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[摘要]
目的 研究蛇足石杉内生真菌Penicillium chrysogenum MT-12经固体发酵培养后的代谢产物。方法 利用硅胶、Sephadex LH-20及半制备液相色谱等方法进行分离纯化,根据化合物的理化性质及IR、MS、NMR等光谱数据鉴定化合物的结构;利用体外模型进行抗炎、乙酰胆碱酯酶抑制活性筛选。结果 从P.chrysogenum MT-12固体发酵培养后的代谢产物中共分离鉴定8个二苯醚类化合物,分别为黄青霉内酯A (1)、黄青霉内酯B (2)、talaromyone A (3)、isopenicillide (4)、penicillide (5)、hydroxypenicillide (6)、purpactin A (7)、黄青霉内酯C (8)。结论 化合物1、2为新化合物,化合物3为首次从青霉属中分离得到,化合物4~8为首次从产黄青霉菌中分离得到;化合物1、2对脂多糖(LPS)诱导的小鼠巨噬细胞RAW264.7的NO产生有一定抑制活性,半数抑制浓度(IC50)值分别为(72.6±2.3)、(41.2±1.4)μmol/L,而所有化合物在100 μmol/L时对乙酰胆碱酯酶不显示抑制活性。
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[Abstract]
Objective To investigate the chemical constituents from Penicillium chrysogenum MT-12, an endophytic fungus isolated from Huperzia serrata.Methods The compounds were isolated and purified by using various column chromatographies including silica gel, Sephadex LH-20, and semi-preparative HPLC. The structures were established using extensive spectroscopic techniques such as IR, MS, and NMR. The anti-inflammatory and AChE inhibitory activities of all the isolates were also preliminarily investigated by using in vitro models.Results Eight diphenyl ether derivatives including penicichrysogenillide A (1), penicichrysogenillide B (2), talaromyone A (3), isopenicillide (4), penicillide (5), hydroxypenicillide (6), purpactin A (7), and penicichrysogenillide C (8) were isolated from the solid fermentation cultures of P.chrysogenum MT-12.Conclusion Compounds 1 and 2 are new compounds, and this is the first report for the isolation of compound 3 from Penicillium species and compounds 4-8 from P. chrysogenum. Compounds 1 and 2 exhibited inhibitory activities anginst the nitric oxide production in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells with IC50 value of (72.6 ±2.3) μmol/L and (41.2 ±1.4) μmol/L, respectively. In contrast, all the compounds didn't exhibit inhibitory activities on AChE at the concentration of 100 μmol/L.
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[基金项目]
国家自然科学基金资助项目(81573312)