辐肛参中4个抗真菌活性海参皂苷
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国家高技术研究发展计划(“863”计划, 2006AA09Z417).


Antifungal activities of four triterpene glycosides derived from sea cucumber Actinopyga sp.
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Supported by National High-tech R&D Program(“863” Program, 2006AA09Z417).

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    摘要:

    目的 研究辐肛参 (Actinopyga sp.) 中三萜皂苷的抗真菌活性。方法 利用大孔树脂柱层析、正相硅胶柱层析、反相硅胶柱层析、Sephadex LH-20以及HPLC等层析手段,对一种辐肛参的皂苷类成分进行分离,应用波谱技术和化学方法,并结合文献对照,对所得的化合物进行结构鉴定。采用微量液基稀释法对提取分离的化合物进行抗真菌(白念株菌、新生隐球菌、熏烟曲霉菌) 活性测试。结果 从该种海参中分离得到4个海参烷型三萜皂苷类化合物,其结构分别鉴定为frondoside A (1)、pervicoside C (2)、holothurin A (3)和holothurin B (4)。化合物1抗真菌活性弱,化合物2对3种真菌的MIC80为1~4 mg/L,有较强的抗真菌活性。结论 化合物1和2均系首次从辐肛参Actinopyga sp.中获得,4个三萜皂苷都具有抗真菌活性,其中pervicoside C 可作为抗真菌药物的先导化合物。

    Abstract:

    Objective To study the antifungal activities of triterpene glycosides derived from the sea cucumber Actinopyga sp. Methods Triterpene glycosides were isolated and purified by silica gel chromatography, reversed-phase silica gel chromatography, Sephadex LH-20, and RP-HPLC from Actinopyga sp. The structures of the triterpene glycosides were elucidated based on spectral data, chemical reactions, and related references. The antifungal activities of the extracts against three strains:Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus were assessed by liquid microdilution method. Results Four triterpene glycosides were identified from Actinopyga sp.; and they included frondoside A (1),pervicoside C (2), holothurin A (3), and holothurin B (4). The MIC80 of compound 2 and compound 3 for antifungal effect were 1-4 mg/L, showing marked antifungal activities.Conclusion Compounds 1 and 2 have been isolated from this halobios for the first time. All the four compounds show considerable antifungal activities, and pervicoside C may be used as a lead compound of antifungal agents.

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  • 收稿日期:2009-10-13
  • 最后修改日期:2010-04-05
  • 录用日期:2010-04-07
  • 在线发布日期: 2010-05-21
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