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优化后的Pom-1衍生物对致病性酵母生物膜的活性增强。

Increased Activities against Biofilms of the Pathogenic Yeast of Optimized Pom-1 Derivatives.

作者信息

Amann Valerie, Kissmann Ann-Kathrin, Krämer Markus, Krebs Imke, Perez-Erviti Julio A, Otero-Gonzalez Anselmo J, Morales-Vicente Fidel, Rodríguez Armando, Ständker Ludger, Weil Tanja, Rosenau Frank

机构信息

Institute of Pharmaceutical Biotechnology, Ulm University, Albert-Einstein-Allee 11, 89081 Ulm, Germany.

Center for Protein Studies, Faculty of Biology, University of Havana, 25 Str. and I Str., La Habana 10400, Cuba.

出版信息

Pharmaceutics. 2022 Jan 28;14(2):318. doi: 10.3390/pharmaceutics14020318.

DOI:10.3390/pharmaceutics14020318
PMID:35214049
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8877593/
Abstract

Antimicrobial peptides (AMPs) are an alternative group for the therapy of infectious diseases, with activity against a wide range of diverse pathogens. However, classical AMPs have significant side effects in human cells due to their unspecific pore formation in biomembranes. Nevertheless, AMPs are promising therapeutics and can be isolated from natural sources, which include sea and freshwater molluscs. The AMPs identified in these organisms show promising antimicrobial activities, as pathogens are mainly fought by innate defence mechanisms. An auspicious candidate among molluscs is the Cuban freshwater snail , from which the peptides Pom-1 and Pom-2 have been isolated and studied. These studies revealed significant antimicrobial activities for both AMPs. Based on the activities determined, Pom-1 was used for further optimization. In order to meet the emerging requirements of improved anti-biofilm activity against naturally occurring species, the six derivatives Pom-1A to F were developed and investigated. Analysis of the derivatives acting on the most abundant naturally occurring yeast () revealed a strong anti-biofilm activity, especially induced by Pom-1 B, C, and D. Furthermore, a moderate decrease in the metabolic activity of planktonic yeast cells was observed.

摘要

抗菌肽(AMPs)是治疗传染病的另一类药物,对多种不同病原体具有活性。然而,经典抗菌肽由于在生物膜中形成非特异性孔道,在人体细胞中具有显著的副作用。尽管如此,抗菌肽仍是有前景的治疗药物,可从包括海洋和淡水软体动物在内的天然来源中分离得到。在这些生物中鉴定出的抗菌肽显示出有前景的抗菌活性,因为病原体主要通过先天防御机制来对抗。软体动物中的一个有前景的候选者是古巴淡水蜗牛,从中分离并研究了肽Pom-1和Pom-2。这些研究揭示了这两种抗菌肽都具有显著的抗菌活性。基于所确定的活性,Pom-1被用于进一步优化。为了满足对针对天然存在的物种提高抗生物膜活性的新要求,开发并研究了六种衍生物Pom-1A至F。对作用于最丰富的天然存在的酵母()的衍生物的分析显示出很强的抗生物膜活性,尤其是由Pom-1 B、C和D诱导的。此外,观察到浮游酵母细胞的代谢活性有适度下降。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/0ea2a624430b/pharmaceutics-14-00318-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/b8f415f5e292/pharmaceutics-14-00318-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/0bcba9cace94/pharmaceutics-14-00318-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/d2a74cf0ecca/pharmaceutics-14-00318-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/fecc3842c7a2/pharmaceutics-14-00318-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/0ea2a624430b/pharmaceutics-14-00318-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/b8f415f5e292/pharmaceutics-14-00318-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/0bcba9cace94/pharmaceutics-14-00318-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/d2a74cf0ecca/pharmaceutics-14-00318-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/fecc3842c7a2/pharmaceutics-14-00318-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8877593/0ea2a624430b/pharmaceutics-14-00318-g005.jpg

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