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  

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

作　　者：张敏[1] 方玉春[1] 朱天骄[1] 赵文英[1] 顾谦群[1] 韩小贤[1] 朱伟明[1] 

机构地区：[1]海洋药物教育部重点实验室中国海洋大学医药学院,山东青岛266003

出　　处：《中国药学杂志》2007年第24期1848-1851,共4页Chinese Pharmaceutical Journal

基　　金：国家863计划(2003AA624020)

摘　　要：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。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 tsFF210,A549 ,BEL-7402,HL60 and P388 cells with the IC50 values in the range of 1×10^-5-1×10^-4mol·L^-1. CONCLUSION All these compounds were obtained from this fungus for the first time.

关 键 词：海洋来源真菌 萨氏曲霉 吲哚-喹唑啉生物碱 抗肿瘤活性 

分 类 号：R284.1[医药卫生—中药学]