陈诺波丁衍生合成的抗菌和抗病毒特性
Marcia L Feijoo-Coronel1, Bruno Mendes1, David Ramírez2
1Biomolecules Discovery Group, Universidad Regional Amazónica Ikiam, Km 7 Via Muyuna, Tena 150101, Ecuador.
Antibiotics (Basel, Switzerland)
|January 22, 2024
概括
来自昆的植物衍生抗微生物.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 药物发现 药物发现 药物发现
背景情况:
- 抗微生物 (AMP) 对于治疗传染病至关重要.
- 来自植物的支架为新型AMP开发提供了潜力.
- 昆的陈诺波丁蛋白是治疗性的有希望的来源.
研究的目的:
- 从陈诺波丁蛋白中设计和制造新的抗微生物.
- 评估这些的抗菌和抗病毒活性.
- 为了研究陈诺波丁衍生的的作用机制.
主要方法:
- 基于计算机和物理化学的酸设计策略.
- 合成和实验室评估四种来自陈诺波丁的 (Chen1, Chen2, ChenR, ChenW) 对抗细菌菌株 (黄金葡萄球菌,大肠杆菌) 和SARS-CoV-2.
- 血液溶解测定和光显微镜测试以评估的毒性和膜相互作用.
- 分子动态模拟以阐明膜破坏的机制.
主要成果:
- 陈1没有显示抗菌活性,而陈2,陈R和陈W则表现出对S. aureus和E. coli的显著抗菌作用.
- 使用阴离子 (ChenR) 或疏水性 (ChenW) 替代物的工程具有增强的活性.
- 酸具有较低的溶血活性,这表明其安全性很好.
- 观察到膜破坏和孔隙形成,一些形成二次结构.
- 陈2和陈R有效地减少了SARS-CoV-2感染.
结论:
- 陈诺波丁作为设计无毒,强效抗菌和抗病毒的宝贵模板.
- 化学修改,如引入阴离子或芳香残留物,增强的疗效.
- 陈诺波丁衍生的可以作为新型治疗药物对抗细菌和病毒感染.
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