First Clinical Hospital of Harbin Medical University, Harbin 150001, China.
First Clinical Hospital of Harbin Medical University, Harbin 150001, China.
Int Immunopharmacol. 2019 Jul;72:301-307. doi: 10.1016/j.intimp.2019.04.006. Epub 2019 Apr 18.
Oridonin, the major terpene isolated from Rabdosia rubescens, has been used as dietary supplement. Recently, it has been known to exhibit anti-inflammatory effect. This study we employed an in vitro model of LPS-stimulated human gingival fibroblasts to investigate the anti-inflammatory effects and mechanism of oridonin. Oridonin (10-30 μg/mL) was administrated 1 h before LPS treatment. The results showed that oridonin significantly inhibited inflammatory mediators PGE, NO, IL-6, and IL-8 production. Immunoblotting experiments revealed that oridonin reduced the expression of phosphorylation levels of NF-κB p65 and IκBα. Furthermore, the expression of PPARγ was up-regulated by the treatment of oridonin. Further studies showed that PPARγ inhibitor GW9662 could reverse the inhibition of oridonin on PGE, NO, IL-6, and IL-8 production. In conclusion, oridonin inhibited LPS-induced microglia activation through activating PPARγ.
冬凌草甲素是从冬凌草中分离得到的主要萜类化合物，已被用作膳食补充剂。最近，它被认为具有抗炎作用。本研究采用脂多糖刺激的人牙龈成纤维细胞体外模型，探讨冬凌草甲素的抗炎作用及其机制。冬凌草甲素（10-30μg/ml）在 LPS 处理前 1 小时给药。结果表明，冬凌草甲素能显著抑制 PGE、NO、IL-6 和 IL-8 等炎症介质的产生。免疫印迹实验显示，冬凌草甲素降低了 NF-κB p65 和 IκBα 的磷酸化水平。此外，冬凌草甲素上调了 PPARγ 的表达。进一步的研究表明，PPARγ 抑制剂 GW9662 可逆转冬凌草甲素对 PGE、NO、IL-6 和 IL-8 产生的抑制作用。综上所述，冬凌草甲素通过激活 PPARγ 抑制 LPS 诱导的小胶质细胞激活。
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