College of Chemistry and Chemical Engineering, Henan University of Technology, Zhengzhou 450001, PR China.
College of Chemistry and Chemical Engineering, Henan University of Technology, Zhengzhou 450001, PR China.
Spectrochim Acta A Mol Biomol Spectrosc. 2025 Jan 15;325:125084. doi: 10.1016/j.saa.2024.125084. Epub 2024 Sep 5.
A series of Andricin B derivatives were designed and synthesized using fatty acid modification at N-terminus of the antimicrobial peptides. The hydrophobicity of Andricin B was altered through fatty acid modification, and the bioactivity was investigated. The interaction between Andricin B and its derivatives with DNA was measured using multi-spectroscopy. Spectroscopic analysis revealed that Andricin B and its derivatives can interact with ct-DNA and G-quadruplexes DNA, and the interaction related with the length of fatty acid chain. Antimicrobial activity tests showed a significant increase using peptides with 8-10 carbons fatty acid chain. C10-Andricin B exhibited the highest antimicrobial activity, with up to a 16-fold enhancement compared to the original peptide Andricin B. Meanwhile, the protease hydrolysis stability test showed that fatty acid modification improved the stability of Andricin B against protease. Scanning electron microscopy results distinctly showed that C8-Andricin B could rupture the cell wall of bacteria. All results indicated that fatty acid modification peptides are an effective strategy for enhancing activity and stability of antimicrobial peptides. This research provides valuable insights for further research on antimicrobial peptides.
一系列安普霉素 B 衍生物被设计和合成，方法是在抗菌肽的 N 端进行脂肪酸修饰。通过脂肪酸修饰改变了安普霉素 B 的疏水性，并研究了其生物活性。使用多光谱法测量了安普霉素 B 及其衍生物与 DNA 的相互作用。光谱分析表明，安普霉素 B 及其衍生物可以与 ct-DNA 和 G-四链体 DNA 相互作用，并且这种相互作用与脂肪酸链的长度有关。抗菌活性测试表明，使用具有 8-10 个碳原子脂肪酸链的肽可显著提高抗菌活性，与原始肽安普霉素 B 相比，抗菌活性提高了 16 倍。同时，蛋白酶水解稳定性测试表明，脂肪酸修饰提高了安普霉素 B 对蛋白酶的稳定性。扫描电子显微镜的结果明显表明，C8-安普霉素 B 可以破坏细菌的细胞壁。所有结果表明，脂肪酸修饰肽是增强抗菌肽活性和稳定性的有效策略。本研究为进一步研究抗菌肽提供了有价值的见解。
