Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.
College of Food Science and Bioengineering, Tianjin Agricultural University, Tianjin 300384, China.
Molecules. 2023 Mar 30;28(7):3098. doi: 10.3390/molecules28073098.
Garlic ( L.) is a traditional plant with antimicrobial activity. This study aimed to discover new antifungal peptides from garlic, identify their structure, and explore the antimicrobial mechanism. Peptides were separated by chromatography and identified by MALDI-TOF analysis. Structure and conformation were characterized by CD spectrum and NMR analysis. Mechanism studies were conducted by SEM, membrane depolarization, and transcriptomic analysis. The cytotoxicity to mammalian cells as well as drug resistance development ability were also evaluated. A novel antifungal peptide named NpRS with nine amino acids (RSLNLLMFR) was obtained. It was a kind of cationic peptide with a α-helix as the dominant conformation. NOESY correlation revealed a cyclization in the molecule. The peptide significantly inhibited the growth of . The mechanism study indicated that membrane destruction and the interference of ribosome-related pathways might be the main mechanisms of antifungal effects. In addition, the resistance gene for azole was down-regulated and the drug resistance was hardly developed in 21 days by the serial passage study. The present study identified a novel antifungal garlic peptide with low toxicity and provided new mechanism information for the peptide at the gene expression level to counter drug resistance.
大蒜（L.）是一种具有抗菌活性的传统植物。本研究旨在从大蒜中发现新的抗真菌肽，鉴定其结构，并探索其抗菌机制。通过色谱法分离肽，并通过 MALDI-TOF 分析进行鉴定。通过 CD 光谱和 NMR 分析对结构和构象进行了表征。通过 SEM、膜去极化和转录组分析进行了机制研究。还评估了对哺乳动物细胞的细胞毒性以及耐药性发展能力。获得了一种新型的具有九个氨基酸（RSLNLLMFR）的抗真菌肽，命名为 NpRS。它是一种带有 α-螺旋作为主要构象的阳离子肽。NOESY 相关揭示了分子中的环化。该肽显著抑制了 的生长。机制研究表明，膜破坏和核糖体相关途径的干扰可能是抗真菌作用的主要机制。此外，通过连续传代研究发现，唑类耐药基因 下调，21 天内耐药性很难发展。本研究鉴定了一种新型的低毒性抗真菌大蒜肽，为该肽在基因表达水平上对抗耐药性提供了新的机制信息。
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