Synthetic non-toxic anti-biofilm agents as a strategy in combating bacterial resistance

Hassan, Rasha Mohamed; Abd El-Maksoud, Mohamed Samir; Ghannam, Iman Ahmed Youssef; El-Azzouny, Aida Abdel- Sattar; Aboul-Enein, Mohamed Nabil

doi:10.1016/j.ejmech.2023.115867

Cited by 7 publications

(3 citation statements)

References 155 publications

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“…Considering the resistance of microbial communities organized in biofilms to conventional antibiotic treatment, which makes biofilm-related infections challenging to treat, new anti-biofilm options are urgently needed [12][13][14][15][16][17][18]. The main aim of this in vitro study was to evaluate the anti-staphylococcal biofilm potential of a commercial formulation constituted by a mixture of citrus polyphenols encapsulated in liposomes.…”

Section: Discussionmentioning

confidence: 99%

“…In addition, biofilms can contribute to the spreading of drug resistance, thus constituting a serious threat for human health [12]. Therefore, many efforts have been made in developing novel anti-biofilm strategies, and some options, including quorum-sensing (QS) inhibitors, bacteriophages, and natural molecules with antimicrobial and anti-biofilm activities, have been proposed [13,[15][16][17]. In addition, particular emphasis has been placed on the development of innovative delivery systems for antimicrobial encapsulation, which can cross the biofilm matrix, releasing their cargo directly on biofilm-embedded cells [18].…”

Section: Introductionmentioning

confidence: 99%

“…Since both polyphenols and liposomes are now believed to be potential innovative anti-biofilm options [13,[15][16][17][18]21], in this study we spotlight the anti-biofilm activity of the liposomal polyphenol formulation, focusing on its ability to affect biofilm formation and eradicate mature biofilms. The anti-biofilm activity of the liposome-based product was tested against S. aureus and S. epidermidis, which are the most common agents of ocular infections and known to be biofilm-proficient [4][5][6].…”

Section: Introductionmentioning

confidence: 99%

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Anti-Staphylococcal Biofilm Effects of a Liposome-Based Formulation Containing Citrus Polyphenols

Mazzantini,

Massimino,

Calvigioni

et al. 2024

Antibiotics

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Biofilms are surface-associated microbial communities embedded in a matrix that is almost impenetrable to antibiotics, thus constituting a critical health threat. Biofilm formation on the cornea or ocular devices can lead to serious and difficult-to-treat infections. Nowadays, natural molecules with antimicrobial activity and liposome-based delivery systems are proposed as anti-biofilm candidates. In this study, the anti-biofilm activity of a formulation containing citrus polyphenols encapsulated in liposomes was evaluated against Staphylococcus aureus and Staphylococcus epidermidis, the most common agents in ocular infections. The formulation activity against planktonic staphylococci was tested by broth microdilution and sub-inhibitory concentrations were used to evaluate the effect on biofilm formation using the crystal violet (CV) assay. The eradicating effect of the preparation on mature biofilms was investigated by the CV assay, plate count, and confocal laser scanning microscopy. The product was bactericidal against staphylococci at a dilution of 1:2 or 1:4 and able to reduce biofilm formation even if diluted at 1:64. The formulation also had the ability to reduce the biomass of mature biofilms without affecting the number of cells, suggesting activity on the extracellular matrix. Overall, our results support the application of the used liposome-encapsulated polyphenols as an anti-biofilm strategy to counter biofilm-associated ocular infections.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Anti-Staphylococcal Biofilm Effects of a Liposome-Based Formulation Containing Citrus Polyphenols

Mazzantini,

Massimino,

Calvigioni

et al. 2024

Antibiotics

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Engineering the novel azobenzene‐based molecular photoswitches for suppressing bacterial infection through dynamic regulation of biofilm formation

Zhang,

Yang,

Feng

et al. 2024

Pest Management Science

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BACKGROUNDBacterial biofilm is a strong fortress for bacteria to resist harsh external environments, which can enhance their tolerance and exacerbate the drug/pesticide resistance risk. Currently, photopharmacology provides an advanced approach via precise spatiotemporal control for regulating biological activities by light‐controlling the molecular configurations, thereby having enormous potential in the development of drug/pesticides.RESULTSTo further expand the photopharmacology application for discovering new antibiofilm agents, we prepared a series of light‐controlled azo‐active molecules and explored their photo isomerization, fatigue resistance, and anti‐biofilm performance. Furthermore, their mechanisms of inhibiting biofilm formation were systematically investigated. Overall, designed azo‐derivative A11 featured excellent anti‐Xoo activity with an half‐maximal effective concentration (EC50) value of 5.45 μg mL−1, and the EC50 value could be further elevated to 2.19 μg mL−1 after ultraviolet irradiation (converted as cis‐configuration). The photo‐switching behavior showed that A11 had outstanding anti‐fatigue properties. An in‐depth analysis of the action mechanism showed that A11 could effectively inhibit biofilm formation and the expression of relevant virulence factors. This performance could be dynamically regulated via loading with private light‐switch property.CONCLUSIONIn this work, designed light‐controlled azo molecules provide a new model for resisting bacterial infection via dynamic regulation of bacterial biofilm formation. © 2024 Society of Chemical Industry.

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Design and synthesis of new quinazolinone derivatives: investigation of antimicrobial and biofilm inhibition effects

Hassan,

Yehia,

El-Behairy

et al. 2024

Mol Divers

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New quinazolin-4-ones 9–32 were synthesized in an attempt to overcome the life-threatening antibiotic resistance phenomenon. The antimicrobial screening revealed that compounds 9, 15, 16, 18, 19, 20 and 29 are the most broad spectrum antimicrobial agents in this study with safe profile on human cell lines. Additionally, compounds 19 and 20 inhibited biofilm formation in Pseudomonas aeruginosa, which is regulated by quorum sensing system, at sub-minimum inhibitory concentrations (sub-MICs) with IC50 values 3.55 and 6.86 µM, respectively. By assessing other pseudomonal virulence factors suppression, it was found that compound 20 decreased cell surface hydrophobicity compromising bacterial cells adhesion, while both compounds 19 and 20 curtailed the exopolysaccharide production which constitutes the major component of the matrix binding biofilm components together. Also, at sub-MICs Pseudomonas cells twitching motility was impeded by compounds 19 and 20, a trait which augments the cells pathogenicity and invasion potential. Molecular docking study was performed to further evaluate the binding mode of candidates 19 and 20 as inhibitors of P. aeruginosa quorum sensing transcriptional regulator PqsR. The achieved results demonstrate that both compounds bear promising potential for discovering new anti-biofilm and quorum quenching agents against Pseudomonas aeruginosa without triggering resistance mechanisms as the normal bacterial life cycle is not disturbed. Graphical abstract New 4-quinazolinones were synthesized and screened for their antimicrobial activity. Compounds 19 and 20 inhibited biofilm formation in Pseudomonas aeruginosa at sub- minimum inhibitory concentrations. Also, they decreased other virulence factors at low concentrations without affecting bacterial growth bacteria indicating their promising profile as anti-virulence agents that cause less bacterial resistance than the conventional antibiotics.

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Synthetic non-toxic anti-biofilm agents as a strategy in combating bacterial resistance

Cited by 7 publications

References 155 publications

Anti-Staphylococcal Biofilm Effects of a Liposome-Based Formulation Containing Citrus Polyphenols

Anti-Staphylococcal Biofilm Effects of a Liposome-Based Formulation Containing Citrus Polyphenols

Engineering the novel azobenzene‐based molecular photoswitches for suppressing bacterial infection through dynamic regulation of biofilm formation

Design and synthesis of new quinazolinone derivatives: investigation of antimicrobial and biofilm inhibition effects

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