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一种可光活化的二芳基乙炔对革兰氏阳性菌的抗菌活性。

The antibacterial activity of a photoactivatable diarylacetylene against Gram-positive bacteria.

作者信息

Waite Ryan, Adams Candace T, Chisholm David R, Sims C H Cole, Hughes Joshua G, Dias Eva, White Emily A, Welsby Kathryn, Botchway Stanley W, Whiting Andrew, Sharples Gary J, Ambler Carrie A

机构信息

Department of Biosciences, Durham University, Science Site, Durham, United Kingdom.

LightOx Limited, Newcastle, United Kingdom.

出版信息

Front Microbiol. 2023 Sep 22;14:1243818. doi: 10.3389/fmicb.2023.1243818. eCollection 2023.

DOI:10.3389/fmicb.2023.1243818
PMID:37808276
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10556703/
Abstract

The emergence of antibiotic resistance is a growing threat to human health, and therefore, alternatives to existing compounds are urgently needed. In this context, a novel fluorescent photoactivatable diarylacetylene has been identified and characterised for its antibacterial activity, which preferentially eliminates Gram-positive over Gram-negative bacteria. Experiments confirmed that the Gram-negative lipopolysaccharide-rich outer surface is responsible for tolerance, as strains with reduced outer membrane integrity showed increased susceptibility. Additionally, bacteria deficient in oxidative damage repair pathways also displayed enhanced sensitivity, confirming that reactive oxygen species production is the mechanism of antibacterial activity. This new diarylacetylene shows promise as an antibacterial agent against Gram-positive bacteria that can be activated , potentially for the treatment of skin infections.

摘要

抗生素耐药性的出现对人类健康构成了日益严重的威胁，因此，迫切需要现有化合物的替代品。在此背景下，一种新型的荧光光活化二芳基乙炔已被鉴定并表征其抗菌活性，该化合物对革兰氏阳性菌的消除作用优于革兰氏阴性菌。实验证实，富含革兰氏阴性菌脂多糖的外表面是耐受性的原因，因为外膜完整性降低的菌株显示出更高的敏感性。此外，缺乏氧化损伤修复途径的细菌也表现出更高的敏感性，这证实了活性氧的产生是抗菌活性的机制。这种新型二芳基乙炔有望成为一种可被激活的抗革兰氏阳性菌的抗菌剂，有可能用于治疗皮肤感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/b0fa7e2eea99/fmicb-14-1243818-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/61554a60fa8f/fmicb-14-1243818-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/0ddec54ff74d/fmicb-14-1243818-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/d3c97acbc64d/fmicb-14-1243818-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/0d774d9ee30f/fmicb-14-1243818-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/80628816baed/fmicb-14-1243818-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/2732f8958851/fmicb-14-1243818-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/69ec6451c7bc/fmicb-14-1243818-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/957d70c5d35a/fmicb-14-1243818-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/b0fa7e2eea99/fmicb-14-1243818-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/61554a60fa8f/fmicb-14-1243818-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/0ddec54ff74d/fmicb-14-1243818-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/d3c97acbc64d/fmicb-14-1243818-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/0d774d9ee30f/fmicb-14-1243818-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/80628816baed/fmicb-14-1243818-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/2732f8958851/fmicb-14-1243818-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/69ec6451c7bc/fmicb-14-1243818-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/957d70c5d35a/fmicb-14-1243818-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8e34/10556703/b0fa7e2eea99/fmicb-14-1243818-g009.jpg

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