螃蟹甲内生真菌Chaetosphaeronema sp.的化学成分研究

Chemical constituents of an endophytic fungus Chaetosphaeronema sp. from Phlomis younghusbandii Mukerjee

目的研究一株来源于藏药螃蟹甲内生真菌PHY-24的化学成分。方法采用麦麸培养基,对内生真菌PHY-24进行放大培养,通过硅胶柱色谱、MCI柱色谱、ODS柱色谱、Sephadex LH-20柱色谱、高效液相色谱等对其发酵液中的化学成分进行分离纯化,利用NMR、MS等波谱方法进行化学成分的结构鉴定,并测定这些成分抗HIV-1整合酶链转移反应活性。结果从内生真菌PHY-24发酵液的乙酸乙酯提取部分分离并鉴定了4个化合物,分别是:integrastatin B(1)、2-乙酰基-3,5-二羟基-苯乙酸(2)、curvulin(3)、O-methylcurvulinic acid(4)。其中化合物(1)和(2)具有抗HIV-1整合酶链转移反应活性,其IC50分别为6.22和75.1μmol/L。结论 4个化合物均为从此属真菌中首次分得,其中化合物(1)、(2)具有抗HIV-1整合酶链转移反应活性。化合物(2)的活性为首次报道。

Objective To study the chemical constituents of an endophytic fungus PHY-24 （Chaetosphaeronema sp.） from Tibetan medicinal plants Phlomis younghusbandii Mukerjee. Methods PHY-24 culture was scaled-up using wheat bran medium. The chemical constituents from the fermentation broth of the strain PHY-24 were isolated and purified by silica gel, MCI, ODS and Sephadex LH-20 column chromatography, and their chemical structures were identified by analysis of MS and NMR. Bioactivities of the constituents were tested with anti-HIV-1 integrase strand transfer reaction. Results Four compounds were separated and identified from the fermentation broth, including integrastatin B, curvulin acid, curvulin, O-methylcurvulinic acid. Integrastatin B and curvulin acid have anti-HIV-1 activity with IC50 being 6.22 μmol/L and 75.1μmol/L, respectively. Conclusion The four compounds were firstly obtained from the Chaetosphaeronema genus, with integrastatin B and curvulin acid having anti-HIV-1 integrase strand transfer reaction activity. The activity of curvulin acid was firstly reported.