CAS and Shandong Province Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences, Nanhai Road 7, Qingdao 266071, China.
University of Chinese Academy of Sciences, Yuquan Road 19A, Beijing 100049, China.
Mar Drugs. 2023 Mar 22;21(3):195. doi: 10.3390/md21030195.
A large body of fungal secondary metabolites has been discovered to exhibit potent antibacterial activities with distinctive mechanisms and has the potential to be an untapped resource for drug discovery. Here, we describe the isolation and characterization of five new antibacterial indole diketopiperazine alkaloids, namely 24,25-dihydroxyvariecolorin G (), 25-hydroxyrubrumazine B (), 22-chloro-25-hydroxyrubrumazine B (), 25-hydroxyvariecolorin F (), and 27-epi-aspechinulin D (), along with the known analogue neoechinulin B () from a fungal strain of deep-sea cold seep-derived . Among these compounds, and represented a class of infrequently occurring fungal chlorinated natural products. Compounds - showed inhibitory activities against several pathogenic bacteria with MIC values ranging from 4 to 32 μg/mL. It was revealed that compound could induce structural damage to the cells based on the observation by scanning electron microscopy (SEM), which led to the bacteriolysis and death of , suggesting that neoechinulin B () might be a potential alternative to novel antibiotics development.
大量真菌次生代谢产物被发现具有强大的抗菌活性,其作用机制独特,有可能成为药物发现的未开发资源。在这里,我们描述了五个新的具有抗菌作用的吲哚二酮哌嗪生物碱的分离和特性,分别为 24,25-二羟基变色酸 G (), 25-羟基红紫素 B (), 22-氯-25-羟基红紫素 B (), 25-羟基变色酸 F (), 和 27-表-阿皮素灵 D (), 以及从深海冷渗流衍生的真菌菌株中分离得到的已知类似物 neoechinulin B ()。在这些化合物中, 和 代表了一类罕见的真菌氯化天然产物。化合物 - 对几种致病菌具有抑制活性,MIC 值范围为 4 至 32 μg/mL。扫描电子显微镜 (SEM) 的观察结果表明,化合物 可以诱导 细胞的结构损伤,导致 细菌溶解和死亡,这表明 neoechinulin B ()可能是新型抗生素开发的潜在替代品。