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[摘要]
目的 探究芒果Mangifera indica核仁的抗炎活性,并筛选出其中具有抗炎作用的药效物质。方法 利用二甲苯诱导的小鼠耳肿胀模型和肿瘤坏死因子-α(TNF-α)诱导的人胚肾细胞293(HEK-293)炎症模型对芒果核仁提取物的抗炎作用进行评价,并采用UPLC-Q/TOF结合核因子-κB(NF-κB)萤光素酶报告基因检测系统进行谱效关系研究,筛选芒果核仁提取物中具有抗炎活性的药效物质。结果 芒果核仁提取物能显著改善小鼠耳廓的肿胀情况并能显著抑制细胞中NF-κB的表达;经UPLC-Q/TOF谱效关系分析筛选出10个具有NF-κB抑制活性的化合物为芒果苷和没食子酸鞣质类化合物,后者包括:没食子酸、1-没食子酰-β-D-吡喃葡萄糖基-(1→4)-β-D-半乳糖苷、1-没食子酰-β-D-吡喃葡萄糖基-(1→6)-β-D-半乳糖苷、1,2,3-三-O-没食子酰-β-D-葡萄糖、1,2,3,4-四没食子酰-β-D-葡萄糖、1,2,3,4,6-五没食子酰葡萄糖、六没食子酰葡萄糖。结论 芒果核仁提取物具有较好的抗炎作用,芒果苷和没食子酸系列衍生物为其提取物中主要的抗炎活性物质。
[Key word]
[Abstract]
Objective To investigate the anti-inflammatory effects of Mangiferae Indicae Semen (MIS) and to screen its bioactive components on nuclear factor-κappa B (NF-κB) inhibition. Methods The anti-inflammatory effects of MIS were assessed in the swelling of mouse ear induced by dimethylbenzene and the HEK293 inflammatory models induced by TNF-α. UPLC-Q/TOF MS coupled with NF-κB activity luciferase reporter assay system was applied to detect the potential anti-inflammatory components in MIS extract. Results MIS extract could ameliorate the edema in swelling of mouse ear induced by dimethylbenzene. Ten components were screened to have the potential NF-κB inhibitory effects based on the bioactivity-integrated UPLC-Q/TOF assay system. MIS could contribute to the alleviation of inflammation in the swelling of mouse ear and inhibit the expression of NF-κB. Ten potential active ingredients were found to have anti-inflammatory effects as NF-κB inhibitors, which were mangiferin and gallotannins. The gallotannins included gallic acid, 1-galloyl-β-D-glucopyranosyl-(1→4)-β-D-galactopyranoside, 1-galloyl-β-D-glucopyranosyl- (l→6)-β-D-galactopyranoside, 1,2,3-tri-O-galloyl-β-D-glucose, 1,2,3,4-tetragalloyl-β-D-glucose, 1,2,3,4,6-pentagalloylglucose, and hexagalloylglucose. Conclusion Mangiferin and gallotannins are verified to be the main bioactive compounds in MIS.
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[基金项目]
广西中药药效研究重点实验室开放课题(14-045-12)