Synthesis and Antibacterial Activities of Amphiphilic Neomycin B-based Bilipid Conjugates and Fluorinated Neomycin B-based Lipids
Synthesis and Antibacterial Activities of Amphiphilic Neomycin B-based Bilipid Conjugates and Fluorinated Neomycin B-based Lipids
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DOI：
10.3390/molecules17089129
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发表时间：
2012-08-01
期刊：
影响因子：
4.6
通讯作者：
Schweizer, Frank
中科院分区：
文献类型：
--
作者：
Bera, Smritilekha;Dhondikubeer, Ramesh;Schweizer, Frank
为了研究脂质疏水性对两亲性新霉素 B 缀合物活性的影响，创建了六种聚阳离子两亲物 (PA)。其中四种新化合物结合了棕榈酸或花生二脂赖氨酸尾部，而两种则具有单氟化十一烷酸尾部。通过掺入六个胍部分增加了一半化合物的碱度，以评估碱强度对抗菌活性的影响。测试使用了一组十种细菌，其中七种菌株来自美国典型培养物保藏中心系列，三种临床分离株来自加拿大重症监护病房。与之前的碳氢单脂结果相比，发现所有化合物的活性均降低，但具有氟化尾部的化合物的溶血活性急剧降低，抗菌活性仅中度降低。
Investigating the effect of lipid hydrophobicity on the activity of amphiphilic neomycin B conjugates, six polycationic amphiphiles (PAs) were created. Four of the new compounds incorporated either palmitic or arachidic di-lipid lysine tails, while two had single fluorinated undecanoic acid tails. The basicity of half of the compounds was increased through the incorporation of six guanidine moieties, in order to assess the effect of base strength on antimicrobial activity. A panel of ten bacteria was used for the testing, with seven strains obtained from the American Type Culture Collection series and three clinical isolates from Canadian Intensive Care Units. When compared to previous results with hydrocarbon monolipids the PAs all compounds were found to have reduced activity, though the hemolytic activity of the compounds with fluorinated tails was sharply reduced, with only a moderate reduction in antimicrobial activity.