盐碱地真菌棘孢曲霉Aspergillus aculeatus的化学成分研究△﹡

目的 对一株具有抗肿瘤活性的滨州盐碱地真菌棘孢曲霉Aspergillus aculeatus的活性次级代谢产物进行研究。方法 采用硅胶柱层析、LH-20凝胶色谱和半制备高效液相色谱分离纯化代谢产物,通过理化性质、波谱手段结合X-ray单晶衍射技术鉴定化合物,采用MTT法测试所得化合物对肿瘤细胞A549的增殖抑制活性。结果 从棘孢曲霉Aspergillus aculeatus中分离得到8个化合物(1～8),分别鉴定为5-Hydroxymethyl-2-furoic acid (1)、Isorhodoptilometrin (2)、Secalonic acid F (3)、Emodin (4)、Protocatechuic acid (5)、Altechromones B (6)、Cyclo (L-Tyr-L-Leu) (7)和Cyclo (L-Phe-L-Ala) (8)。化合物3对A549细胞具有一定的增殖抑制活性,其IC50值为14.9 μM。结论 首次研究了来源于盐碱地真菌棘孢曲霉Aspergillus aculeatus的活性次级代谢产物,并首次报道secalonic acid F对A549肿瘤细胞增殖抑制活性。

Studies on secondary metabolites of Aspergillus aculeatus derived from coastal saline soil

Objective Study on the secondary metabolites of one fungus named Aspergillus aculeatus derived from coastal saline soil with antitumor activity. Methods The extract of this fungus was purified by repeated column chromatography on silica gel, sephadex LH-20 and semi-prepartive high performance liquid chromatography (HPLC). The structures of the compounds were determined by their physicochemical and spectroscopic data couple with X-ray diffraction. Antitumor activities were tested by MTT methods. Result Eight compounds were isolated and their structures were elucidated as 5-Hydroxymethyl-2-furoic acid (1), Isorhodoptilometrin (2), Secalonic acid F (3), Emodin (4), Protocatechuic acid (5), Altechromones B (6), Cyclo (L-Tyr-L-Leu) (7) and Cyclo (L-Phe-L-Ala) (8). Compound 3 showed middle cytotoxic activity, and the others showed weak cytotoxic activities. Conclusion This was the first report of isolation of Aspergillus aculeatus derived from coastal saline soil. The inhibitory effect of SAF on A549 cell line was also assayed for the first time.