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Biologically active triterpene saponins from the root of the medicinal plant Polygala senega L.

机译:药用植物远志(Polygala senega L)的根中具有生物活性的三萜皂苷。

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摘要

Polygala senega L., known as senega root, is an indigenous plant to the Canadian prairies traditionally used as an expectorant.; In this work, the isolation of pure saponin compounds from crude saponin extracts and their biological evaluation are reported. Using reverse-phase low-pressure liquid column chromatography and semi-preparative HPLC, eight saponin compounds were isolated and their structure partially elucidated primarily by LC-MS, FAB-MS and NMR techniques. All were found to be triterpenoid saponins with a common aglycone, presenegenin, to which sugar moieties are attached via ether and ester bonds at positions C-3 and C-28, respectively. The HPLC analysis, which indicated a baseline separation between the eight saponins, and spectroscopic data for the isolated saponin compounds, PS 1 (m/z = 1847), PS 2 (m/z = 1601), PS 3 (m/z = 1703), PS 4 (m/z = 1455), PS 5 (m/z = 1571), PS 6 (m/z = 1557), PS 7 (m/z = 1425) and PS 8 (m/z = 1587), are presented.; Evaluation of immunological activities of isolated saponins revealed that there was a preferential increase of the IgG2a subclass, and upon in vitro secondary antigen stimulation, high IL-2 and IFN-gamma levels were observed in spleen cell cultures from Polygala senega saponins-immunized animals. The saponins were tested for their toxicity by lethality in mice and were found to be less toxic at the same dose than their counterpart Quil A. This study has shown the potential of these compounds to be considered as natural sources of vaccine adjuvants, since their biological activity was comparable to Quillaja saponaria saponins that have long been used as adjuvants in vaccine formulations.; Cytotoxic activity against human breast cancer cell line, MDA-MB231, and colon cancer cell line, WiDr, was also detected, although these are only preliminary findings.
机译:Polygala senega L.,被称为senega根,是加拿大大草原上的土生植物,传统上用作祛痰剂。在这项工作中,报道了从粗皂苷提取物中分离出纯皂苷化合物及其生物学评价。使用反相低压液相色谱和半制备型HPLC,分离了8种皂苷化合物,主要通过LC-MS,FAB-MS和NMR技术部分阐明了它们的结构。发现所有这些都是三萜类皂苷,具有常见的糖苷配基皂苷元,其糖部分分别通过C-3和C-28位的醚键和酯键连接。 HPLC分析表明,这8种皂苷之间存在基线分离,分离出的皂苷化合物PS 1(m / z = 1847),PS 2(m / z = 1601),PS 3(m / z = 1703),PS 4(m / z = 1455),PS 5(m / z = 1571),PS 6(m / z = 1557),PS 7(m / z = 1425)和PS 8(m / z = (1587)。对分离的皂苷的免疫活性的评估表明,IgG2a亚类有优先增加,并且在体外次级抗原刺激下,在以参芪皂苷免疫的动物的脾细胞培养物中观察到高的IL-2和IFN-γ水平。通过在小鼠中的致死性测试了皂苷的毒性,发现在相同剂量下其皂苷的毒性低于其对应的QuilA。这项研究表明,这些化合物具有被视为疫苗佐剂的天然来源的潜力,因为它们具有生物学上的意义活性与早已被用作疫苗制剂佐剂的Quillaja saponaria皂苷相当。尽管仅是初步发现,但也检测到了针对人乳腺癌细胞MDA-MB231和结肠癌细胞WiDr的细胞毒活性。

著录项

  • 作者

    Katselis, Georgios Simeon.;

  • 作者单位

    The University of Saskatchewan (Canada).;

  • 授予单位 The University of Saskatchewan (Canada).;
  • 学科 Health Sciences Pharmacology.
  • 学位 Ph.D.
  • 年度 2006
  • 页码 275 p.
  • 总页数 275
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药理学;
  • 关键词

  • 入库时间 2022-08-17 11:40:48

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