一株半夏内生青霉属真菌次级代谢产物及生物活性的研究

The Secondary Metabolites Isolated from One Endophytic Fungi of Pinellia Ternate and Biological Activity

目的：对半夏中分离的一株内生真菌BX－9（青霉属）次级代谢产物进行分离鉴定及生物活性研究。方法：将一株半夏内生真菌（ BX－9）用PDB培养基进行发酵培养，菌丝体用甲醇回流提取2次，菌液用乙酸乙酯萃取两次，通过各种柱色谱分离得到次级代谢化合物。采用MTT法和改良的Ellman法测定化合物抗肿瘤和抗乙酰胆碱酯酶活性。结果：分离得到7个化合物，分别为2－Hydroxy－14－tricosenvic acid（1）、4，6，8，22－tetraen－3－one－ergostane（2）、Ergosterol（3）、Ergosterol peroxide（4）、（＋）－Brefeldin A （5）、7－oxobrefeldin A （6）、4－epi－Brefeldin A （7）。化合物3～6对Hela、7721、HL60三株肿瘤细胞均有显著活性。这7个化合物均无乙酰胆碱酯酶抑制活性。结论：从半夏内生菌BX－9中能分离出具有抗肿瘤活性的次生代谢产物，其中Brefeldin A含量较高。

Objective：To isolate the secondary metabolites from the fermentation broth and mycelium of an endophytic fun-gi BX-9 （ Penicillium sp.） isolated from Pinellia ternate （ Thunb.） and detect the biological activity of these secondary metabolites.Methods：The strain BX-9 was fermented in PDB culture,and fermentation broth was extracted by ethyl acetate,and the mycelia of endophytic were extracted in methanol for two times.The chemical constituents of the strain BX-9 were isolated by variety of chromatographyic methods.The AChE inhibitory and antitumor activity was deter-mined by modified Ellman’ s method and MTT method.Results：Seven compounds were isolated from the fermentation broth and mycelium of endophytic fungi from Pinellia ternate and they were identified as 2-Hydroxy-14-tricosenvic acid （1）, [4, 6, 8, 22-tetraen-3-one-ergostane] （2）,Ergosterol （3）,Ergosterol peroxide （4）,（ ＋） -Brefel-din A （5）, 7-oxobrefeldin A （6）, 4-epi-Brefeldin A （7）.All of the compounds had no AChE inhibitory activity. Compounds （3~6） had a remarkably antitumor activity against Hela,7721, HL60.Conclusion：It is possible to isolate antitumor compounds from endophytic fungi of Pinellia ternate and the strain BX-9 can produce large numbers of brefel-din A.