中文摘要：

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.

英文摘要：

From the fermentation broth of the marine-derived Actinoalloteichus cyanogriseus WH1-2216-6, a new 5,5,6-polycyclic tetramate macrolactam（PTM） named 16-hydroxymaltophilin（1） was isolated and identified along with five known analouges, dihydromaltophilin（2）, 4-deoxydihydromaltophilin（3）, maltophilin（4）, xanthobaccin C（5） and FI-2（6）, by means of UV-guided isolation as well as the spectroscopic identification. The cytotoxicities of compounds 1-5 were tested against the human normal hepatic cell line（L-02） and the seven human cancer cell lines, A549, MCF-7, Jurkat, BXPC-3, HCT-116, PANC-1 and K562. The results showed that compounds 1-5 were active against the above human cancer cell lines with the IC50 values of 0.1-9.7 μmol·L-1, among which the new compound 1 was the lowest toxic to L-02 cell and the most selective to Jurkat, HCT-116 and BXPC-3 cells with the selection index（SI） of 31.5, 41.4 and 52.4, respectively. The antifungal activities of 1-6 against Aspergillus fumigatus AF293 were also tested by two-fold dilution method. Compounds 2 and 4were active against A. fumigatus AF293 with the minimum inhibitory concentration（MIC） values of 3.04 and 6.12 μmol·L-1, respectively. To the best of our knowledge, this is the first time to report the antifungal activity of 5,5,6-PTMs against A. fumigatus AF293. Apart from the cytotoxicity of compounds 2 and 3 against A549 and MCF-7 tumor cells lines, the other cytotoxicities were reported here for the first time, indicating the potential use of PTMs as the antitumor and antifungal lead compounds against A. fumigatus.