Djoko Bambang, Chiou Robin Y-Y, Shee Jia-Jen, Liu Yi-Wen
Department of Food Science, College of Life Sciences, National Chiayi University, Chiayi, Taiwan.
J Agric Food Chem. 2007 Mar 21;55(6):2376-83. doi: 10.1021/jf062741a. Epub 2007 Feb 23.
Biological activities of peanut stilbenoids, mainly resveratrol and its derivatives, have attracted increased attention and interest because of peanut being a potent producer and a dietary channel to convey these polyphenols to the human body. As arachidin-1 and piceatannol are structurally close to resveratrol, it is worthy to investigate their immunological activities on inhibition of lipopolysaccharide (LPS)-induced production of PGE2 and NO and mediation of the related transcription factors (NF-kappaB and C/EBP) of RAW 264.7 macrophage cells. Productions of PGE2 and NO were inhibited by all the test stilbenoids in a dose-dependent manner while gene and protein expressions of COX-2 and iNOS were not inhibited. As shown by NF-kappaB-driven luciferase assay, LPS-induced NF-kappaB activities were also reduced by the stilbenoids. In further, when these stilbenoids were subjected to monitoring their inhibitory effectiveness on LPS-induced transcription factor expressions of C/EBPdelta and C/EBPbeta, only C/EBPdelta expressions were reduced. Thus, these stilbenoids were effective in inhibition of PGE2- or NO-mediated inflammation and NF-kappaB- or C/EBPdelta-mediated inflammatory gene expression. In comparison, the highest inhibitory activity on LPS-induced PGE2/NO production, C/EBPdelta gene expression, and NF-kappaB activation was piceatannol which was followed in order by arachidin-1 and resveratrol. The observed anti-inflammatory activities of these peanut stilbenoids are of merit in further consideration for nutraceutical applications.
花生芪类化合物,主要是白藜芦醇及其衍生物,因其在花生中含量丰富且是人体摄入这些多酚类物质的饮食渠道,其生物活性已引起越来越多的关注。由于花生四烯酸-1和3,4,5-三甲氧基芪在结构上与白藜芦醇相近,因此研究它们对脂多糖(LPS)诱导的RAW 264.7巨噬细胞产生前列腺素E2(PGE2)和一氧化氮(NO)的抑制作用以及对相关转录因子(核因子κB和C/EBP)的调节作用,具有重要意义。所有受试芪类化合物均呈剂量依赖性抑制PGE2和NO的产生,但对COX-2和诱导型一氧化氮合酶(iNOS)的基因和蛋白表达无抑制作用。核因子κB驱动的荧光素酶检测结果表明,芪类化合物也能降低LPS诱导的核因子κB活性。此外,当检测这些芪类化合物对LPS诱导的C/EBPδ和C/EBPβ转录因子表达的抑制效果时,发现只有C/EBPδ的表达受到抑制。因此,这些芪类化合物能有效抑制PGE2或NO介导的炎症以及核因子κB或C/EBPδ介导的炎症基因表达。相比之下,3,4,5-三甲氧基芪对LPS诱导的PGE2/NO产生、C/EBPδ基因表达和核因子κB激活的抑制活性最高,其次是花生四烯酸-1和白藜芦醇。这些花生芪类化合物的抗炎活性在营养保健品应用中值得进一步研究。