獐牙菜苦苷的抗炎活性及其对NF-κB通路相关因子p65和IKK-α表达的影响

Anti-inflammatory Activity of Swertiamarin and Its Effect on the Expression of NF-κB Pathway-related Factors p65 and IKK-α

目的观察獐牙菜苦苷(Swertiamarin)的抗炎活性以及对核转录因子-κB(NF-κB)通路的调控作用。方法采用脂多糖(LPS)诱导小鼠巨噬细胞RAW264.7构建体外炎症模型,CCK-8法观察獐牙菜苦苷对细胞活性的影响,ELISA法检测其对炎症相关因子肿瘤坏死因子-α(TNF-α)、白介素-6(IL-6)表达的影响,RT-PCR法测定其对NF-κB通路相关因子p65和IKK-α的mRNA表达的影响。结果 100μg·mL^(-1)獐牙菜苦苷能降低细胞存活率,3.125～50μg·mL^(-1)浓度对细胞存活率无影响;25～50μg·mL^(-1)獐牙菜苦苷能降低炎症相关因子TNF-α及IL-6的释放;12.5～50μg·mL^(-1)獐牙菜苦苷能抑制p65的mRNA表达,50μg·mL^(-1)獐牙菜苦苷能抑制IKK-α的mRNA表达。结论獐牙菜苦苷对LPS诱导的炎症模型中TNF-α、IL-6的生成具有抑制作用,其机制可能与抑制NF-κB通路相关因子p65、IKK-α的表达有关。

OBJECTIVE To observe the anti-inflammatory activity of Swertiamarin and its regulation effect on the nuclear transcription factor-κB(NF-κB) pathway.METHODS Lipopolysaccharid(LPS) induced murine macrophage raw 264.7 cell was used to establish an inflammatory model in vitro.CCK-8 method was used to observe the effect of Swertiamarin on cell activity.ELISA was used to detect its effect on the expression of tumor necrosis factor-α(TNF-α) and interleukin-6(IL-6).RT-PCR was used to detect its effect on mRNA expression of NF-κB pathway related factors p65 and Ikk-α.RESULTS The 100 μg·mL 1 Swertiamarin could decrease the cell survival rate,and 3.12550 μg·mL 1 had no effect on the cell survival rate.The 2550 μg·mL 1 Swertiamarin could reduce the release of TNF-α and IL-6.It was found that 12.550 μg·mL 1 Swertiamarin could inhibit the mRNA expression of p65,and the mRNA expression of Ikk-α could be inhibited by 50 μg·mL 1 Swertiamarin.CONCLUSION Swertiamarin has inhibitory effect on TNF-α and IL-6 production in LPS-induced inflammatory model,and its mechanism may be related to the inhibition of the expression of p65 and IKK-α,which are related factors of NF-κB pathway.