Beijing Key Laboratory of Drug Target and Screening Research, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, PR China.
Int Immunopharmacol. 2013 Feb;15(2):303-8. doi: 10.1016/j.intimp.2012.11.014. Epub 2012 Dec 4.
Ethyl salicylate 2-O-β-d-glucoside (ESG) is a derivative of natural salicylate isolated from Gaultheria yunnanensis (Franch.) Rehder, it has been used for the treatments of rheumatoid arthritis, swelling and pain. The aim of this study was to evaluate the anti-inflammatory effects of ESG and explore the anti-inflammatory mechanisms. We found that ESG had potent anti-inflammatory effects on the lipopolysaccharide (LPS)-activated murine macrophages RAW264.7. ESG exerted a dose-dependent inhibition of the LPS-stimulated release of the pro-inflammatory cytokines TNF-α and IL-1β. Moreover, it significantly inhibited LPS-stimulated the production of NO and PGE2 by repressing the expression of iNOS and COX protein respectively. Western blot analysis showed that ESG prominently inhibited LPS-induced activation of NF-κB in RAW264.7 cells by blocking phosphorylation of inhibitor IκBα and p65. Consistent with these results, we found that ESG prevented the nuclear translocation of NF-κB induced by LPS. Our study suggests that ESG may be effective in the treatment of inflammatory diseases by inhibiting the pro-inflammatory cytokine production and regulating the NF-κB signal pathway.
水杨酸乙酯 2-O-β-D-葡萄糖苷（ESG）是从云南产白珠树（Gaultheria yunnanensis （Franch.） Rehder）中分离出的天然水杨酸衍生物，已用于治疗类风湿性关节炎、肿胀和疼痛。本研究旨在评价 ESG 的抗炎作用，并探讨其抗炎机制。我们发现 ESG 对脂多糖（LPS）激活的小鼠巨噬细胞 RAW264.7 具有很强的抗炎作用。ESG 呈剂量依赖性抑制 LPS 刺激的促炎细胞因子 TNF-α和 IL-1β的释放。此外，它通过分别抑制 iNOS 和 COX 蛋白的表达，显著抑制 LPS 刺激的 NO 和 PGE2 的产生。Western blot 分析表明，ESG 通过阻断抑制物 IκBα和 p65 的磷酸化，显著抑制 LPS 诱导的 RAW264.7 细胞中 NF-κB 的激活。与这些结果一致，我们发现 ESG 可防止 LPS 诱导的 NF-κB 核转位。我们的研究表明，ESG 通过抑制促炎细胞因子的产生和调节 NF-κB 信号通路，可能对炎症性疾病的治疗有效。
