Chien Shih-Chang, Tseng Yen-Hsueh, Hsu Wei-Ning, Chu Fang-Hua, Chang Shang-Tzen, Kuo Yueh-Hsiung, Wang Sheng-Yang
Nat Prod Commun. 2014 Nov;9(11):1589-90.
Dendropanax dentiger has been used as a folk medicine since ancient times. In our current study, we observed that D. dentiger exhibited a significant anti-inflammatory activity, which could efficiently inhibit nitric oxide (NO) production in the lipopolysaccharide (LPS)-induced macrophage inflammation assay. (9Z,16S)-16-Hydroxy-9,17-octadecadiene-12,14-diynoic acid (HODA) was isolated from the leaves of D. dentiger following a bioactivity guided fractionation protocol. Our data indicated that HODA significantly inhibited the NO production in LPS-induced RAW 264.7 murine macrophage cells (IC50 = 4.28 μM). Consistent with these observations, the mRNA and protein expression levels of iNOS were also inhibited by HODA in a dose-dependent manner. HODA also reduced the translocation of NF-κB into nuclear fractions. Meanwhile, HODA enhanced Nrf-2 activation and its downstream antioxidant gene HO-1. We concluded that HODA possessed significant anti-inflammatory and anti-oxidative activity; the compound may have a potential for development as a chemoprevention agent.
齿叶树参自古以来就被用作民间药物。在我们目前的研究中,我们观察到齿叶树参表现出显著的抗炎活性,在脂多糖(LPS)诱导的巨噬细胞炎症试验中能有效抑制一氧化氮(NO)的产生。通过生物活性导向的分级分离方案,从齿叶树参的叶子中分离出了(9Z,16S)-16-羟基-9,17-十八碳二烯-12,14-二炔酸(HODA)。我们的数据表明,HODA显著抑制LPS诱导的RAW 264.7小鼠巨噬细胞中NO的产生(IC50 = 4.28 μM)。与这些观察结果一致,HODA还以剂量依赖性方式抑制诱导型一氧化氮合酶(iNOS)的mRNA和蛋白表达水平。HODA还减少了核因子κB(NF-κB)向核部分的转位。同时,HODA增强了核因子E2相关因子2(Nrf-2)的激活及其下游抗氧化基因血红素加氧酶-1(HO-1)。我们得出结论,HODA具有显著的抗炎和抗氧化活性;该化合物可能具有作为化学预防剂开发的潜力。