首页|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

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

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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(NMR)、质谱(MS)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3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6个化合物,包括1个新的硫代二酮哌嗪类化合物aspersin(1)与5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6具有肿瘤细胞毒活性.
A new antitumor thiodiketopiperazine from the marine-derived fungus Aspergillus sp.HH-3
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(A549,HepG2,HeLa)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).Compounds 1,2,and 6 showed moderate cytotoxic activities against tumour cells of A549,HepG2 and HeLa.Conclusion Compound 1 is a new thiodiketopiperazine.Compounds 1,2,and 6 exhibit moderate antitumor activity.

marine-derived fungiAspergillus sp.secondary metabolitescytotoxic activity

管新帅、周侠、杨婧怡、曹胜、张雪梅

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山东国欣颐养集团枣庄中心医院药学部,山东枣庄 277100

山东理工大学生命科学学院,山东淄博 255000

枣庄学院食品科学与制药工程学院,山东枣庄 277000

山东国欣颐养集团枣庄中心医院重症监护室,山东枣庄 277100

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海洋真菌 Aspergillus sp. 次级代谢产物 细胞毒活性

白求恩医学科学研究基金

AE023AN

2024

中国海洋药物
中国药学会

中国海洋药物

CSTPCD
影响因子:0.539
ISSN:1002-3461
年,卷(期):2024.43(3)