Department of Natural Drugs, Faculty of Pharmacy, Masaryk University, Palackého třída 1946/1, 61200 Brno, Czech Republic.
Department of Molecular Pharmacy, Faculty of Pharmacy, Masaryk University, Palackého třída 1946/1, 61200 Brno, Czech Republic.
Bioorg Chem. 2020 Nov;104:104298. doi: 10.1016/j.bioorg.2020.104298. Epub 2020 Sep 19.
Extensive phytochemical analysis of the CHCl-soluble part of an ethanolic extract of branches and twigs of Broussonetia papyrifera led to the isolation of fourteen compounds, including a novel 5,11-dioxabenzo[b]fluoren-10-one derivative named broussofluorenone C (12). The isolated compounds 1-14 were characterized based on their NMR and HRMS data, and examined for their anti-inflammatory activities in LPS-stimulated THP-1 cells as well as for their cellular antioxidant effects. Compounds 7-10 and 12 showed inhibitory effects on NF-κB/AP-1 activation and compounds 7-9 were subsequently confirmed to suppress the secretion of both IL-1β and TNF-α in LPS-stimulated THP-1 cells more significantly than the prednisone used as a positive control. In the CAA assay, compound 10 exhibited the greatest antioxidant effect, greater than that of the quercetin used as a positive control. The results show possible beneficial effects and utilization of B. papyrifera wood in the treatment of inflammatory diseases as well as oxidative stress.
对构树嫩枝和小枝的乙醇提取物的 CHCl 可溶部分进行了广泛的植物化学分析,从中分离得到了 14 种化合物,包括一种名为构树酮 C(12)的新型 5,11-二氧苯并[b]荧蒽-10-酮衍生物。根据化合物的 NMR 和 HRMS 数据对分离得到的化合物 1-14 进行了表征,并研究了它们在 LPS 刺激的 THP-1 细胞中的抗炎活性以及细胞抗氧化作用。化合物 7-10 和 12 对 NF-κB/AP-1 激活具有抑制作用,化合物 7-9 随后被证实比用作阳性对照的泼尼松更能显著抑制 LPS 刺激的 THP-1 细胞中 IL-1β 和 TNF-α 的分泌。在 CAA 测定中,化合物 10 表现出最大的抗氧化作用,大于用作阳性对照的槲皮素。结果表明,构树木材可能具有治疗炎症性疾病和氧化应激的有益作用和利用价值。