Department of Pharmacology, College of Medicine, Kangwon National University, Chuncheon 200-701, Korea.
Korean J Physiol Pharmacol. 2011 Feb;15(1):9-15. doi: 10.4196/kjpp.2011.15.1.9. Epub 2011 Feb 28.
Although various derivatives of caffeic acid have been reported to possess a wide variety of biological activities such as protection of neuronal cells against excitotoxicity, the biological activity of 1-docosanoyl cafferate (DC) has not been examined. The objective of the present study was to evaluate the anti-inflammatory effects of DC, isolated from the stem bark of Rhus verniciflua, on lipopolysaccharide (LPS)-stimulated BV2 microglial cells. Pretreatment of cells with DC significantly attenuated LPS-induced NO production, and mRNA and protein expression of iNOS in a concentration-dependent manner. DC also significantly suppressed LPS-induced release of cytokines such as TNF-α and IL-1β . Consistent with the decrease in cytokine release, DC dose-dependently and significantly attenuated LPS-induced mRNA expression of these cytokines. Furthermore, DC significantly suppressed LPS-induced degradation of IKB, which retains NF-kB in the cytoplasm. Therefore, nuclear translocation of NF-kB induced by LPS stimulation was significantly suppressed with DC pretreatment. Taken together, the present study suggests that DC exerts its anti-inflammatory activity through the suppression of NF-kB translocation to the nucleus.
虽然已经报道了咖啡酸的各种衍生物具有广泛的生物活性，如保护神经元细胞免受兴奋毒性，但是 1-二十二烷酰基咖啡酸（DC）的生物活性尚未被检测到。本研究的目的是评估从盐肤木茎皮中分离得到的 DC 对脂多糖（LPS）刺激的 BV2 小胶质细胞的抗炎作用。细胞用 DC 预处理可显著抑制 LPS 诱导的 NO 产生，以及 iNOS 的 mRNA 和蛋白表达呈浓度依赖性。DC 还显著抑制 LPS 诱导的细胞因子如 TNF-α和 IL-1β的释放。与细胞因子释放减少一致，DC 剂量依赖性地显著抑制这些细胞因子的 LPS 诱导的 mRNA 表达。此外，DC 显著抑制 LPS 诱导的 IKB 降解，IKB 将 NF-kB 保留在细胞质中。因此，用 DC 预处理可显著抑制 LPS 刺激诱导的 NF-kB 向核内易位。总之，本研究表明 DC 通过抑制 NF-kB 向核内易位发挥其抗炎活性。
