Murakami A, Gao G, Omura M, Yano M, Ito C, Furukawa H, Takahashi D, Koshimizu K, Ohigashi H
Department of Biotechnological Science, Faculty of Biology-Oriented Science and Technology, Kinki University, Iwade-Uchita, Wakayama, Japan.
Bioorg Med Chem Lett. 2000 Jan 3;10(1):59-62. doi: 10.1016/s0960-894x(99)00578-8.
We investigated the suppressive effects of 16 coumarin-related compounds on both lipopolysaccharide (LPS)- and interferon (IFN)-gamma-induced nitric oxide (NO) generation in a mouse macrophage cell line, RAW 264.7. Notably, coumarins possessing prenyl unit(s) were found to be highly active, a tendency consistent with our previous study. Among the coumarins tested, 1,1-dimethylallylcoumarins showed the highest inhibitory activity. Western blotting analysis revealed that they inhibited NO generation by suppressing inducible NO synthase (iNOS) protein expression. Our ongoing studies suggest that coumarins are prominent natural compounds that attenuate excessive and prolonged NO generation at inflammatory sites.
我们研究了16种香豆素相关化合物对小鼠巨噬细胞系RAW 264.7中脂多糖(LPS)和干扰素(IFN)-γ诱导的一氧化氮(NO)生成的抑制作用。值得注意的是,含有异戊烯基单元的香豆素具有高活性,这一趋势与我们之前的研究一致。在所测试的香豆素中,1,1-二甲基烯丙基香豆素表现出最高的抑制活性。蛋白质印迹分析表明,它们通过抑制诱导型一氧化氮合酶(iNOS)蛋白表达来抑制NO生成。我们正在进行的研究表明,香豆素是一类重要的天然化合物,可减轻炎症部位过度且持续的NO生成。