Biospectrum Life Science Institute, Eines Platz 11th FL, 442-13 Sangdaewon Dong, Seoungnam City, 462-807 Gyunggi Do, Republic of Korea.
Food Chem Toxicol. 2011 Oct;49(10):2580-5. doi: 10.1016/j.fct.2011.06.076. Epub 2011 Jul 13.
Although (-)-α-bisabolol, a natural monocyclic sesquiterpene alcohol, is often used as a cosmetic soothing supplement, little is known about its mechanisms of anti-inflammatory effects. Therefore, this study was designed to investigate anti-inflammatory effects of (-)-α-bisabolol and its mechanisms of action. In this study, we found that (-)-α-bisabolol inhibited lipopolysaccharide (LPS)-induced production of nitric oxide (NO) and prostaglandin E(2) (PGE(2)) in RAW264.7 cells. In addition, expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) genes was reduced, as evidenced by Western blot and luciferase reporter assays for COX-2 and iNOS. To assess the mechanism of the anti-inflammatory property of (-)-α-bisabolol, its effects on the activity of AP-1 and NF-κB promoters were examined. LPS-induced activation of AP-1 and NF-κB promoters was significantly reduced by (-)-α-bisabolol. Consistently, (-)-α-bisabolol reduced LPS-induced phosphorylation of IκBα. In addition, while LPS-induced phosphorylation of ERK and p38 was attenuated by (-)-α-bisabolol, significant changes in the level of phosphorylated JNK were not observed. Our results indicate that (-)-α-bisabolol exerts anti-inflammatory effects by downregulating expression of iNOS and COX-2 genes through inhibition of NF-κB and AP-1 (ERK and p38) signaling.
虽然（-）-α- 倍半水芹醇是一种常用的天然单环倍半萜醇，常被用作化妆品的舒缓补充剂，但对其抗炎作用的机制知之甚少。因此，本研究旨在研究（-）-α- 倍半水芹醇的抗炎作用及其作用机制。在这项研究中，我们发现（-）-α- 倍半水芹醇抑制脂多糖（LPS）诱导的 RAW264.7 细胞中一氧化氮（NO）和前列腺素 E（2）（PGE（2））的产生。此外，通过 Western blot 和 COX-2 和 iNOS 的荧光素酶报告基因检测，发现环氧合酶-2（COX-2）和诱导型一氧化氮合酶（iNOS）基因的表达减少。为了评估（-）-α- 倍半水芹醇抗炎特性的机制，研究了其对 AP-1 和 NF-κB 启动子活性的影响。LPS 诱导的 AP-1 和 NF-κB 启动子的激活被（-）-α- 倍半水芹醇显著抑制。一致地，（-）-α- 倍半水芹醇减少了 LPS 诱导的 IκBα磷酸化。此外，虽然（-）-α- 倍半水芹醇减弱了 LPS 诱导的 ERK 和 p38 的磷酸化，但观察到磷酸化 JNK 的水平没有显著变化。我们的结果表明，（-）-α- 倍半水芹醇通过抑制 NF-κB 和 AP-1（ERK 和 p38）信号通路下调 iNOS 和 COX-2 基因的表达来发挥抗炎作用。
