Department of Cardiology, First Affiliated Hospital of Soochow University, Soochow, China.
Pharmacol Rep. 2011;63(3):781-9. doi: 10.1016/s1734-1140(11)70590-4.
Puerarin (7,4'-dihydroxy-8-C-glucosylisoflavone) is the most abundant isoflavone-C-glucoside extracted from Radix puerariae, and it has been used for various medicinal purposes in traditional oriental medicine for thousands of years. In the present study, the ability of the puerarin to modulate inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and C reactive protein (CRP) expression and induce changes in the nuclear factor κB (NF-κB) pathway in RAW264.7 macrophage cells was examined. The protein and mRNA levels of lipopolysaccharide (LPS)-induced iNOS, COX-2 and CRP were determined in RAW246.7 macrophage cells. Inhibitor κB (I-κB) phosphorylation and p65NF-κB expression in RAW246.7 macrophage cells were also detected under our experimental conditions. The results indicated that puerarin inhibited the expression of LPS-induced iNOS, COX-2 and CRP proteins and also suppressed their mRNAs from RT-PCR experiments in RAW264.7 cells. Subsequently, we determined that the inhibition of iNOS, COX-2 and CRP expression was due to a dose-dependent inhibition of phosphorylation and degradation of I-κB, which resulted in the reduction of p65NF-κB nuclear translocation. These data suggested that the effect of puerarin-mediated inhibition of LPS-induced iNOS, COX-2 and CRP expression is attributed to suppressed NF-κB activation at the transcriptional level.
葛根素（7,4'-二羟基-8-C-葡萄糖基异黄酮）是从葛根中提取的最丰富的异黄酮-C-葡萄糖苷，在传统东方医学中已有数千年用于各种药用目的。在本研究中，研究了葛根素调节诱导型一氧化氮合酶（iNOS）、环氧化酶-2（COX-2）和 C 反应蛋白（CRP）表达的能力，并诱导 RAW264.7 巨噬细胞中核因子κB（NF-κB）途径的变化。在 RAW246.7 巨噬细胞中测定了脂多糖（LPS）诱导的 iNOS、COX-2 和 CRP 的蛋白和 mRNA 水平。在我们的实验条件下，还检测了 RAW246.7 巨噬细胞中抑制剂κB（I-κB）磷酸化和 p65NF-κB 表达。结果表明，葛根素抑制 LPS 诱导的 iNOS、COX-2 和 CRP 蛋白的表达，并通过 RAW264.7 细胞中的 RT-PCR 实验抑制其 mRNAs。随后，我们确定 iNOS、COX-2 和 CRP 表达的抑制是由于 I-κB 的磷酸化和降解的剂量依赖性抑制，导致 p65NF-κB 核易位减少。这些数据表明，葛根素介导的 LPS 诱导的 iNOS、COX-2 和 CRP 表达抑制作用归因于转录水平抑制 NF-κB 激活。
