螃蟹甲内生真菌Chaetosphaeronema sp.的化学成分研究

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。

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

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.