海南红树林内生真菌Fusarium sp.HSL-3次级代谢产物研究

Study on Secondary Metabolites of Endophytic Fungus Fusarium sp.HSL-3 from Hainan Mangrove

目的研究海南红树林内生真菌Fusarium sp.HSL-3次级代谢产物,并对其进行抗炎和抗肿瘤活性筛选。方法采用大米培养基对菌株静置培养,同时采用柱层析色谱法和HPLC对该真菌的次级代谢产物进行分离纯化,并且通过核磁共振及质谱等有机波谱手段,对得到的化合物进行结构鉴定。结果共分离得到8个化合物,分别为lateritin(1)、4-carbomethoxy-6-hydroxy-2-quinolone(2)、3,5-dimethoxydihydrofusarubin D(3)、anhydrofusarbin(4)、3,3’-methylene-bis(4-hydroxybenzaldehyde)(5)、crypticin B(6)、vanillyl alcohol(7)和3,4-dihydroxyphenylaceticacid(8),其中化合物2和5为首次从镰刀菌属Fusarium中分离得到。化合物3和5对RAW264.7细胞表现出良好的抗炎活性(化合物3在50μmol·L^(–1)时的NO抑制率为87%,化合物5在50μmol·L^(–1)时的NO抑制率为71%),而化合物1对非小细胞肺癌细胞A549有显著的细胞毒活性,IC50值为(7.92±0.27)μmol·L^(–1)。结论从海南红树林内生真菌Fusarium sp.HSL-3中分离得到的化合物3和5具有较强的抗炎活性,化合物1有显著的抗肿瘤活性。

OBJECTIVE To study the secondary metabolites of the endophytic fungus Fusarium sp.HSL-3 isolated from Hainan Mangrove and screen their anti-inflammatory and anti-tumor activities.METHODS This fungus was fermented statically by using rice medium,and the secondary metabolites of the fungus were isolated and purified by column chromatography and HPLC.Structures indentification of the ortained compounds was carried out through MS and NMR.RESULTS Eight compounds were respectively isolated and identified as follows:lateritin(1),4-carbomethoxy-6-hydroxy-2-quinolone(2),3,5-dimethoxydihydro-fusarubin D(3),anhydrofusarbin(4),3,3’-methylene-bis(4-hydroxybenzaldehyde)(5),crypticin B(6),vanillyl alcohol(7)and 3,4-dihydroxyphenylaceticacid(8),among which,compounds 2 and 5 were isolated from the genus Fusarium for the first time.Compounds 3 and 5 showed good anti-inflammatory activity on RAW264.7 cells with the inhibition rate of NO at 50µmol·L^(–1) were 87%for compound 3 and 71%for compound 5,while compound 1 showed significant cytotoxic activity against human non-small cell lung cancer cell line A549,among which the IC50 value was(7.92±0.27)µmol·L^(–1).CONCLUSION Compounds 3 and 5 isolated from endophytic fungus Fusarium sp.HSL-3 isolated from Hainan Mangrove show strong anti-inflammatory activity,while compound 1 shows significant anti-tumor activity.