PDF(Pubmed)
Abstract：
The fungal genus Trichoderma is a rich source of structurally diverse secondary metabolites with remarkable pharmaceutical properties. The chemical constituents and anticancer activities of the marine-derived fungus Trichoderma lixii have never been investigated. In this study, a bioactivity-guided investigation led to the isolation of eleven compounds, including trichodermamide A (1), trichodermamide B (2), aspergillazine A (3), DC1149B (4), ergosterol peroxide (5), cerebrosides D/C (6/7), 5-hydroxy-2,3-dimethyl-7-methoxychromone (8), nafuredin A (9), and harzianumols E/F (10/11). Their structures were identified by using various spectroscopic techniques and compared to those in the literature. Notably, compounds 2 and 5-11 were reported for the first time from this species. Evaluation of the anticancer activities of all isolated compounds was carried out. Compounds 2, 4, and 9 were the most active antiproliferative compounds against three cancer cell lines (human myeloma KMS-11, colorectal HT-29, and pancreas PANC-1). Intriguingly, compound 4 exhibited anti-austerity activity with an IC50 of 22.43 μM against PANC-1 cancer cells under glucose starvation conditions, while compound 2 did not.
摘要：
真菌木霉属是结构多样的次生代谢产物的丰富来源,具有显著的药物特性。从未研究过海洋真菌木霉的化学成分和抗癌活性。在这项研究中,一项以生物活性为指导的研究导致了11种化合物的分离，包括曲霉菌酰胺A（1），曲菌酰胺B(2),曲霉素A（3），DC1149B(4),麦角甾醇过氧化物（5），脑苷脂D/C（6/7），5-羟基-2,3-二甲基-7-甲氧基色酮(8)，nafuredinA（9），和harzianumolsE/F（10/11）。通过使用各种光谱技术鉴定了它们的结构，并将其与文献中的结构进行了比较。值得注意的是,化合物2和5-11为首次从该物种中报道。对所有分离的化合物的抗癌活性进行评价。化合物2、4和9是针对三种癌细胞系(人骨髓瘤KMS-11、结肠直肠HT-29和胰腺PANC-1)的最具活性的抗增殖化合物。有趣的是，化合物4在葡萄糖饥饿条件下对PANC-1癌细胞表现出抗紧缩活性，IC50为22.43μM，而化合物2没有。
