Tilianin, a representative flavonoid ingredient of Dracocephalum moldavica L., has been used to treat several diseases for centuries, including atherosclerosis (AS). However, pharmacological mechanisms underlying its biological functions remain elusive. In the present study, we investigated the anti-AS mechanisms of tilianin through establishing in vitro models using three types of cells that contributed to AS progression, including macrophage, vascular smooth muscle cells and human umbilical vein endothelial cells, which were proved to be involve in LPS/TNF-α/oxidized low density lipoprotein (ox-LDL)-induced inflammation and ox-LDL induced foam cell formation. Our results indicate that tilianin significantly suppressed LPS induced inflammatory responses on macrophage and remarkably inhibited TNF-α induced VSMCs proliferation and migration. Furthermore, the anti-inflammatory effect of tilianin on macrophages and VSMCs was proved to be mainly by downregulating TNF-α/NF-κB pathway. Moreover, our results demonstrate that tilianin significantly ameliorated ox-LDL induced macrophages oriented foam cells formation through repressing mRNA expression of SR-A1 and inducting the expression of genes related to cholesterol efflux including SRB-1 and ABCA1. However, tilianin had no effect on ox-LDL induced HUVECs injury.

中文翻译：

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Tilianin通过下调NF-κB途径和泡沫细胞形成抑制炎症的动脉粥样硬化保护机制。

Tilianin是Dracocephalum Moldavica L.的代表类黄酮成分，已经被用于治疗包括动脉粥样硬化（AS）在内的多种疾病。但是，其生物学功能所依据的药理机制仍然难以捉摸。在本研究中，我们通过建立体外模型来研究tilianin的抗AS机制，该模型使用了三种类型的有助于AS进展的细胞，包括巨噬细胞，血管平滑肌细胞和人脐静脉内皮细胞，这些细胞被证明参与其中LPS /TNF-α/氧化的低密度脂蛋白（ox-LDL）诱导的炎症和ox-LDL诱导的泡沫细胞形成的过程。我们的结果表明，tilianin显着抑制LPS诱导的巨噬细胞炎症反应，并显着抑制TNF-α诱导的VSMC增殖和迁移。此外，tilianin对巨噬细胞和VSMC的抗炎作用主要是通过下调TNF-α/NF-κB途径来实现的。此外，我们的结果表明，tilianin通过抑制SR-A1的mRNA表达并诱导与胆固醇外排有关的基因（包括SRB-1和ABCA1）的表达，显着改善了ox-LDL诱导的巨噬细胞定向泡沫细胞的形成。然而，tilianin对ox-LDL诱导的HUVEC损伤没有影响。我们的结果表明，tilianin通过抑制SR-A1的mRNA表达并诱导与胆固醇流出相关的基因（包括SRB-1和ABCA1）表达，从而显着改善了ox-LDL诱导的巨噬细胞定向泡沫细胞的形成。然而，tilianin对ox-LDL诱导的HUVEC损伤没有影响。我们的结果表明，tilianin通过抑制SR-A1的mRNA表达并诱导与胆固醇流出相关的基因（包括SRB-1和ABCA1）的表达，显着改善了ox-LDL诱导的巨噬细胞定向泡沫细胞的形成。然而，tilianin对ox-LDL诱导的HUVEC损伤没有影响。