Department of Orthopedic Surgery, The Second Hospital of Harbin Medical University, Harbin, Heilongjiang Province, 150086, People's Republic of China.
Children's Hospital of Harbin, Harbin, Heilongjiang Province, 150010, People's Republic of China.
Inflammation. 2016 Apr;39(2):543-9. doi: 10.1007/s10753-015-0278-y.
Echinocystic acid (EA), a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, displays a range of pharmacological activities including anti-inflammatory and antioxidant effects. However, the effect of EA on IL-1β-stimulated osteoarthritis chondrocyte has not been reported. The purpose of this study was to assess the effects of EA on IL-1β-stimulated human osteoarthritis chondrocyte. Chondrocytes were stimulated with IL-1β in the absence or presence of EA. NO and PGE2 production were measured by Griess reagent and ELISA. The expression of COX-2, iNOS, nuclear factor-κB (NF-κB), inhibitory kappa B (IκBα), c-Jun N-terminal kinase (JNK), p38, and extracellular signal-regulated kinase (ERK) were detected by Western blot analysis. The results showed that EA suppressed IL-1β-induced collagenase-3 (MMP-13), NO, and PGE2 production in a dose-dependent manner. IL-1β up-regulated the expression of COX-2 and iNOS, and the increase was inhibited by EA. Furthermore, IL-1β-induced NF-κB and mitogen-activated protein kinase (MAPK) activation were inhibited by EA. In conclusion, EA effectively attenuated IL-1β-induced inflammatory response in osteoarthritis chondrocyte which suggesting that EA may be a potential agent in the treatment of osteoarthritis.
羽扇豆醇（EA）是从皂角果实中分离出来的一种五环三萜，具有多种药理活性，包括抗炎和抗氧化作用。然而，EA 对白细胞介素-1β（IL-1β）刺激的骨关节炎软骨细胞的影响尚未报道。本研究旨在评估 EA 对 IL-1β刺激的人骨关节炎软骨细胞的作用。在不存在或存在 EA 的情况下，用 IL-1β刺激软骨细胞。通过格里斯试剂和 ELISA 测定 NO 和 PGE2 的产生。通过 Western blot 分析检测 COX-2、iNOS、核因子-κB（NF-κB）、抑制性κB（IκBα）、c-Jun N-末端激酶（JNK）、p38 和细胞外信号调节激酶（ERK）的表达。结果表明，EA 以剂量依赖性方式抑制 IL-1β诱导的胶原酶-3（MMP-13）、NO 和 PGE2 的产生。IL-1β 上调 COX-2 和 iNOS 的表达，EA 抑制了这种上调。此外，EA 抑制了 IL-1β诱导的 NF-κB 和丝裂原活化蛋白激酶（MAPK）的激活。总之，EA 有效减轻了 IL-1β诱导的骨关节炎软骨细胞炎症反应，这表明 EA 可能是治疗骨关节炎的一种潜在药物。
