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超越两平衡:变化的子单元立体化学改变了尼龙-3聚合物的孔形成活性
Lei Liu1, Kevin C Courtney2,3, Sean W Huth1
1Department of Chemistry, University of Wisconsin-Madison, Madison, Wisconsin 53706, United States.
Journal of the American Chemical Society
|February 22, 2021
概括
立体化学,不仅仅是两平衡,对真核细胞膜的合成聚合物活性有显著影响. 这一发现为设计有效和特定的抗菌聚合物提供了新的途径.
科学领域:
- 聚合物化学
- 生物材料科学
- 抗微生物剂
背景情况:
- 两性尼龙-3聚合物作为抗菌剂具有前景,模仿天然,具有高细菌效能和低真核毒性.
- 两平衡是关键特征,决定了聚合物的活性,而疏水性水平对疗效和安全至关重要.
研究的目的:
- 调查两平衡之外的因素是否会影响合成聚合物的生物活性.
- 探索立体化学在调节尼龙-3聚合物的活性和毒性概况中的作用.
主要方法:
- 合成具有乙基和氨基甲基侧链的立体异构子单元的新尼龙-3聚合物.
- 对抗菌活性和真核细胞膜破坏的评估.
- 使用平面脂质双层和合成脂质体来阐明膜相互作用机制的实验.
主要成果:
- 尽管两性平衡相似,但子单元中的立体化学差异显著改变了真核细胞膜的破坏.
- 抗菌活性在很大程度上不受子单元立体化学的影响.
- 由聚合物介导的孔隙形成引起的真核膜破坏.
结论:
- 超出两平衡的因素,如子单元立体化学,对合成聚合物的膜活性产生重要影响.
- 由立体化学产生的不同形状倾向可以导致聚合物链形状和膜相互作用的变化.
- 立体化学是优化抗菌聚合物特异性和有效性的关键,以前被低估的设计参数.
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