College of Pharmacy and Research Center for Cell Fate Control, Sookmyung Women's University, Seoul 04310, Korea.
School of Industrial Bio-Pharmaceutical Science, Semyung University, Jecheon, Chungbuk 27136, Korea.
Molecules. 2018 Mar 12;23(3):639. doi: 10.3390/molecules23030639.
Excessive nitric oxide (NO) production by macrophages has been involved in inflammatory diseases. Seven polyphenols (-) were isolated from and investigated as potential inhibitors of NO overproduction in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Among them, four prenylated polyphenols (- and ) with a catechol moiety efficiently suppressed the LPS-induced high level of NO with IC values of less than 6 µM. The compounds - and also attenuated protein and mRNA levels of inducible nitric oxide synthase (iNOS). Moreover, they suppressed the nuclear factor κB (NF-κB) activity by inhibiting the degradation of inhibitory-κB-α (I-κB-α) and the translocation of NF-κB into the nucleus in LPS-activated macrophages. Taken together, these findings suggest that polyphenols from might be beneficial for treatment of inflammatory diseases.
巨噬细胞中过量的一氧化氮（NO）产生与炎症性疾病有关。从 中分离出 7 种多酚（-），并将其作为潜在的脂多糖（LPS）激活的 RAW 264.7 细胞中过量 NO 产生的抑制剂进行研究。其中，四个具有儿茶酚结构的香叶烯基化多酚（-和 ）能有效抑制 LPS 诱导的高水平 NO，IC 值低于 6µM。化合物 - 和 还能降低诱导型一氧化氮合酶（iNOS）的蛋白和 mRNA 水平。此外，它们通过抑制 LPS 激活的巨噬细胞中抑制性κB-α（I-κB-α）的降解和 NF-κB 向核内易位来抑制核因子κB（NF-κB）的活性。总之，这些发现表明 中的多酚可能有益于治疗炎症性疾病。
