调整两性多化衍生物的血液溶解和抗菌活性
M Firat Ilker1, Klaus Nüsslein, Gregory N Tew
1Department of Polymer Science and Engineering, University of Massachusetts Amherst, Amherst, Massachusetts 01003, USA.
Journal of the American Chemical Society
|December 2, 2004
概括
新型的两性阴阳性多元生物体具有强大的抗菌活性,具有很高的选择性. 调整聚合物水性是实现非溶血性质的关键,提供有前途的抗菌剂.
科学领域:
- 聚合物化学 聚合物化学
- 材料科学 材料科学 材料科学
- 抗菌研究 抗菌研究
背景情况:
- 开发有效的抗微生物药物对于打击抗生素耐药性的增加至关重要.
- 性聚合物因其破坏膜的抗微生物机制而被探索.
- 设计高选择性聚合物对细菌而不是宿主细胞仍然是一个挑战.
研究的目的:
- 为了合成和表征两类阴阳性多化衍生物.
- 评估这些聚合物的抗菌和溶血活性.
- 研究聚合物结构 (疏水性,分子量) 对抗微生物选择性的影响.
主要方法:
- 通过控制分子量和狭窄的多分散度的模块化norbornene单体合成多诺基基.
- 使用增长抑制试验评估的抗菌活性.
- 对人类红细胞评估的血液溶解活性.
- 脂质膜的破坏,通过来自大型单状囊泡的染料泄漏试验得到证实.
主要成果:
- 聚合物具有广泛的分子重量 (1600-137,500 g/mol) 和狭窄的多分散性 (1.1-1.3).
- 单体重复单元的疏水性显著影响了抗菌和溶血活性.
- 通过通过随机共聚合来调整聚合物疏水性,实现了高度选择性的非溶血性抗菌活性.
- 针对细菌而对人类红细胞的选择性比率在优化组合时超过100.
结论:
- 两性阴阳性多聚诺基基基是有效的和可调节的抗菌剂.
- 疏水性是平衡抗菌有效性和宿主细胞安全性的关键参数.
- 这些聚合物显示出作为具有低血溶性毒性选择性抗菌剂的显著潜力.
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