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Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial...
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Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial Biofilm Control in Human Medicine II

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 12618

Special Issue Editors

Dr. Rossella Grande

E-Mail Website
Guest Editor
Department of Pharmacy, University “G. d'Annunzio” of Chieti-Pescara, 66100 Chieti, Italy
Interests: microbial biofilms; Helicobacter pylori; Lactobacillus reuteri; outer membrane vesicles; extracellular DNA; antimicrobial/antibiofilm activity; human microbiome; probiotics; prebiotics and symbiotics
Special Issues, Collections and Topics in MDPI journals
Dr. Simone Carradori

E-Mail Website
Guest Editor
Department of Pharmacy, University “G. d'Annunzio” of Chieti-Pescara, Chieti, Italy
Interests: chemical modification of natural compounds; medicinal chemistry; food chemistry; antioxidants; antimicrobials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Microbial biofilms are complex structures formed by cells embedded in an extracellular polymeric substance (EPS) matrix, a mixture of macromolecules such as exopolysaccharides, proteins, extracellular DNA, and, in some cases, outer membrane vesicles. EPS composition may differ with bacterial strains, culture conditions, and biofilm age. Biofilm formation ensures antibiotic tolerance and protection from the host immune system, making microbial biofilms difficult to eradicate. Biofilms are responsible for chronic infections, and biofilms developed by a wide range of microorganisms are considered a “virulence factor”. The variability in the composition of the biofilm matrix and in biofilm development as well as tolerance versus antimicrobials used in conventional therapies suggest the need for multitargeted or combinational therapies aimed at the eradication of biofilms. Antimicrobial tolerance is due to different mechanisms, such as the presence of an extracellular matrix that does not allow or slow the penetration of drugs as well as the presence of a metabolic dormancy adopted by many cells inside a biofilm. Furthermore, polymicrobial biofilms represent an additional problem that necessitates the use of antimicrobials that are efficacious versus all pathogens in biofilms restricting the success of species-specific biofilm-targeting strategies. New antimicrobials and anti-biofilm agents can be of synthetic or natural origin (the biological activity of natural extracts without a proper chemical characterization will not be considered).

Following the wide interest in the first edition of the Molecules Special Issue “Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial Biofilm Control in Human Medicine”, we are pleased to announce the second edition of this Special Issue. This Special Issue aims to collect the latest research focused on biofilm removal strategies/compounds as well as biofilm formation inhibition aimed at (a) the control of biofilm infections and (b) the eradication of a preformed biofilm and/or biofilm monitoring in medicine, food, industry, and natural environments. Submissions of original research articles, review articles, and communications are encouraged.

Dr. Rossella Grande
Dr. Simone Carradori
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Biofilm
  • Drug tolerance
  • Nanosystems
  • Biomaterials
  • Anti-biofilm activity
  • Natural compounds
  • Antimicrobial peptides
  • Anti-quorum sensing molecules
  • New antimicrobials
  • Bioactive agents
  • Drug delivery
  • Surfactants
  • Synthetic inhibitors
  • Food contamination
  • Medical device contamination

Published Papers (5 papers)

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Research

15 pages, 2385 KiB  
Article
Antimicrobial and Antibiofilm Photodynamic Action of Photosensitizing Nanoassemblies Based on Sulfobutylether-β-Cyclodextrin
by Domenico Franco, Roberto Zagami, Laura Maria De Plano, Nina Burduja, Salvatore Pietro Paolo Guglielmino, Luigi Monsù Scolaro and Antonino Mazzaglia
Molecules 2023, 28(6), 2493; https://doi.org/10.3390/molecules28062493 - 08 Mar 2023
Cited by 4 | Viewed by 1662
Abstract
Developing new broad-spectrum antimicrobial strategies, as alternatives to antibiotics and being able to efficiently inactivate pathogens without inducing resistance, is one of the main objectives in public health. Antimicrobial photodynamic therapy (aPDT), based on the light-induced production of reactive oxygen species from photosensitizers [...] Read more.
Developing new broad-spectrum antimicrobial strategies, as alternatives to antibiotics and being able to efficiently inactivate pathogens without inducing resistance, is one of the main objectives in public health. Antimicrobial photodynamic therapy (aPDT), based on the light-induced production of reactive oxygen species from photosensitizers (PS), is attracting growing interest in the context of infection treatment, also including biofilm destruction. Due to the limited photostability of free PS, delivery systems are increasingly needed in order to decrease PS photodegradation, thus improving the therapeutic efficacy, as well as to reduce collateral effects on unaffected tissues. In this study, we propose a photosensitizing nanosystem based on the cationic porphyrin 5,10,15,20-tetrakis (N-methyl- 4-pyridyl)-21H,23H-porphyrin (TMPyP), complexed with the commerical sulfobutylether-beta-cyclodextrin (CAPTISOL®), at a 1:50 molar ratio (CAPTISOL®/TMPyP)50_1. Nanoassemblies based on (CAPTISOL®/TMPyP)50_1 with photodynamic features exhibited photo-antimicrobial activity against Gram-negative and Gram-positive bacteria. Moreover, results from P. aeruginosa reveal that CAPTISOL® alone inhibits pyocyanin (PYO) production, also affecting bacterial biofilm formation. Finally, we obtained a synergistic effect of inhibition and destruction of P. aeruginosa biofilm by using the combination of CAPTISOL® and TMPyP. Full article
(This article belongs to the Special Issue Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial Biofilm Control in Human Medicine II)
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17 pages, 4467 KiB  
Article
Hydrophobic Chitosan Nanoparticles Loaded with Carvacrol against Pseudomonas aeruginosa Biofilms
by Ariadna Thalia Bernal-Mercado, Josué Juarez, Miguel Angel Valdez, Jesus Fernando Ayala-Zavala, Carmen Lizette Del-Toro-Sánchez and David Encinas-Basurto
Molecules 2022, 27(3), 699; https://doi.org/10.3390/molecules27030699 - 21 Jan 2022
Cited by 22 | Viewed by 2929
Abstract
Pseudomonas aeruginosa infections have become more challenging to treat and eradicate due to their ability to form biofilms. This study aimed to produce hydrophobic nanoparticles by grafting 11-carbon and three-carbon alkyl chains to a chitosan polymer as a platform to carry and deliver [...] Read more.
Pseudomonas aeruginosa infections have become more challenging to treat and eradicate due to their ability to form biofilms. This study aimed to produce hydrophobic nanoparticles by grafting 11-carbon and three-carbon alkyl chains to a chitosan polymer as a platform to carry and deliver carvacrol for improving its antibacterial and antibiofilm properties. Carvacrol–chitosan nanoparticles showed ζ potential values of 10.5–14.4 mV, a size of 140.3–166.6 nm, and an encapsulation efficiency of 25.1–68.8%. Hydrophobic nanoparticles reduced 46–53% of the biomass and viable cells (7–25%) within P. aeruginosa biofilms. Diffusion of nanoparticles through the bacterial biofilm showed a higher penetration of nanoparticles created with 11-carbon chain chitosan than those formulated with unmodified chitosan. The interaction of nanoparticles with a 50:50 w/w phospholipid mixture at the air–water interface was studied, and values suggested that viscoelasticity and fluidity properties were modified. The modified nanoparticles significantly reduced viable P. aeruginosa in biofilms (0.078–2.0 log CFU·cm−2) and swarming motility (40–60%). Furthermore, the formulated nanoparticles reduced the quorum sensing in Chromobacterium violaceum. This study revealed that modifying the chitosan polarity to synthesize more hydrophobic nanoparticles could be an effective treatment against P. aeruginosa biofilms to decrease its virulence and pathogenicity, mainly by increasing their ability to interact with the membrane phospholipids and penetrate preformed biofilms. Full article
(This article belongs to the Special Issue Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial Biofilm Control in Human Medicine II)
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14 pages, 2349 KiB  
Article
Ionic Silver and Electrical Treatment for Susceptibility and Disinfection of Escherichia coli Biofilm-Contaminated Titanium Surface
by Kritphudis Suttasattakrit, Arnon Khamkeaw, Chanchana Tangwongsan, Prasit Pavasant and Muenduen Phisalaphong
Molecules 2022, 27(1), 180; https://doi.org/10.3390/molecules27010180 - 28 Dec 2021
Cited by 2 | Viewed by 2216
Abstract
In this work, surface disinfection and biofilm susceptibility were investigated by applying ionic silver of 0.4–1.6 µg/mL and cathodic voltage-controlled electrical treatment of 1.8 V and a current of 30 mA to Escherichia coli (E. coli) ATCC 25922 biofilm-contaminated titanium substrates. [...] Read more.
In this work, surface disinfection and biofilm susceptibility were investigated by applying ionic silver of 0.4–1.6 µg/mL and cathodic voltage-controlled electrical treatment of 1.8 V and a current of 30 mA to Escherichia coli (E. coli) ATCC 25922 biofilm-contaminated titanium substrates. Herein, it is evident that the treatment exhibited the potential use to enhance the susceptibility of bacterial biofilms for surface disinfection. In vitro studies have demonstrated that the ionic silver treatment of 60 min significantly increased the logarithmic reduction (LR) of bacterial populations on disinfectant-treated substrates and the electrical treatment enhanced the silver susceptibility of E. coli biofilms. The LR values after the ionic silver treatments and the electric-enhanced silver treatments were in the ranges of 1.94–2.25 and 2.10–2.73, respectively. The treatment was also associated with morphological changes in silver-treated E. coli cells and biofilm-contaminated titanium surfaces. Nevertheless, the treatments showed no cytotoxic effects on the L929 mouse skin fibroblast cell line and only a slight decrease in pH was observed during the electrical polarization of titanium substrate. Full article
(This article belongs to the Special Issue Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial Biofilm Control in Human Medicine II)
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20 pages, 6020 KiB  
Article
In Silico Screening and In Vitro Assessment of Natural Products with Anti-Virulence Activity against Helicobacter pylori
by Maciej Spiegel, Paweł Krzyżek, Ewa Dworniczek, Ryszard Adamski and Zbigniew Sroka
Molecules 2022, 27(1), 20; https://doi.org/10.3390/molecules27010020 - 21 Dec 2021
Cited by 7 | Viewed by 3101
Abstract
Helicobacter pylori is one of the most frequent human pathogens and a leading etiological agent of various gastric diseases. As stringent response, coordinated by a SpoT protein, seems to be crucial for the survivability of H. pylori, the main goal of this [...] Read more.
Helicobacter pylori is one of the most frequent human pathogens and a leading etiological agent of various gastric diseases. As stringent response, coordinated by a SpoT protein, seems to be crucial for the survivability of H. pylori, the main goal of this article was to use in silico computational studies to find phytochemical compounds capable of binding to the active site of SpoT from H. pylori and confirm the ability of the most active candidates to interfere with the virulence of this bacterium through in vitro experiments. From 791 natural substances submitted for the virtual screening procedure, 10 were chosen and followed for further in vitro examinations. Among these, dioscin showed the most interesting parameters (the lowest MIC, the highest anti-biofilm activity in static conditions, and a relatively low stimulation of morphological transition into coccoids). Therefore, in the last part, we extended the research with a number of further experiments and observed the ability of dioscin to significantly reduce the formation of H. pylori biofilm under Bioflux-generated flow conditions and its capacity for additive enhancement of the antibacterial activity of all three commonly used antibiotics (clarithromycin, metronidazole, and levofloxacin). Based on these results, we suggest that dioscin may be an interesting candidate for new therapies targeting H. pylori survivability and virulence. Full article
(This article belongs to the Special Issue Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial Biofilm Control in Human Medicine II)
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14 pages, 5305 KiB  
Article
Voice Prosthesis Coated with Sustained Release Varnish Containing Clotrimazole Shows Long-Term Protection against Candida albicans: An In Vitro Study
by Ronit Vogt Sionov, Irith Gati, David Kirmayer, Michael Friedman, Doron Steinberg and Menachem Gross
Molecules 2021, 26(17), 5395; https://doi.org/10.3390/molecules26175395 - 05 Sep 2021
Cited by 2 | Viewed by 1765
Abstract
Fungal biofilm formation on voice prosthesis (VP) is a major health problem that requires repeated replacement of the prosthesis. Candida albicans is one of the pathogens that frequently inhabits the VP. We proposed that coating VPs with sustained-release varnish (SRV) containing clotrimazole (CTZ) [...] Read more.
Fungal biofilm formation on voice prosthesis (VP) is a major health problem that requires repeated replacement of the prosthesis. Candida albicans is one of the pathogens that frequently inhabits the VP. We proposed that coating VPs with sustained-release varnish (SRV) containing clotrimazole (CTZ) might prevent fungal biofilm formation. The long-term antifungal activities of SRV-CTZ- versus SRV-placebo-coated VPs was tested daily by measuring the inhibition zone of C. albicans seeded on agar plates or by measuring the fungal viability of C. albicans in suspension. The extent of biofilm formation on coated VPs was analyzed by confocal microscopy and scanning electron microscopy. We observed that SRV-CTZ-coated VPs formed a significant bacterial inhibition zone around the VPs and prevented the growth of C. albicans in suspension during the entire testing period of 60 days. Fungal biofilms were formed on placebo-coated VPs, while no significant biofilms were observed on SRV-CTZ-coated VPs. HPLC analysis shows that CTZ is continuously released during the whole test period of 60 days at a concentration above the minimal fungistatic concentration. In conclusion, coating VPs with an SRV-CTZ film is a potential effective method for prevention of fungal infections and biofilm formation on VPs. Full article
(This article belongs to the Special Issue Novel Biologically Active Molecules, Biomaterials and Nanoparticles for the Microbial Biofilm Control in Human Medicine II)
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