针对变形链球菌的新型抗菌肽GA-C16G2的开发和表征。

IF 4.8 2区医学 Q1 DENTISTRY, ORAL SURGERY & MEDICINE

Journal of dentistry Pub Date : 2025-06-25 DOI:10.1016/j.jdent.2025.105927

Yipeng Fu , Richard D. Cannon , Kai Chun Li , Manikandan Ekambaram , Paul R. Cooper , May L. Mei

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引用次数: 0

摘要

目的：研制一种治疗龋齿的变形链球菌（S. mutans）靶向肽并评价其抗菌效果。方法：将没食子酸（GA）附着于S. mutans靶向抗菌肽C16G2上，合成了一种新的肽GA-C16G2。采用高效液相色谱法测定多肽纯度和稳定性。采用圆二色（CD）光谱法评估GA-C16G2的二级结构，采用PrestoBlue法评估其细胞毒性。采用最小抑菌浓度（MIC）和最小杀菌浓度（MBC）测定其对口腔细菌的抑菌活性。时间杀伤和生物膜抑制试验进一步表征了肽的活性。采用透射电镜（TEM）和扫描电镜（SEM）对细菌形态和生物膜结构进行了分析。结果：合成的GA-C16G2纯度为95.02%，二级结构与母肽C16G2相似。GA-C16G2在人工唾液中表现出良好的稳定性，对人牙龈成纤维细胞具有较低的细胞毒性。GA-C16G2对S. mutans （MIC: 3.1 μM, MBC: 20.8 μM）表现出较强的抑菌活性，而对共生菌的抑菌作用较弱。时间杀伤实验证实了GA-C16G2的快速杀菌活性，在1分钟内使S. mutans的存活率降低了97.22%。GA-C16G2还能抑制变形链球菌生物膜的形成。TEM和SEM图像证实细菌和生物膜破坏。结论：本研究成功开发了一种具有生物相容性和稳定性的肽类药物GA-C16G2，该肽类药物对变形链球菌具有快速、有效的体外选择性抗菌活性。临床意义：GA-C16G2为有针对性地预防和治疗龋齿提供了一种新的治疗途径。

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Development and characterisation of a novel antimicrobial peptide GA-C16G2 targeting Streptococcus mutans

Objectives

This study aimed to develop a Streptococcus mutans (S. mutans)-targeted peptide for caries management and evaluate its antibacterial efficacy.

Methods

A novel peptide, GA-C16G2, was synthesised by attaching gallic acid (GA) onto an S. mutans-targeted antimicrobial peptide, C16G2. Peptide purity and stability were measured using high-performance liquid chromatography (HPLC). The secondary structure of GA-C16G2 was assessed using circular dichroism (CD) spectroscopy, and cytotoxicity was evaluated with the PrestoBlue assay. Antimicrobial activity against oral bacterial species was determined using minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays. Time-kill and biofilm inhibition assays further characterised the peptide’s activity. Bacterial morphology and biofilm structure were analysed by transmission electron microscopy (TEM) and scanning electron microscopy (SEM).

Results

GA-C16G2 was synthesised with 95.02 % purity, and its secondary structure closely resembled that of the parent peptide C16G2. GA-C16G2 exhibited good stability in artificial saliva and showed low cytotoxicity towards human gingival fibroblasts. GA-C16G2 demonstrated potent antimicrobial activity against S. mutans (MIC: 3.1 μM, MBC: 20.8 μM) while showing weaker effects against commensal bacterial species. A time-kill assay confirmed the rapid bactericidal activity of GA-C16G2, reducing S. mutans viability by 97.22 % within one minute. GA-C16G2 also inhibited S. mutans biofilm formation. TEM and SEM images confirmed bacterial and biofilm disruption.

Conclusion

This study demonstrates the successful development of a biocompatible and stable peptide, GA-C16G2, with rapid and potent selective in vitro antimicrobial activity against S. mutans.

Clinical significance

GA-C16G2 offers a novel therapeutic approach for targeted prevention and treatment of dental caries.

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来源期刊

Journal of dentistry 医学-牙科与口腔外科

CiteScore

7.30

自引率

11.40%

发文量

349

审稿时长

35 days

期刊介绍： The Journal of Dentistry has an open access mirror journal The Journal of Dentistry: X, sharing the same aims and scope, editorial team, submission system and rigorous peer review. The Journal of Dentistry is the leading international dental journal within the field of Restorative Dentistry. Placing an emphasis on publishing novel and high-quality research papers, the Journal aims to influence the practice of dentistry at clinician, research, industry and policy-maker level on an international basis. Topics covered include the management of dental disease, periodontology, endodontology, operative dentistry, fixed and removable prosthodontics, dental biomaterials science, long-term clinical trials including epidemiology and oral health, technology transfer of new scientific instrumentation or procedures, as well as clinically relevant oral biology and translational research. The Journal of Dentistry will publish original scientific research papers including short communications. It is also interested in publishing review articles and leaders in themed areas which will be linked to new scientific research. Conference proceedings are also welcome and expressions of interest should be communicated to the Editor.