本文關(guān)鍵詞：海洋異壁放線菌WH1-2216-6產(chǎn)生的多環(huán)含特特拉姆酸大環(huán)內(nèi)酰胺　出處：《有機化學》2017年09期 　論文類型：期刊論文

  更多相關(guān)文章： 異壁放線菌 -多環(huán)含特特拉姆酸大環(huán)內(nèi)酰胺 抗腫瘤活性 抗煙曲霉活性

【摘要】：采用紫外跟蹤分離和波譜鑒定的方法,從海洋異壁放線菌(Actinoalloteichus cyanogriseus WH1-2216-6)的發(fā)酵產(chǎn)物中分離鑒定了6個5,5,6-多環(huán)含特特拉姆酸大環(huán)內(nèi)酰胺(PTMs)類天然產(chǎn)物:16-hydroxymaltophilin(1)、dihydromaltophilin(2)、4-deoxydihydromaltophilin(3)、maltophilin(4)、xanthobaccin C(5)和FI-2(6),其中1為新化合物.評價了化合物1~5對人正常肝細胞L-02及人癌細胞A549、MCF-7、Jurkat、BXPC-3、HCT-116、PANC-1和K562的細胞毒活性,結(jié)果表明:化合物1~5對上述人癌細胞具有細胞毒活性,其半數(shù)抑制濃度(IC50)為0.1~9.7μmol·L-1;新化合物1對L-02的毒性較低,但對Jurkat、HCT-116和BXPC-3的選擇指數(shù)(SI)分別高達31.5、41.1和52.4.除化合物2和3對A549和MCF-7的腫瘤細胞毒活性外,其余的腫瘤細胞毒活性是首次報道.還測試了化合物1~6的抗煙曲霉活性,發(fā)現(xiàn)化合物2和4的活性較好,其最小抑菌濃度(MIC)分別為3.04和6.12μmol·L-1,這是首次發(fā)現(xiàn)5,5,6-PTMs類化合物具有抗煙曲霉活性.
[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.
【作者單位】： 中國海洋大學醫(yī)藥學院海洋藥物教育部重點實驗室;貴州醫(yī)科大學藥物植物功效與利用國家重點實驗室;
【基金】：國家自然科學基金(Nos.81561148012,41376148);國家自然科學基金-廣東聯(lián)合基金(No.U1501221)資助項目~~
【分類號】：R915
【正文快照】： 含氮化合物是藥物的主要形式,也是海洋微生物天然產(chǎn)物的主要結(jié)構(gòu)類型[1].多環(huán)含特特拉姆酸大環(huán)內(nèi)酰 胺類似物(Polycyclic tetramate macrolactams,PTMs)是一類來自微生物或海綿的、具有良好生物活性的天然產(chǎn)物.顧名思義,PTMs類化合物含有一個特特拉姆酸結(jié)構(gòu)單元、一個稠合的，

本文編號：1424672