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鲨胺:对抗多重耐药革兰氏阴性菌出现的合适策略?

Squalamine: an appropriate strategy against the emergence of multidrug resistant gram-negative bacteria?

作者信息

Salmi Chanaz, Loncle Celine, Vidal Nicolas, Letourneux Yves, Fantini Jacques, Maresca Marc, Taïeb Nadira, Pagès Jean-Marie, Brunel Jean Michel

机构信息

UMR-MD1, Facultés de Médecine et de Pharmacie, Marseille, France.

出版信息

PLoS One. 2008 Jul 23;3(7):e2765. doi: 10.1371/journal.pone.0002765.

Abstract

We reported that squalamine is a membrane-active molecule that targets the membrane integrity as demonstrated by the ATP release and dye entry. In this context, its activity may depend on the membrane lipid composition. This molecule shows a preserved activity against bacterial pathogens presenting a noticeable multi-resistance phenotype against antibiotics such as polymyxin B. In this context and because of its structure, action and its relative insensitivity to efflux resistance mechanisms, we have demonstrated that squalamine appears as an alternate way to combat MDR pathogens and by pass the gap regarding the failure of new active antibacterial molecules.

摘要

我们报道,鲨胺是一种膜活性分子,如ATP释放和染料进入所证明的那样,它靶向膜完整性。在这种情况下,其活性可能取决于膜脂质组成。该分子对呈现出对多粘菌素B等抗生素明显多重耐药表型的细菌病原体具有保留活性。在这种情况下,由于其结构、作用以及对耐药机制相对不敏感,我们已经证明鲨胺似乎是对抗多重耐药病原体的一种替代方法,并且可以弥补新型活性抗菌分子失效方面的差距。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2d94/2447875/27297c78ed45/pone.0002765.g001.jpg

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