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磷酸萘喹通过破坏细胞膜和诱导活性氧对耐头孢他啶菌的抗菌活性及机制

Antibacterial activity and mechanism of naphthoquine phosphate against ceftazidime-resistant via cell membrane disruption and ROS induction.

作者信息

Yuan Yongtian, Zhao Liangliang, Bei Zhuchun, Wang Baogang, Zhang Dongna, Xu Likun, Liu Jiahui, Lv Meng, Xu Qin, Song Yabin

机构信息

Artemisinin Research Center, Guangzhou University of Chinese Medicine, Guangzhou, China.

State Key Laboratory of Pathogen and Biosecurity, Academy of Military Medical Sciences, Beijing, China.

出版信息

Front Microbiol. 2025 Aug 4;16:1603462. doi: 10.3389/fmicb.2025.1603462. eCollection 2025.

DOI:10.3389/fmicb.2025.1603462
PMID:40831639
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12358481/
Abstract

INTRODUCTION: Drug-resistant bacteria, particularly , present a significant threat to global public health, highlighting the urgent need for novel antibacterial therapies. Drug repurposing has emerged as a promising strategy to accelerate therapeutic development by identifying new applications for existing pharmaceuticals. This study investigates the potential of naphthoquine phosphate (NQP), an antimalarial agent, as a broad-spectrum antibacterial candidate against the multidrug-resistant strain LAC-4. METHODS: To evaluate the antibacterial activity of NQP, we determined the minimum inhibitory concentration (MIC) against LAC-4. Inhibition kinetics were analyzed to assess concentration-dependent effects. Membrane permeability assays were performed to examine NQP-induced changes in cell membrane integrity. Oxidative damage tests were conducted to investigate impacts on bacterial metabolic processes. Morphological changes in LAC-4 treated with NQP of MIC were observed using transmission electron microscopy (TEM) and scanning electron microscopy (SEM). Additionally, transcriptome analysis was performed to identify disrupted physiological pathways associated with NQP exposure. RESULTS AND DISCUSSION: NQP exhibited broad-spectrum antibacterial activity, with a MIC of 62.5 μg/mL against LAC-4. Its inhibition kinetics curve confirmed a concentration-dependent inhibitory effect. Membrane permeability tests revealed that NQP disrupts cell membrane integrity, enhancing permeability-consistent with TEM/SEM observations showing significant structural damage in NQP-treated , including membrane rupture, cellular deformation, and cytoplasmic disorganization. Oxidative damage tests indicated NQP impacts bacterial metabolism, and transcriptome analysis further demonstrated that NQP disrupts multiple physiological pathways, primarily through enhanced membrane permeability and induced oxidative stress. These findings support NQP as a promising molecular scaffold for developing novel therapies against infections, highlighting its potential in drug repurposing strategies for combating drug resistance.

摘要

引言：耐药细菌，尤其是[具体细菌名称未给出]，对全球公共卫生构成重大威胁，凸显了对新型抗菌疗法的迫切需求。药物重新利用已成为一种有前景的策略，可通过确定现有药物的新用途来加速治疗药物的开发。本研究调查了抗疟药物磷酸萘喹（NQP）作为针对多重耐药菌株LAC - 4的广谱抗菌候选药物的潜力。 方法：为评估NQP的抗菌活性，我们测定了其对LAC - 4的最低抑菌浓度（MIC）。分析抑制动力学以评估浓度依赖性效应。进行膜通透性测定以检查NQP诱导的细胞膜完整性变化。进行氧化损伤测试以研究对细菌代谢过程的影响。使用透射电子显微镜（TEM）和扫描电子显微镜（SEM）观察用MIC浓度的NQP处理的LAC - 4的形态变化。此外，进行转录组分析以确定与NQP暴露相关的受干扰生理途径。 结果与讨论：NQP表现出广谱抗菌活性，对LAC - 4的MIC为62.5μg/mL。其抑制动力学曲线证实了浓度依赖性抑制作用。膜通透性测试表明NQP破坏细胞膜完整性，增强通透性，这与TEM/SEM观察结果一致，显示在NQP处理的[细菌名称未给出]中存在显著结构损伤，包括膜破裂、细胞变形和细胞质紊乱。氧化损伤测试表明NQP影响细菌代谢，转录组分析进一步证明NQP破坏多种生理途径，主要是通过增强膜通透性和诱导氧化应激。这些发现支持NQP作为开发针对[感染类型未明确]感染的新型疗法的有前景分子支架，突出了其在对抗耐药性的药物重新利用策略中的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9965/12358481/07d28aa1fa5b/fmicb-16-1603462-g010.jpg
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[1]
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