Guo Jiacheng, Yang Jin, Wang Pei, Guo Bo, Li Huifang, Zhang Di, An Faliang, Gao Song
Jiangsu Key Laboratory of Marine Biological Resources and Environment, Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, MNR Key Laboratory of Coastal Salt Marsh Ecosystems and Resources, School of Pharmacy, Co-Innovation Center of Jiangsu Marine Bio-Industry Technology, Jiangsu Ocean University, Lianyungang, 222005, China.
Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai, 200237, China.
Bioresour Bioprocess. 2023 Feb 2;10(1):11. doi: 10.1186/s40643-023-00628-5.
Vibrio species (Vibrio sp.) is a class of Gram-negative aquatic bacteria that causes vibriosis in aquaculture, which have resulted in big economic losses. Utilization of antibiotics against vibriosis has brought concerns on antibiotic resistance, and it is essential to explore potential antibiotic alternatives. In this study, seven compounds (compounds 1-7) were isolated from the Arctic endophytic fungus Penicillium sp. Z2230, among which compounds 3, 4, and 5 showed anti-Vibrio activity. The structures of the seven compounds were comprehensively elucidated, and the antibacterial mechanism of compounds 3, 4, and 5 was explored by molecular docking. The results suggested that the anti-Vibrio activity could come from inhibition of the bacterial peptide deformylase (PDF). This study discovered three Penicillium-derived compounds to be potential lead molecules for developing novel anti-Vibrio agents, and identified PDF as a promising antibacterial target. It also expanded the bioactive diversity of polar endophytic fungi by showing an example in which the secondary metabolites of a polar microbe were a good source of natural medicine.
弧菌属细菌是一类革兰氏阴性水生细菌，可在水产养殖中引发弧菌病，已造成巨大经济损失。使用抗生素对抗弧菌病引发了对抗生素耐药性的担忧，因此探索潜在的抗生素替代品至关重要。在本研究中，从北极内生真菌青霉属Z2230中分离出七种化合物（化合物1 - 7），其中化合物3、4和5表现出抗弧菌活性。全面阐明了这七种化合物的结构，并通过分子对接探索了化合物3、4和5的抗菌机制。结果表明，抗弧菌活性可能源于对细菌肽脱甲酰基酶（PDF）的抑制。本研究发现三种源自青霉的化合物是开发新型抗弧菌药物的潜在先导分子，并确定PDF为有前景的抗菌靶点。通过展示极地微生物的次生代谢产物是天然药物良好来源的实例，还扩展了极地内生真菌的生物活性多样性。
