硫酸化修饰对玄参多糖抗炎活性的影响

Effects of Sulfation Modification on Anti-inflammatory Activity of Polysaccharides from Scrophulariae Radix

关键词:  玄参|多糖|硫酸化多糖|细胞因子|NF-κB

Key words:  Scrophulariae Radix|polysaccharide|sulfated polysaccharide|cytokines|NF-κB

摘要:

目的 比较研究玄参多糖经硫酸化修饰前后其抗炎活性的变化及机制。方法 ♂ ICR小鼠经腹腔注射脂多糖（lipopolysaccharide，LPS）建立急性炎症反应模型，分别给予玄参多糖和硫酸化玄参多糖进行药物干预，以阿司匹林作为阳性对照，运用Real time RT-PCR检测肝脏组织白介素-6（interleukin-6，IL-6）、白介素-1β（interleukin-1β，IL-1β）、单核细胞趋化蛋白-1（monocyte chemoattractant protein-1，MCP-1）和肿瘤坏死因子-α（tumor necrosis factor-α，TNF-α）的mRNA表达，运用ELISA检测血清中的IL-6、IL-1β、MCP-1和TNF-α的蛋白表达，运用Western blotting法检测肝脏组织中核因子κB（nuclear factor-kappaB，NF-κB）、phospho-NF-κB的表达水平。结果 硫酸化玄参多糖和玄参多糖均可显著抑制LPS诱导的IL-6、IL-1β、MCP-1和TNF-α mRNA和蛋白表达增加，玄参多糖经硫酸化修饰后，其抗炎活性显著增强，其作用机制可能与调控NF-κB信号转导通路活化有关。结论 硫酸化修饰可显著提高玄参多糖的抗炎活性，具有更好的应用前景，为玄参的开发应用提供了理论基础。

Abstract:

OBJECTIVE To comparative study on the changes and mechanisms of anti-inflammatory activity of polysaccharide from Scrophulariae Radix before and after sulfation modification. METHODS The systemic inflammatory model was established by intraperitoneal injection of lipopolysaccharide(LPS) in male ICR mice. Then polysaccharides from Scrophulariae Radix and sulphated polysaccharides from Scrophulariae Radix were used for drug intervention and aspirin was used as a positive control. Real-time reverse transcription polymerase chain reaction(RT-PCR) was used to detect the mRNA expression of interleukin-6(IL-6), interleukin-1β(IL-1β), monocyte chemoattractant protein-1(MCP-1) and tumor necrosis factor-α(TNF-α) in liver tissue. The protein expression of IL-6, IL-1β, MCP-1 and TNF-α in serum was detected by ELISA. The level of nuclear factor-kappaB(NF-κB) and phospho-NF-κB in liver tissue was detected by Western blotting. RESULTS The results showed that both sulphated polysacharides from Scrophulariae Radix and polysacharides from Scrophulariae Radix significantly inhibited LPS-induced over-expression of IL-6 IL-1β, MCP-1 and TNF-α in both mRNA and protein levels. After sulfation modification, polysacharides from Scrophulariae Radix exerted more significant anti-inflammatory activities and the mechanism might be associated with activation of NF-κB signaling pathway. CONCLUSION Sulfation modification of polysacharides from Scrophulariae Radix can stronger anti-inflammatory efficacy and has better application prospects, which provides a theoretical basis for the development and application of Scrophulariae Radix.