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基于新型D-π-A的香豆素衍生荧光诊疗探针及其广谱抗菌活性

New D-π-A-Based Coumarin- Derived Fluorescent Theranostic Probes With Broad-Spectrum Antimicrobial Activity.

作者信息

Rai Himanshu, Tiwari Atul Kumar, Nikhil Aishwarya, Tiwari Ankit, Bharti Prahalad Singh, Maury Suresh Kumar, Gupta Munesh Kumar, Singh Sundaram, Kumar Saroj, Modi Gyan

机构信息

Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (BHU), Varanasi, India.

Department of Chemistry, Indian Institute of Technology (BHU), Varanasi, India.

出版信息

Arch Pharm (Weinheim). 2025 Jul;358(7):e70032. doi: 10.1002/ardp.70032.

Abstract

Understanding how multidrug-resistant (MDR) bacteria and fungi defy the existing antimicrobial agents requires innovative tools and techniques for real-time, in situ exploration of bacterial responses to antibiotics. Fluorescence-tagged antibiotics or dyes with inherent antimicrobial activity can provide a profound understanding of the molecular biology underlying antibiotic action and resistance mechanisms. Cutting-edge research highlights the pursuit of benzo-α-pyrone (coumarin) derivatives due to their excellent pharmacokinetics, diverse pharmacological activities, and innovative fluorescence molecular probes. In this study, donor-π-acceptor-based coumarin dyes were designed and evaluated for antimicrobial efficacy against fungal strains (Candida albicans), Gram-negative pathogens (Escherichia coli), and Gram-positive bacteria (Staphylococcus aureus). I-6 exhibited notable antimicrobial activity against S. aureus and C. albicans compared with E. coli. Conversely, I-9, a congener of I-6, showed a comparable affinity for S. aureus but found poor activity against the remaining tested strains. Mechanistic investigative studies unveiled that the inhibitory efficacy of I-6 can be attributed to its capacity to generate high reactive oxygen species (ROS) formation. Despite the evident antimicrobial potential of I-6 in the data, our future prospects, including real-time visualization to study physiological processes like uptake, distribution, and mechanism of action through fluorescence-based imaging modalities, could enhance the applicability of these probes.

摘要

了解多重耐药(MDR)细菌和真菌如何对抗现有的抗菌药物,需要创新的工具和技术来实时、原位探索细菌对抗生素的反应。荧光标记抗生素或具有固有抗菌活性的染料,可以深入了解抗生素作用和耐药机制背后的分子生物学。前沿研究强调了对苯并-α-吡喃酮(香豆素)衍生物的追求,因为它们具有出色的药代动力学、多样的药理活性以及创新的荧光分子探针。在本研究中,设计并评估了基于供体-π-受体的香豆素染料对真菌菌株(白色念珠菌)、革兰氏阴性病原体(大肠杆菌)和革兰氏阳性细菌(金黄色葡萄球菌)的抗菌效果。与大肠杆菌相比,I-6对金黄色葡萄球菌和白色念珠菌表现出显著的抗菌活性。相反,I-6的同系物I-9对金黄色葡萄球菌表现出相当的亲和力,但对其余测试菌株的活性较差。机理研究表明,I-6的抑制效果可归因于其产生高活性氧(ROS)形成的能力。尽管数据中I-6具有明显的抗菌潜力,但我们的未来前景,包括通过基于荧光的成像方式进行实时可视化,以研究诸如摄取、分布和作用机制等生理过程,可能会提高这些探针的适用性。

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