Alkaloids from the endophytic fungus Penicillium brefeldianum and their cytotoxic activities

One new indoloditerpene,6,7-dehydropaxilline（1）,one new indole-diketopiperazine,spirotryprostatin F（2）,and one new 13-membered macrolide,N-demethylmelearoride A（3）,as well as 8 known alkaloids（4-11）,were isolated from the solid cultures of the endophytic fungus,Penicillium brefeidianum.The structures and absolute configurations of compounds 1-3 were elucidated by comprehensive spectroscopic analysis and the circular dichroism（CD） exciton chirality method.All the metablites were evaluated for their cytotoxic activites against three human tumor cell lines.Compound 2 exhibited cytotoxicities against HepG2 and MDA-MB-231 cells with IC（50） values of 14.1 μmol/L and 35.5μmol/L,respectively.Compound 3 showed moderate activity against HepG2 cells with IC（50） values of 36.6 μmol/L.

两种海洋真菌混合发酵的次级代谢产物及杀虫活性研究

为了研究海洋真菌哈茨木霉Trichoderma harzianum ABC19819和短柄青霉菌Penicillium Brefeldianum ABC190807混合发酵产生的次级代谢产物,利用硅胶柱色谱、Sephadex LH-20凝胶柱色谱和薄层色谱等多种分离纯化手段对混合发酵所产生的次级代谢产物进行分离纯化,结合波谱分析技术(1H NMR、13C NMR、ESI-MS)及文献对比鉴定了化合物的结构。以埃及伊蚊Aedes aegypti 3龄幼虫为研究对象,对分离鉴定得到的化合物进行活性评价。结果表明,从2株真菌混合培养的发酵产物中分离得到6个已知化合物,分别鉴定为agathic acid(1)、4-羟基苯甲醛(2)、nafuredin(3)、4-羟基-3,6-二甲基-2H-吡喃酮(4)、甲瓦龙酸内酯(5)和brefeldin A(6),其中化合物1为首次由哈茨木霉与短柄青霉菌的混合发酵物中分离得到。化合物1和3对埃及伊蚊3龄幼虫表现出明显的毒杀活性,处理72 h后的LC50值分别为162 mg/L和240 mg/L。该研究对于通过混合发酵得到具有杀虫活性的化合物具有重要参考价值。