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Prenylated Polyphenols from Broussonetia kazinoki as Inhibitors of Nitric Oxide Production

机译:棉铃木中的烯丙基化多酚可作为一氧化氮的抑制剂

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摘要

Excessive nitric oxide (NO) production by macrophages has been involved in inflammatory diseases. Seven polyphenols (>1–>7) were isolated from Broussonetia kazinoki (B. kazinoki) and investigated as potential inhibitors of NO overproduction in lipopolysaccharide (LPS)-activated RAW 264.7 cells. Among them, four prenylated polyphenols (>2–>4 and >6) with a catechol moiety efficiently suppressed the LPS-induced high level of NO with IC50 values of less than 6 µM. The compounds >2–>4 and >6 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 B. kazinoki might be beneficial for treatment of inflammatory diseases.
机译:巨噬细胞产生的一氧化氮(NO)过多与炎症性疾病有关。从百日草(B. kazinoki)(B. kazinoki)中分离了7种多酚(> 1 – > 7 ),并作为脂多糖(LPS)激活的RAW 264.7细胞中NO过量产生的潜在抑制剂进行了研究。其中,具有邻苯二酚部分的四种烯丙基化多酚(> 2 – > 4 和> 6 )可有效抑制LPS诱导的高水平NO(IC50)值小于6 µM。化合物> 2 – > 4 和> 6 也会减弱诱导型一氧化氮合酶(iNOS)的蛋白质和mRNA水平。此外,它们通过抑制LPS活化巨噬细胞中抑制性κB-α(I-κB-α)的降解和NF-κB向核内的转移而抑制了核因子κB(NF-κB)的活性。综上所述,这些发现表明,来自kazinoki的多酚可能对治疗炎性疾病有益。

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