Exploring the antimicrobial potential of the articaine derivative in oral infections.

IF 3.7 2区 医学 Q2 MICROBIOLOGY
Journal of Oral Microbiology Pub Date : 2025-05-11 eCollection Date: 2025-01-01 DOI:10.1080/20002297.2025.2502455
Yongzhen Tan, Yihang Hao, Yihang Fu, Shilong Hu, Xi Yang, Yaling Tang, Bowen Ke, Xinhua Liang
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引用次数: 0

Abstract

Objective: Postoperative infection is one of the most common complications in dental procedures. During local anesthesia in dental treatments, the risk of postoperative infections increases if the oral mucosa is infected, the anesthesia injection site is inadequately disinfected, or the injection needle and anesthetic drugs are contaminated. Thus, developing new oral local anesthetics that offer superior anesthesia, enhanced safety, and antimicrobial properties could greatly enhance their clinical value.

Methods: The anesthetic effects and antibacterial properties of articaine derivatives were screened using membrane chromatography techniques, animal experiments, and cellular molecular assays. Safety assessments were conducted on the selected target compounds. Additionally, the antibacterial mechanisms of the compounds were investigated through molecular dynamics simulations and cryo-electron microscopy.

Results: Through the screening of articaine derivatives, a novel local anesthetic, AT-15, was identified, which combines effective anesthetic properties with antibacterial activity. This compound exhibits strong pharmacological activity and high safety. Its antibacterial effect is believed to result from the disruption of bacterial cell membranes and the inhibition of topoisomerase, an enzyme essential for bacterial DNA synthesis.

Conclusion: AT-15 discovered in this study is a promising candidate for further development in clinical settings.

探索阿替卡因衍生物在口腔感染中的抗菌潜力。
目的:术后感染是口腔手术中最常见的并发症之一。在口腔局部麻醉治疗过程中,口腔黏膜感染、麻醉注射部位消毒不充分、注射针头和麻醉药物被污染等因素会增加术后感染的风险。因此,开发新的口服局部麻醉剂,提供更好的麻醉,提高安全性和抗菌性能,可以大大提高其临床价值。方法:采用膜层析、动物实验和细胞分子分析等方法对阿替卡因衍生物的麻醉作用和抗菌性能进行筛选。对选定的目标化合物进行了安全性评估。此外,通过分子动力学模拟和低温电子显微镜研究了化合物的抗菌机制。结果:通过对阿替卡因衍生物的筛选,鉴定出一种新型的局部麻醉剂AT-15,它既具有有效的麻醉性能,又具有抗菌活性。该化合物具有很强的药理活性和较高的安全性。它的抗菌作用被认为是由于破坏细菌细胞膜和抑制拓扑异构酶,一种细菌DNA合成所必需的酶。结论:本研究发现的AT-15具有进一步临床开发的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
8.00
自引率
4.40%
发文量
52
审稿时长
12 weeks
期刊介绍: As the first Open Access journal in its field, the Journal of Oral Microbiology aims to be an influential source of knowledge on the aetiological agents behind oral infectious diseases. The journal is an international forum for original research on all aspects of ''oral health''. Articles which seek to understand ''oral health'' through exploration of the pathogenesis, virulence, host-parasite interactions, and immunology of oral infections are of particular interest. However, the journal also welcomes work that addresses the global agenda of oral infectious diseases and articles that present new strategies for treatment and prevention or improvements to existing strategies. Topics: ''oral health'', microbiome, genomics, host-pathogen interactions, oral infections, aetiologic agents, pathogenesis, molecular microbiology systemic diseases, ecology/environmental microbiology, treatment, diagnostics, epidemiology, basic oral microbiology, and taxonomy/systematics. Article types: original articles, notes, review articles, mini-reviews and commentaries
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