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。
Abstract
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.
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
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Key words
marine-derived fungal /
Aspergillus sydowi /
indole-quinazolines alkaloid /
cytotoxicity
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张敏;方玉春;朱天骄;赵文英;顾谦群;韩小贤;朱伟明.
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[J]. 中国药学杂志, 2007, 42(24): 1848-1851
ZHNG Min;FNG Yu-chun;ZHU Tin-jio;ZHO Wen-ying;GU Qin-qun;HN Xio-xin;ZHU Wei-ming.
Study on Indole-Quinazolines Alkaloids from Marine-Derived Fungus Aspergillus sydowi PFW-13 and their Anti-Tumor Activities [J]. Chinese Pharmaceutical Journal, 2007, 42(24): 1848-1851
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参考文献
[1] MIAO L，ZHENG Z H，SU W J.Research development of bioactive substance of symbiotic and epibiotic marine microorganisms [J] .Marine Sci Bull(海洋通报)，2002，21 (3)：62-66.
[2] IM S B，CHRIS M I.Marine-derived fungi：a chemically and biologically diverse group of microorganisms [J] .Nat Prod Rep，2004，21 (1)：143-163.
[3] VIGUSHIN D M，MIRSAIDI N，BROOKE G，et al.Gliotoxin is a dual inhibitor of farnesyltransferase and geranylgeranyltransferase I with ant-tumor activity against breast cancer in vivo[J] .Med Oncol，2004，21 (1)：21-30.
[4] TAKAHASHI C，MATSUSHITA T，DOI M，et al. Fumiquinazolines A～G，novel metabolites of a fungus separated from a Pseudolabrus marine fish [J] .J Chem Soc Perkin Trans I，1995，18：2345-2352.
[5] BELOFSKY G N，ANGUERA M，JENSEN P R，et al. Oxepinamides A～C and fumiquinazolines H～I：bioactive metabolites from a marine isolate of a fungus of the genus Acremonium[J] . Chemistry A European J，2000，6 (8)：1355-1360.
[6] SKEHAN P，STORENG R，SCUDIERO D，et al.New colorimetric cytotoxicity assay for anticancer drug screening[J] .J Natl Cancer Inst，1990，82 (13)：1107-1113.
[7] HEREDIA M L，CUESTA D E，AVENDANO C.Acid-promoted reactions in 1-hydroxy- 1-dimethylaminomethyl and 1-methylene-4-arylmethyl-2，4-dihydro-1H-pyrazino [2，1-b] - quinazoline-3，6-diones[J] .Tetrahedron，2002，58 (31)：6163-6170.
[8] DAVID J H，NABI A M.Synthesis of ent-alantrypinone[J] .J Am Chem Soc，2001，123 (25)：5892-5899.
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脚注
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基金
国家863计划(2003AA624020)
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