海洋来源真菌Aspergillus sydowi PFW-13中的吲哚-喹唑啉类生物碱及其抗肿瘤活性

 目的研究海洋来源真菌萨氏曲霉(Aspergillus sydowi)PFW-13发酵产物中的抗肿瘤活性次级代谢产物。方法采用活性追踪的方法、利用色谱手段分离获得单体化合物,根据波谱分析及其理化性质确定其结构,利用SRB法评价单体化合物的细胞毒活性。结果获得6个吲哚-喹唑啉类生物碱,其结构分别鉴定为fumiquinazolines A(1)、fumiquinazolines C(2)、fu-miquinazolines D(3)、fumiquinazolines F(4)、fumiquinazolines G(5)、fumiquinazolines J(6),其中化合物6为新天然产物。化合物2和6对肿瘤细胞tsFT210、A549、BEL-7402、HL60和P388的半数抑制浓度(IC₅₀)在1×10^-5～1×10^-4mol·L^-1之间。结论以上化合物均为首次从该种真菌中分离得到。

Study on Indole-Quinazolines Alkaloids from Marine-Derived Fungus Aspergillus sydowi PFW-13 and their Anti-Tumor Activities

OBJECTIVE To investigate the cytotoxic secondary metabolites of marine-derived fungus Aspergillus sydowi PFW-13.METHODS Active compounds were isolated with bioassay-guided separation procedure and their structures were identified by means of spectral analysis and physicochemical properties.Their anti-tumor activities were preliminarily evaluated in vitro by the SRB method.RESULTS Six quinazoline alkaloids including a new natural product(6) were isolated and their structures were identified as fumiquinazolines A(1),fumiquinazolines C(2),fumiquinazolines D(3),fumiquinazolines F(4),fumiquinazolines G(5),fumiquinazolines J(6),respectively.Compound 2 and 6 showed cytotoxicity against tsFT210,A549,BEL-7402,HL60 and P388 cells with the IC₅₀ values in the range of 1×10^-5～1×10^-4 mol·L^-1.CONCLUSION All these compounds were obtained from this fungus for the first time.