Antibacterial and Anti-Inflammatory Activity of Branched Peptides Derived from Natural Host Defense Sequences,Journal of Medicinal Chemistry

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Antibacterial and Anti-Inflammatory Activity of Branched Peptides Derived from Natural Host Defense Sequences
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2024-09-11 , DOI: 10.1021/acs.jmedchem.4c00810
Giada Meogrossi ₁ , Eva Tollapi ₁ , Alessandro Rencinai ₁ , Jlenia Brunetti ₁ , Silvia Scali ₁ , Eugenio Paccagnini ₂ , Mariangela Gentile ₂ , Pietro Lupetti ₂ , Simona Pollini _{3,

4} , Gian Maria Rossolini _{3,

4} , Andrea Bernini ₅ , Alessandro Pini _{1,

6,

7} , Luisa Bracci _{1,

6} , Chiara Falciani ₁

Affiliation

Antibiotic resistance is a major global health threat, necessitating the development of new treatments and diverse molecules to combat severe infections and preserve the efficacy of existing drugs. Antimicrobial peptides (AMPs) offer a versatile arsenal against bacteria, and peptide structure branching can enhance their resistance to proteases and improve their overall efficacy. A small library of peptides derived from natural host defense peptides and synthesized in a tetrabranched form was selected against E. coli. Six selected branched peptides were further studied for antibacterial activity against a panel of strains, biofilm inhibition, protease resistance, and cytotoxicity. Their structure was predicted computationally and their mechanism of action was investigated by electron microscopy and by using fluorescent dyes. The peptide BAMP2 showed promise in a mouse skin infection model, indicating the potential for local infection treatment.

中文翻译：

源自天然宿主防御序列的支链肽的抗菌和抗炎活性

抗生素耐药性是一个主要的全球健康威胁，需要开发新的治疗方法和多样化的分子来对抗严重感染并保持现有药物的疗效。抗菌肽（AMP）提供了对抗细菌的多功能武器库，肽结构支化可以增强它们对蛋白酶的抵抗力并提高它们的整体疗效。针对大肠杆菌，选择了源自天然宿主防御肽并以四支链形式合成的小型肽库。进一步研究了 6 个选定的支链肽对一组菌株的抗菌活性、生物膜抑制、蛋白酶耐药性和细胞毒性。通过计算预测它们的结构，并通过电子显微镜和荧光染料研究它们的作用机制。肽 BAMP2 在小鼠皮肤感染模型中显示出前景，表明局部感染治疗的潜力。

更新日期：2024-09-11

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