LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
CNC.IBILI, Faculty of Pharmacy, University of Coimbra, Health Sciences Campus, 3000-548 Coimbra, Portugal.
Int J Mol Sci. 2020 Sep 20;21(18):6897. doi: 10.3390/ijms21186897.
Due to their large spectrum of bioactive properties, much attention has recently been drawn to phlorotannins-i.e., phenolic compounds characteristic from brown macroalgae. This study aimed to evaluate the antioxidant and anti-inflammatory properties of phlorotannin extracts and purified fractions. Overall, the crude extract and its ethyl acetate fraction (EtOAc) showed good radical scavenging activity, particularly towards nitric oxide (NO). Subsequent subfractions of EtOAc (F1 to F9) with different molecular weights were then shown to inhibit lipopolysaccharide-induced NO production in macrophages, with stronger effects being observed for fractions of lower MWs. Of the three intracellular markers analyzed, inducible NO synthase showed the highest sensitivity to almost all the phlorotannin-rich samples, followed by interleukin 1β and cyclooxygenase 2, which was only inhibited by F2. Furthermore, this subfraction inhibited the phosphorylation and degradation of inhibitory protein κBα, thus preventing the activation of NF-κB and blocking the inflammatory cascade at the transcriptional level. This sample was characterized by the presence of a major compound with a deprotonated molecular ion at 507 with a fragmentation pattern coherent with that of a phlorotannin derivative. Overall, this work unveiled some of the mechanistic aspects behind the anti-inflammatory capacity of phlorotannins from , endorsing its use as a possible natural source of anti-inflammatory compounds.
由于其具有广泛的生物活性特性,近年来人们对 phlorotannins(即来自褐藻的酚类化合物)给予了极大关注。本研究旨在评估 phlorotannin 提取物和纯化馏分的抗氧化和抗炎特性。总的来说,粗提取物及其乙酸乙酯馏分(EtOAc)表现出良好的自由基清除活性,特别是对一氧化氮(NO)。随后对 EtOAc 的亚馏分(F1 至 F9)进行了研究,这些亚馏分具有不同的分子量,它们能够抑制巨噬细胞中脂多糖诱导的 NO 产生,其中低分子量的馏分效果更强。在所分析的三种细胞内标志物中,诱导型一氧化氮合酶对几乎所有富含 phlorotannin 的样品表现出最高的敏感性,其次是白细胞介素 1β 和环氧化酶 2,只有 F2 能够抑制其表达。此外,该亚馏分还抑制了抑制蛋白 κBα 的磷酸化和降解,从而阻止了 NF-κB 的激活,并在转录水平阻断了炎症级联反应。该样品的特征是存在一个主要化合物,其去质子分子离子在 507 处,其碎片模式与 phlorotannin 衍生物的碎片模式一致。总的来说,这项工作揭示了 phlorotannins 抗炎能力的一些机制方面,支持将其作为抗炎化合物的天然来源。