藏药绿萝花相关单体对3T3-L1细胞内PPARs蛋白表达的影响

Effects of Components from Edgeworthia gardneri Meissn on PPARs Level in 3T3-L1 Cells

目的研究藏药绿萝花中12种单体化合物[水杨酸、去甲基丁香色原酮、银锻苷、十五烷酸、伞形酮、西瑞香素、结香酸、结香苷C、(3S)-1,2,3,4-四氢-β-咔啉-3-羧酸、gardenrd A、西瑞香素-5-O-β-D-吡喃葡萄糖苷、西瑞香素-5-O-β-D-吡喃葡萄糖基-(1→2)-O-β-D-吡喃葡萄糖苷]对过氧化物酶体增殖因子活化受体(PPARs)蛋白表达水平的影响。方法采用高胰岛素诱导建立3T3-L1胰岛素抵抗细胞模型,以降低细胞中PPARs水平,并给予12种绿萝花单体化合物低、高剂量(40、80μmol·L-1)进行干预;采用蛋白质免疫印迹(Western Blot)法检测模型细胞PPAR-α/β/γ蛋白表达情况。结果与正常组比较,模型组3T3-L1胰岛素抵抗细胞中的PPAR-α/β/γ蛋白表达水平均显著降低(P <0.01)。与模型组比较,西瑞香素、结香苷C、gardenrd A、西瑞香素-5-O-β-D-吡喃葡萄糖、西瑞香素-5-O-β-D-吡喃葡萄糖基-(1→2)-O-β-D-吡喃葡萄糖苷高剂量组的PPAR-α蛋白表达显著升高(P <0.05,P <0.01);去甲丁香色原酮低剂量组、西瑞香素高剂量组及西瑞香素-5-O-β-D-吡喃葡萄糖基-(1→2)-O-β-D-吡喃葡萄糖苷高、低剂量组的PPAR-β蛋白表达水平显著提高(P <0.05,P <0.01);十五烷酸高剂量组、gardenrd A高剂量组、西瑞香素-5-O-β-D-吡喃葡萄糖基-(1→2)-O-β-D-吡喃葡萄糖苷高剂量组及西瑞香素高、低剂量组的PPAR-γ蛋白表达水平显著提高(P <0.05,P <0.01)。结论藏药绿萝花中的单体化合物西瑞香素、西瑞香素-5-O-β-D-吡喃葡萄糖基-(1→2)-O-β-D-吡喃葡萄糖苷、gardenrd A能够三重/双重激活3T3-L1胰岛素抵抗细胞内的PPARs蛋白表达水平,为潜在的PPARs激动剂。

Objective To study the effects of 12 compounds(pentadecanoic acid, umbelliferone, daphnoretin,salicylic acid, noreugenin, tiliroside, edgeworic acid, edgeworoside C,(3 S)-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid, gardenrd A, daphnoretin-5-O-β-D-glucopyranoside, daphnoretin-5-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranoside) from Edgeworthia gardneri Meissn on peroxisome proliferator-activated receptors(PPARs) level. Methods 3 T3-L1 cell model of insulin resistance was established to decreasingthe PPAR-α/β/γ level,and effects of 12 compounds at 2 different concentrations on increasing PPARs level wereinvestigated through Western Blot. Results Compared with the normal group, the PPAR-α/β/γ levels weresignificantly decreased(P < 0.01). Compared with the model group,daphnoretin,edgeworoside C,gardenrd A,daphnoretin-5-O-β-D-glucopyranoside,daphnoretin-5-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranosideat their concentrations of 80 μmol·L^-1 significantly increased the PPAR-α level(P < 0.05, P < 0.01),umbelliferone at 40 μmol·L^-1,daphnoretin at 80 μmol·L^-1,daphnoretin-5-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranoside at both 40 and 80 μmol·L^-1 concentrations significantly increased the PPAR-β level(P < 0.05,P < 0.01). Salicylic acid,umbelliferone,gardenrd A,daphnoretin-5-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranoside at 80 μmol·L-1,daphnoretin at both 40 and 80 μmol·L^-1 concentrations significantly increased thePPAR-γ level(P < 0.05, P < 0.01). Conclusion The daphnoretin, gardenrd A, daphnoretin-5-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranoside of Edgeworthia gardneri Meissn can increased the PPARs level inthe 3 T3-L1 cell model of insulin resistance,which are potential PPARs agonists.