霉酚酸抑制内皮细胞核因子—κB的活性

目的：研究霉酚酸对内皮细胞核因子－κB（NF－κB）活力及其抑制因子IκBa的影响。方法：利用凝胶迁移率实验（EMSA）检测不同浓度的霉酚酸对一般培养状态和佛波脂（PMA）激活的内皮细胞的NF－κB活力影响。并用Western blot方法检测霉酚酸对NF－κB抑制因子IκBa的作用。结果：PMA显著激活内皮细胞中的NF－κB活性。降低IκBα的蛋白水平,霉酚酸抑制PMA刺激的内皮细胞NF－κB活性升高,并抑制内皮细胞胞浆IκBα蛋白的降解,结论：霉酚酸可影响内皮细胞NF－κB的活性,这可能是MPA影响内皮细胞功能的作用机制之一。

Inhibition of mycophenolic acid on NF-kappaB activity in human endothelial cells

AIM: To examine the effect of mycophenolic acid (MPA) on the activity of nuclear factor-kappaB (NF-kappaB) and its inhibitor (IkappaBalpha) in 4-phorbal-12-myristate-13-acetate (PMA) stimulated and non-stimulated human umbilical vein endothelial cells (HUVEC). METHODS: MPA at various concentrations were applied to cultured HUVEC, pre-incubated or not pre-incubated with PMA (100 microg/L for 30 min). The activity of NF-kappaB in endothelial cells was measured with electrophoretic mobility shift assays (EMSA), and IkappaBalpha protein levels were detected by Western blot method. RESULTS: Incubation with PMA was found to result in rapid increment of NF-kappaB activity in cultured HUVEC. MPA treatment decreased the activities of NF-kappaB, both in PMA treatment and un-treatment HUVEC. Protein level of IkappaBalpha was decreased in PMA-treatment HUVEC. MPA treatment increased IkappaBalpha protein levels in both PMA-treatment and un-treatment HUVEC. CONCLUSION: MPA is a potent inhibitor of NF-kappaB activation in endothelial cells, which might explain its beneficial effect in endothelial cells.