM, 24 hours) and incubated with IL-1β (10 ng/mL, 24 hours) in vitro. Expression of PGE2, TNF-α and NO was measured by the ELISA and Griess reaction. The expression of iNOs, COX-2, aggrecan, ADAMTS-5, MMP-13, IκB-α, p65, P-AKT, AKT, PI3K and P-PI3K was analysed by Western blotting. The expression of collagen II and p65-active protein was detected by immunofluorescence. Moreover, the serious level of OA was evaluated by histological analysis in vivo. We identified that maltol could suppress the IL-1β-stimulated generation of PGE2 and NO. Besides, maltol not only suppressed the production of COX-2, iNOs, TNF-α, IL-6, ADAMTS-5, MMP-13, but also attenuated the degradation of collagen II and aggrecan. Furthermore, maltol remarkably suppressed the phosphorylation of PI3K/AKT and NF-κB induced by IL-1β in human OA chondrocytes. Moreover, maltol could block the cartilage destroy in OA mice in vivo. To date, all data indicate maltol is a potential therapeutic agent by inhibiting inflammatory response via the regulation of NF-κB signalling for OA.
骨关节炎（OA）是一种常见的退行性关节炎疾病，主要特征是软骨破坏，并伴有炎症反应。麦芽酚是红参（Panax ginseng，CA Meyer）加工过程中的产物，据报道具有抗炎作用。然而，其具体机制尚未得到证实。我们通过体外和体内实验研究了麦芽酚在 OA 进展中的保护作用。体外实验中，先用麦芽酚（0、20、40、60 μM，24 小时）预处理人软骨细胞，然后用白细胞介素-1β（10ng/mL，24 小时）孵育。通过 ELISA 和格里斯反应测定 PGE2、TNF-α 和 NO 的表达。通过 Western blot 分析 iNOS、COX-2、聚集蛋白聚糖、ADAMTS-5、MMP-13、IκB-α、p65、P-AKT、AKT、PI3K 和 P-PI3K 的表达。通过免疫荧光检测胶原 II 和 p65 活性蛋白的表达。此外，还通过体内组织学分析评估 OA 的严重程度。我们发现麦芽酚可以抑制 IL-1β 刺激的 PGE2 和 NO 的产生。此外，麦芽酚不仅抑制 COX-2、iNOS、TNF-α、IL-6、ADAMTS-5、MMP-13 的产生，还减弱了胶原 II 和聚集蛋白聚糖的降解。此外，麦芽酚还显著抑制了 IL-1β 诱导的人 OA 软骨细胞中 PI3K/AKT 和 NF-κB 的磷酸化。此外，麦芽酚可以阻断体内 OA 小鼠的软骨破坏。到目前为止，所有数据表明，麦芽酚通过抑制 NF-κB 信号通路抑制炎症反应，是一种治疗 OA 的潜在治疗药物。
