曼陀罗内生真菌Fusarium solani MBM-5活性次级代谢产物研究

Active secondary metabolites from an endophytic fungus Fusarium solani MBM-5 of Datura arborea

该文对木本曼陀罗内生真菌Fusarium solani MBM-5(茄腐皮镰刀菌)的次级代谢产物进行了化学及生物活性研究。运用多种色谱方法(如开放ODS柱色谱、硅胶柱色谱、Sephadex LH-20凝胶柱色谱及半制备型HPLC等),从F.solani MBM-5培养物的乙酸乙酯萃取物中共分离得到6个烯酸类化合物,包括1个新化合物和5个已知化合物。利用化合物的理化常数和波谱学(UV、IR、NMR、HR-ESI-MS等)方法及Mosher′s反应,鉴定了化合物结构,分别为fusaridioic acid E (1)、fusaridioic acid C (2)、fusaridioic acid A (3)、L660282 (4)、hymeglusin (5)、hymeglnone (6),其中化合物1为新化合物。采用MTT法和Griss法,分别评价了所有化合物对2种肿瘤细胞的生长抑制作用,以及对脂多糖(LPS)诱导巨噬细胞RAW264.7释放NO的影响及其抗炎作用。实验结果表明,化合物5对A549和HepG2细胞株具有较强的生长抑制活性(IC_(50)分别为4.70、13.57μmol·L^(-1)),并且化合物1和6可显著抑制LPS诱导RAW264.7细胞的NO释放量,其IC_(50)分别为77.00、70.33μmol·L^(-1)。

This study investigated the chemical and biological activity of the secondary metabolites from an endophytic fungus Fusa-rium solani MBM-5 of Datura arborea.A total of six alkenoic acid compounds,including a new compound and five known ones,were isolated from the ethyl acetate extract of F.solani MBM-5 by using the chromatographic methods(open ODS column chromatography,silica gel column chromatography,Sephadex LH-20,and semi-preparative HPLC).The structures of the compounds were identified by using their physical and chemical data,spectroscopic methods(UV,IR,NMR,and HR-ESI-MS),and Mosher′s reaction,which were fusaridioic acid E(1),fusaridioic acid C(2),fusaridioic acid A(3),L660282(4),hymeglusin(5),and hymeglnone(6).Compound 1 is new.MTT assay and Griss method were used to evaluate the growth inhibition of all the compounds against two tumor cells,as well as their influence and anti-inflammatory action on the release of NO from LPS-induced RAW264.7 cells.The results showed that compound 5 had strong growth inhibition activity against A549 and HepG2 cell lines,with IC_(50) values of 4.70 and 13.57 μmol·L~(-1),respectively.Compounds 1 and 6 significantly inhibited the release of NO from LPS-induced RAW264.7 cells,with IC_(50) values of 77.00 and 70.33 μmol·L~(-1),respectively.