辐肛参中4个抗真菌活性海参皂苷

Antifungal activities of four triterpene glycosides derived from sea cucumber Actinopyga sp.

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frondo-side 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1～4mg/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。

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.