Epsilon-poly-<scp>l</scp>-lysine conjugated erythromycin for enhanced antibiotic therapy

Yu, Jie; Cen, Danwei; Chen, Yongcheng; Zhao, Hailan; Xu, Mingang; Wu, Sulan; Wang, Shuo; Jin, Qiao; Shen, Ting

doi:10.1039/d3ra03168c

Cited by 3 publications

(4 citation statements)

References 36 publications

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“…ε-PL and nisin A have synergistic antibacterial effects on gram positive foodborne pathogens such as Bacillus cereus and Listeria monocytogenes [34]. Additionally, ε-PL coupled with erythromycin demonstrated relatively strong antibacterial activity against Staphylococcus aureus and Enterococcus faecalis, compared with the ε-PL alone [35]. In this study, an innovative combination of ε-PL, FP and domiphen was developed and its superior antibacterial effect was proved.…”

Section: Discussionmentioning

confidence: 94%

Efficacy of a mouthwash containing ε-poly-L-lysine, funme peptides and domiphen in reducing halitosis and supragingival plaque: a randomized clinical trial

Shen,

Liu,

Huang

et al. 2024

BMC Oral Health

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Objective To evaluate the antibacterial effectiveness of a combination of ε-poly-L-lysine (ε-PL), funme peptide (FP) as well as domiphen against oral pathogens, and assess the efficacy of a BOP® mouthwash supplemented with this combination in reducing halitosis and supragingival plaque in a clinical trial. Materials and methods The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the compound against Fusobacterium nucleatum, Porphyromonas gingivalis, Streptococcus mutans, and Aggregatibacter actinomycetemcomitans were determined by the gradient dilution method. Subsequently, the CCK-8 assay was used to detect the toxicity of mouthwash on human gingival fibroblastst, and the effectiveness in reducing halitosis and supragingival plaque of the mouthwash supplemented with the combination was analyzed by a randomized, double-blind, parallel-controlled clinical trial. Results The combination exhibited significant inhibitory effects on tested oral pathogens with the MIC < 1.56% (v/v) and the MBC < 3.13% (v/v), and the mouthwash containing this combination did not inhibit the viability of human gingival fibroblasts at the test concentrations. The clinical trial showed that the test group displayed notably lower volatile sulfur compounds (VSCs) at 0, 10, 24 h, and 7 d post-mouthwash (P < 0.05), compared with the baseline. After 7 days, the VSC levels of the and control groups were reduced by 50.27% and 32.12%, respectively, and notably cutting severe halitosis by 57.03% in the test group. Additionally, the Plaque Index (PLI) of the test and control group decreased by 54.55% and 8.38%, respectively, and there was a significant difference in PLI between the two groups after 7 days (P < 0.01). Conclusions The combination of ε-PL, FP and domiphen demonstrated potent inhibitory and bactericidal effects against the tested oral pathogens, and the newly formulated mouthwash added with the combination exhibited anti-dental plaque and anti-halitosis properties in a clinical trial and was safe. Trial registration The randomized controlled clinical trial was registered on Chinese Clinical Trial Registry (No. ChiCTR2300073816, Date: 21/07/2023).

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Section: Discussionmentioning

confidence: 94%

Efficacy of a mouthwash containing ε-poly-L-lysine, funme peptides and domiphen in reducing halitosis and supragingival plaque: a randomized clinical trial

Shen,

Liu,

Huang

et al. 2024

BMC Oral Health

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“…Expanding beyond β-lactam antibiotics, Yu et al demonstrated an enhanced antimicrobial ability of EPL-conjugated erythromycin compared to erythromycin alone. 35 This provides evidence to extend the conjugation strategy to more kinds of antibiotics, especially those with a poor or diminishing efficiency. However, with the limitation of this work, further investigation is needed to assess their properties against MDR pathogens and in vivo.…”

Section: Prospects For the Epl−β-lactam Antibiotic Covalent Conjugatesmentioning

confidence: 99%

“…33 In spite of these, limited research has explored the combinations and conjugations of EPL with other antibiotics. 34,35 Among conventional antibiotics, β-lactam antibiotics remain a preferred choice for empiric use due to a low required concentrations. 4 However, their great potential to induce drug resistance and poor synergy with several types of peptides constrain their broader utility.…”

Section: Introductionmentioning

confidence: 99%

“…Similarly, Prasad et al observed improved antibiofilm activity and enhanced antimicrobial potency against MDR pathogens when EPL was conjugated with Au nanoparticles and octadecanethiol, potentially attributed to their altered transmembrane pathways . In spite of these, limited research has explored the combinations and conjugations of EPL with other antibiotics. , Among conventional antibiotics, β-lactam antibiotics remain a preferred choice for empiric use due to a low required concentrations . However, their great potential to induce drug resistance and poor synergy with several types of peptides constrain their broader utility. , Since the interaction between β-lactam antibiotics and penicillin-binding proteins (PBPs) occurs in the periplasmic space, enhancing membrane permeability becomes crucial for this class of antibiotic.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Synergistic Antimicrobial Efficacy of Covalent Conjugates Composed of Epsilon-Poly-l-lysine and Beta-Lactam Antibiotics

Chen,

Qian,

Wan

et al. 2024

ACS Appl. Bio Mater.

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The increasing severity of problems posed by drugresistant pathogens has compelled researchers to explore innovative approaches for infection prevention. Among these strategies, conjugation methods stand out for their convenience and high efficacy. In this study, multiple covalent conjugates were synthesized, incorporating the natural antimicrobial peptide epsilon-poly-L-lysine (EPL) and two commonly used β-lactam antibiotics: penicillin G or ampicillin. Enhanced antimicrobial efficacy against typical Gram-negative pathogens, along with faster kill kinetics compared to combination approaches, was demonstrated by the EPL−Ampicillin covalent conjugates. Their antimicrobial mechanism was also substantiated through SEM and fluorescence tests in this work, confirming the inheritance of membrane-disrupting properties from EPL. Furthermore, the excellent biocompatibility of the raw materials was reserved in the covalent conjugates. This simplified conjugation method holds promise for the development of infection therapeutic drugs and potentially restores the sensitivity of conventional antibiotics to drug-resistant pathogens by introducing membrane-disrupting mechanisms.

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Epsilon-poly-l-lysine inhibits biofilm formation and aids dispersion in Acinetobacter baumannii

Saha,

Shinde,

Jadhav

et al. 2024

Medicine in Microecology

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Epsilon-poly-l-lysine conjugated erythromycin for enhanced antibiotic therapy

Abstract: Erythromycin was conjugated to ε-poly-l-lysine (EPL) for enhanced antibiotic therapy while not bringing hemolysis and cytotoxicity.

Cited by 3 publications

References 36 publications

Efficacy of a mouthwash containing ε-poly-L-lysine, funme peptides and domiphen in reducing halitosis and supragingival plaque: a randomized clinical trial

Efficacy of a mouthwash containing ε-poly-L-lysine, funme peptides and domiphen in reducing halitosis and supragingival plaque: a randomized clinical trial

Synthesis and Synergistic Antimicrobial Efficacy of Covalent Conjugates Composed of Epsilon-Poly-l-lysine and Beta-Lactam Antibiotics

Epsilon-poly-l-lysine inhibits biofilm formation and aids dispersion in Acinetobacter baumannii

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