Triterpenoid saponins and flavonoids from licorice residues with anti-inflammatory activity
Triterpenoid saponins and flavonoids from licorice residues with anti-inflammatory activity
复制标题
DOI：
10.1016/j.indcrop.2018.08.075
复制
发表时间：
2018-12-01
影响因子：
5.9
通讯作者：
Song, Shao-Jiang
中科院分区：
文献类型：
--
作者：
Bai, Ming;Yao, Guo-Bong;Song, Shao-Jiang
光果甘草的工业化加工导致相当数量的残留物通常被随意丢弃或由垃圾填埋场处理。因此，本研究的目的是开发甘草残渣作为生物活性化合物的来源，具有潜在的应用前景。从甘草残渣中分离得到4个新的三萜皂苷(1-3，12)和10个已知皂苷(4-11，13-14)和5个黄酮类化合物(15-19)。通过全面的波谱分析确定了它们的结构。分离得到的化合物对脂多糖诱导的RAW 264.7细胞产生一氧化氮(NO)有明显的抑制作用。结果表明，化合物18的NO抑制作用最强(IC50为9.89 mU M)，而阳性对照药物米诺环素的IC50为33.20 mU M。进一步研究表明，化合物18可显著下调促炎细胞因子IL-1β和IL-6以及诱导酶诱导型一氧化氮合酶(INOS)和环氧合酶-2(COX-2)的水平。此外，Western blotting分析表明，化合物18可能通过下调自噬水平而减轻炎症效应。总体而言，这项研究表明，甘草残留物是一种很有前途的废物，也是制药业生物活性化合物的宝贵来源。
Industrial processing of licorice (Glycyrrhiza glabra L.) leads to a considerable quantity of residues which are normally discarded randomly or treated by landfill. Therefore, the aim of this study was to develop licorice residues as a source of bioactive compounds with potentially applications. Chemical investigation of licorice residues led to the isolation of four new triterpenoid saponins (1-3, 12), along with ten known saponins (4-11, 13-14) and five flavonoids (15-19). The structures were established by comprehensive spectroscopic analyses. All the isolated compounds were tested for their inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW 264.7 cells. Among the results, compound 18 displayed the most potent NO inhibitory effect (IC50 9.89 mu M) compared with the positive control drug minocycline (IC50 33.20 mu M). Further studies showed that the levels of pro-inflammatory cytokines interleukin (IL)-1 beta and interleukin (IL)-6 and inducible enzymes inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) were markedly down regulated by compound 18. In addition, the Western blotting assay showed that compound 18 might reduce the inflammatory effect by down-regulating autophagy level. Overall, this study suggest that licorice residues are a promising waste and a valuable source of bioactive compounds for the pharmaceutical industry.