管新帅,周侠,杨婧怡,等.海洋真菌Aspergillus sp.HH-3中1个新的抗肿瘤硫代二酮哌嗪类化合物[J].中国海洋药物,2024,43(3):67-72. |
海洋真菌Aspergillus sp.HH-3中1个新的抗肿瘤硫代二酮哌嗪类化合物 |
A New Antitumor Thiodiketopiperazine from the Marine-Derived Fungus Aspergillus sp. HH-3 |
投稿时间:2023-11-08 修订日期:2023-11-29 |
DOI:10.13400/j.cnki.cjmd.2024.03.008 |
中文关键词: 海洋真菌 Aspergillus sp. 次级代谢产物 细胞毒活性 |
English Keywords:Marine-derived fungi Aspergillus sp. secondary metabolites cytotoxic activity |
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中文摘要: |
目的 研究海泥真菌Aspergillus sp.HH-3的次级代谢产物及其抗肿瘤活性。方法 使用硅胶色谱柱、LH-20凝胶色谱等对代谢粗提物进行分离纯化;运用核磁共振、质谱等方法并结合文献报道数据确定化合物的结构;采用CCK-8法评价化合物对三种肿瘤细胞(A549、HepG2、Hela)的抑制活性。结果 从Aspergillus sp.HH-3中分离获得六个化合物,包括一个新的硫代二酮哌嗪类化合物aspersin(1)与五个已知化合物dehydroxymethylbis(dethio)bis(methylthio)gliotoxin(2)、trypacidin(3)、monomethylsubchrin(4)、verruculogen(5)及chaetominine(6)。化合物1、2和6显示有一定的肿瘤细胞抑制活性。结论 化合物1为新的硫代二酮哌嗪类化合物;化合物1、2和4具有肿瘤细胞毒活性。 |
English Summary: |
Objective To study the cytotoxic secondary metabolites of the Marine-Derived Fungus Aspergillus sp. HH-3. Methods The crude metabolite was purified by silica gel and Sephadex LH-20 chromatography. The structures of the compounds were elucidated by MS and NMR analysis. The cytotoxities of the compounds against three tumor cells were evaluated using CCK-8 method. Results Six compounds were isolated from the marine-derived fungus Aspergillus sp. HH-3 including one new compound aspersin (1), and five known ones dehydroxymethylbis(dethio)bis(methylthio)gliotoxin (2), trypacidin (3), monomethylsubchrin (4), verruculogen (5) and chaetominine (6). Compound 1, 2, and 4 showed moderate cytotoxic activities against tumour cells of A549, HepG2 and HCT116. Conclusion Compound 1 is a new thiodiketopiperazine. Compounds 1, 2, and 4 exhibit moderate antitumor activity. |
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