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新型喹喔啉衍生物 2-氯-3-肼基喹喔啉对念珠菌属真菌的杀菌效果。

The fungicidal effectiveness of 2-Chloro-3-hydrazinylquinoxaline, a newly developed quinoxaline derivative, against Candida species.

机构信息

Faculty of Medicine, Department of Clinical Microbiology and Immunology, King Abdulaziz University, Jeddah, Saudi Arabia.

Center of Research Excellence for Drug Research and Pharmaceutical Industries, King Abdulaziz University, Jeddah, Saudi Arabia.

出版信息

PLoS One. 2024 May 10;19(5):e0303373. doi: 10.1371/journal.pone.0303373. eCollection 2024.

DOI:10.1371/journal.pone.0303373
PMID:38728271
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11086890/
Abstract

BACKGROUND

Candida represents a prevalent fungal infection, notable for its substantial implications on morbidity and mortality rates. In the landscape of prospective treatments, quinoxaline derivatives emerge as a category of compact compounds exhibiting notable potential in addressing infections. These derivatives showcase promising antimicrobial efficacy coupled with favorable pharmacokinetic and safety characteristics.

AIMS

The central aim of this investigation was to examine the antifungal characteristics of 2-Chloro-3-hydrazinylquinoxaline against diverse strains of Candida and Aspergillus in vitro. Additionally, we endeavored to assess the in vivo efficacy of 2-Chloro-3-hydrazinylquinoxaline using a murine model for oral candidiasis induced by C. albicans cells ATCC 10231.

RESULTS

2-Chloro-3-hydrazinylquinoxaline demonstrated noteworthy effectiveness when tested against various reference strains of Candida species. It exhibited heightened efficacy, particularly against Candida krusei isolates. However, its performance against Candida albicans, Candida tropicalis, Candida glabrata, Candida parapsilosis, and Candida auris isolates exhibited variability. Notably, 2-Chloro-3-hydrazinylquinoxaline manifests variable efficacy against Aspergillus fumigatus, Aspergillus niger, Aspergillus terreus and Aspergillus flavus and no effect against Aspergillus brasiliensis. In a murine model, 2-Chloro-3-hydrazinylquinoxaline exhibited significant efficacy in combating the C. albicans cells ATCC 10231 strain, underscoring its potential as a viable treatment option.

CONCLUSION

2-Chloro-3-hydrazinylquinoxaline has demonstrated substantial potential in effectively addressing various Candida and Aspergillus species, showcasing dual attributes of antifungal and anti-inflammatory properties. However, to attain a more comprehensive understanding of its therapeutic capabilities, further investigations, incorporating additional tests and experiments, are imperative.

摘要

背景

念珠菌是一种常见的真菌感染,其对发病率和死亡率有重大影响。在前景治疗中,喹喔啉衍生物作为一类具有显著潜力的紧凑型化合物出现,可用于治疗感染。这些衍生物表现出有希望的抗菌功效,同时具有良好的药代动力学和安全性特征。

目的

本研究的主要目的是检查 2-氯-3-肼基喹喔啉对体外不同念珠菌和曲霉菌株的抗真菌特性。此外,我们还试图使用白色念珠菌 ATCC 10231 细胞诱导的口腔念珠菌病的小鼠模型来评估 2-氯-3-肼基喹喔啉的体内疗效。

结果

2-氯-3-肼基喹喔啉对各种参考念珠菌属菌株表现出显著的有效性。它对克柔念珠菌分离株表现出更高的功效,但对白色念珠菌、热带念珠菌、光滑念珠菌、近平滑念珠菌和耳念珠菌分离株的功效则表现出变异性。值得注意的是,2-氯-3-肼基喹喔啉对烟曲霉、黑曲霉、土曲霉和黄曲霉表现出可变的功效,而对巴西曲霉则没有效果。在小鼠模型中,2-氯-3-肼基喹喔啉对白色念珠菌 ATCC 10231 菌株表现出显著的疗效,突出了其作为一种可行治疗选择的潜力。

结论

2-氯-3-肼基喹喔啉在有效治疗各种念珠菌和曲霉菌方面表现出了巨大的潜力,具有抗真菌和抗炎的双重特性。然而,为了更全面地了解其治疗能力,需要进行进一步的研究,包括进行更多的测试和实验。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d1c/11086890/81bce296e672/pone.0303373.g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d1c/11086890/7edce315d725/pone.0303373.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d1c/11086890/c185fa65c699/pone.0303373.g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d1c/11086890/81bce296e672/pone.0303373.g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d1c/11086890/7edce315d725/pone.0303373.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d1c/11086890/c185fa65c699/pone.0303373.g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d1c/11086890/81bce296e672/pone.0303373.g003.jpg

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PLoS One. 2024 Aug 15;19(8):e0309235. doi: 10.1371/journal.pone.0309235. eCollection 2024.

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