Antibacterial properties of cationic steroid antibiotics.

Antibacterial properties of cationic steroid antibiotics.
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DOI:
10.1111/j.1574-6968.2002.tb11448.x
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发表时间:
2002-11
影响因子:
2.1
通讯作者:
P. Savage;Chunhong Li;U. Taotafa;Bangwei Ding;Qunying Guan
P. Savage;Chunhong Li;U. Taotafa;Bangwei Ding;Qunying Guan
中科院分区:
生物学4区
文献类型:
--
作者:
P. Savage;Chunhong Li;U. Taotafa;Bangwei Ding;Qunying Guan

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已开发出显示广谱抗菌活性的阳离子类固醇抗生素。这些化合物由附加有胺基团的甾族化合物组成,所述胺基团被排列以产生表面两亲性形态。这些抗生素的例子具有高度杀菌性,而相关化合物有效地渗透革兰氏阴性细菌的外膜,使这些生物体对疏水性抗生素敏感。阳离子类固醇抗生素表现出各种水平的真核生物与原核生物细胞选择性,并且细胞选择性可以通过原核细胞的电荷识别来增加。对这些抗生素作用机制的研究表明,它们与阳离子肽类抗生素具有相同的作用机制。
Cationic steroid antibiotics have been developed that display broad-spectrum antibacterial activity. These compounds are comprised of steroids appended with amine groups arranged to yield facially amphiphilic morphology. Examples of these antibiotics are highly bactericidal, while related compounds effectively permeabilize the outer membranes of Gram-negative bacteria sensitizing these organisms to hydrophobic antibiotics. Cationic steroid antibiotics exhibit various levels of eukaryote vs. prokaryote cell selectivity, and cell selectivity can be increased via charge recognition of prokaryotic cells. Studies of the mechanism of action of these antibiotics suggest that they share mechanistic aspects with cationic peptide antibiotics.