Hubrecht Institute-KNAW and University Medical Center Utrecht, Utrecht, The Netherlands.
Institute Biology Leiden, Leiden University, Leiden, The Netherlands.
Sci Rep. 2021 Sep 21;11(1):18774. doi: 10.1038/s41598-021-98252-w.
Antimicrobial resistance has become one of the major threats to human health. Therefore, there is a strong need for novel antimicrobials with new mechanisms of action. The kingdom of fungi is an excellent source of antimicrobials for this purpose because it encompasses countless fungal species that harbor unusual metabolic pathways. Previously, we have established a library of secondary metabolites from 10,207 strains of fungi. Here, we screened for antimicrobial activity of the library against seven pathogenic bacterial strains and investigated the identity of the active compounds using ethyl acetate extraction, activity-directed purification using HPLC fractionation and chemical analyses. We initially found 280 antimicrobial strains and subsequently identified 17 structurally distinct compounds from 26 strains upon further analysis. All but one of these compounds, berkchaetoazaphilone B (BAB), were known to have antimicrobial activity. Here, we studied the antimicrobial properties of BAB, and found that BAB affected energy metabolism in both prokaryotic and eukaryotic cells. We conclude that fungi are a rich source of chemically diverse secondary metabolites with antimicrobial activity.
抗菌耐药性已成为人类健康的主要威胁之一。因此,我们迫切需要具有新型作用机制的新型抗菌药物。真菌界是此类抗菌药物的绝佳来源,因为它包含无数具有独特代谢途径的真菌物种。此前,我们已经建立了一个包含 10207 株真菌次级代谢产物的文库。在这里,我们筛选了该文库对七种致病菌的抗菌活性,并使用乙酸乙酯萃取、HPLC 分级分离和化学分析的活性导向纯化方法来研究活性化合物的结构。我们最初发现了 280 株具有抗菌活性的菌株,随后在进一步分析中从 26 株菌株中鉴定出 17 种结构不同的化合物。除了一个化合物 berkchaetoazaphilone B (BAB) 之外,其余化合物都具有抗菌活性。在这里,我们研究了 BAB 的抗菌特性,发现 BAB 影响原核和真核细胞的能量代谢。我们得出结论,真菌是具有抗菌活性的化学多样性次级代谢产物的丰富来源。