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采用紫外跟踪分离和波谱鉴定的方法,从海洋异壁放线菌(Actinoalloteichus cyanogriseus WH1-2216-6)的发酵产物中分离鉴定了6个5,5,6-多环含特特拉姆酸大环内酰胺(PTMs)类天然产物:16-hydroxymaltophilin(1)、dihydromaltophilin(2)、4-deoxydihydromaltophilin(3)、maltophilin(4)、xanthobaccin C(5)和FI-2(6),其中1为新化合物.评价了化合物1~5对人正常肝细胞L-02及人癌细胞A549、MCF-7、Jurkat、BXPC-3、HCT-116、PANC-1和K562的细胞毒活性,结果表明:化合物1~5对上述人癌细胞具有细胞毒活性,其半数抑制浓度(IC50)为0.1~9.7μmol·L-1;新化合物1对L-02的毒性较低,但对Jurkat、HCT-116和BXPC-3的选择指数(SI)分别高达31.5、41.1和52.4.除化合物2和3对A549和MCF-7的肿瘤细胞毒活性外,其余的肿瘤细胞毒活性是首次报道.还测试了化合物1~6的抗烟曲霉活性,发现化合物2和4的活性较好,其最小抑菌浓度(MIC)分别为3.04和6.12μmol·L-1,这是首次发现5,5,6-PTMs类化合物具有抗烟曲霉活性.
Using ultraviolet tracing and spectral analysis, six 5,5,6-polycyclic tetracarboxylic acids were isolated and identified from the fermentation products of Actinoalloteichus cyanogriseus WH1-2216-6 Natural products of cyclic lactam (PTMs): 16-hydroxymaltophilin (1), dihydromaltophilin (2), 4-deoxydihydromaltophilin (3), maltophilin (4), xanthobaccin C (5) and FI-2 New compounds. The cytotoxic activities of compounds 1 to 5 against human normal hepatocytes L-02 and human cancer cells A549, MCF-7, Jurkat, BXPC-3, HCT-116, PANC-1 and K562 were evaluated. Compounds 1 to 5 showed cytotoxic activity against human cancer cells above, and their IC50 values ranged from 0.1 to 9.7 μmol·L-1. The toxicity of compound 1 to L-02 was lower than that of Jurkat, HCT-116 And SI (Selective index) of BXPC-3 were as high as 31.5, 41.1 and 52.4, respectively.Other than the cytotoxic activity of compounds 2 and 3 on A549 and MCF-7 tumor cells, the cytotoxic activity of the remaining tumor cells was first reported.Compounds 1 to 6 against Aspergillus fumigatus activity. Compounds 2 and 4 were found to be more active with minimal inhibitory concentrations (MICs) of 3.04 and 6.12 μmol·L-1, respectively 5,5,6-PTMs compounds having activity against Aspergillus smoke.