海洋异壁放线菌WH1-2216-6产生的多环含特特拉姆酸大环内酰胺

发布时间：2018-01-14 18:02

  本文关键词：海洋异壁放线菌WH1-2216-6产生的多环含特特拉姆酸大环内酰胺　出处：《有机化学》2017年09期 　论文类型：期刊论文

  更多相关文章： 异壁放线菌 -多环含特特拉姆酸大环内酰胺 抗肿瘤活性 抗烟曲霉活性

【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.
[Abstract]:UV tracing separation and spectral identification were used. From the fermentation products of Actinoalloteichus cyanogriseus WH1-2216-6, six 5G 5 were isolated and identified from the fermentation products of Actinoalloteichus cyanogriseus WH1-2216-6. 6-polycyclic macrocyclic lactam (PTMs1) is a natural product of the class: 16-hydroxymaltophilin1). Dihydromaltophilin2) 4-deoxydihydromaltophilin3 (maltophilin4). Xanthobaccin Cn5) and FI-2O6, of which 1 is a new compound. The effects of compound 1 on human normal hepatocytes L-02 and human cancer cell A549 were evaluated. Cytotoxic activities of MCF-7 Jurkatine BXPC-3 HCT-116HPANC-1 and K562. The results showed that compound 1t5 had cytotoxic activity to the above mentioned human cancer cells, and its IC50 was 0.1 渭 mol 路L -1; The toxicity of new compound 1 to L-02 was low, but the selection index of HCT-116 and BXPC-3 was as high as 31.5 for Jurkatine HCT-116 and BXPC-3, respectively. 41.1 and 52.4. Except for the cytotoxic activity of compounds 2 and 3 to A549 and MCF-7. The cytotoxic activity of other tumor cells was reported for the first time. The activity of compound 1 / 6 against Aspergillus fumigatus was also tested, and it was found that compounds 2 and 4 had better activity. The minimum inhibitory concentration (MIC) was 3.04 渭 mol 路L-1 and 6.12 渭 mol 路L-1, respectively.
【作者单位】： 中国海洋大学医药学院海洋药物教育部重点实验室;贵州医科大学药物植物功效与利用国家重点实验室;
【基金】：国家自然科学基金(Nos.81561148012,41376148);国家自然科学基金-广东联合基金(No.U1501221)资助项目~~
【分类号】：R915
【正文快照】： 含氮化合物是药物的主要形式,也是海洋微生物天然产物的主要结构类型[1].多环含特特拉姆酸大环内酰 胺类似物(Polycyclic tetramate macrolactams,PTMs)是一类来自微生物或海绵的、具有良好生物活性的天然产物.顾名思义,PTMs类化合物含有一个特特拉姆酸结构单元、一个稠合的，

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