Biology Institute, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250103, China.
East China University of Science and Technology, 130 Meilong Road, Shanghai, 200237, China.
J Antibiot (Tokyo). 2021 May;74(5):317-323. doi: 10.1038/s41429-020-00398-8. Epub 2021 Feb 8.
Fungi are important resources for drug development, as they have a diversity of genes, that can produce novel secondary metabolites with effective bioactivities. Here, five depsidone-based analogs were isolated from the rice media of Chaetomium brasiliense SD-596. Their structures were elucidated using NMR and mass spectrometry analysis. Five compounds, including three new depsidone analogs, mollicellin S (1), mollicellin T (2), and mollicellin U (3), and two known compounds, mollicellin D (4) and mollicellin H (5), exhibited significant inhibition against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA), with MIC values ranging from 6.25 to 12.5 μg ml. Herein, we identified the predicted plausible biosynthetic cluster of the compounds and discussed the structure-activity relationship. Finally, we found that the introduction of aldehyde and methoxyl groups provide marked improvement for the inhibition against MRSA.
真菌是药物开发的重要资源，因为它们具有多样性的基因，可以产生具有有效生物活性的新型次级代谢产物。在这里，从 Chaetomium brasiliense SD-596 的大米培养基中分离出了五种基于去甲二萜的类似物。通过 NMR 和质谱分析阐明了它们的结构。五种化合物，包括三种新的去甲二萜类似物，莫利西林 S（1）、莫利西林 T（2）和莫利西林 U（3），以及两种已知化合物，莫利西林 D（4）和莫利西林 H（5），对金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌（MRSA）表现出显著的抑制作用，MIC 值范围为 6.25 至 12.5μg/ml。在此，我们鉴定了化合物的预测合理生物合成簇，并讨论了结构-活性关系。最后，我们发现醛基和甲氧基的引入对抑制 MRSA 有显著改善。
