Biofilm Inhibitors of Marine Origin

A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (30 November 2019) | Viewed by 9020

Special Issue Editor


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Guest Editor
Department of Chemistry, University of Alabama at Birmingham, Birmingham, AL, USA
Interests: organic/medicinal chemistry; drug discovery and development; anti-cancer and anti-infective agents; synthesis of marine natural products and their analogs; structure based drug design; SAR studies and lead optimization
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Special Issue Information

Dear Colleagues,

Marine natural products have recently received increased attention as a source of lead compounds for drug discovery. Many of these compounds are anti-biofilm agents that may play a role in the field of antibacterial drug discovery. These compounds are identified based on bioactivity screens of marine natural products and their mode of action is generally unknown at the time of discovery. Discerning their mode of action is a critical step in their further development as potential drugs. This Special Issue focuses on such marine derived natural products or their analogs that are inhibitors or disruptors of biofilm. The coverage includes the biological activities of the lead compounds, discovery of their mode of action and their potential use in drug discovery. We aim to publish original research articles and review articles in this Special Issue.

Prof. Dr. Sadanandan E. Velu
Guest Editor

Manuscript Submission Information

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Keywords

  • Marine alkaloid
  • Analogs
  • Synthesis
  • Antibiofilm
  • Antibacterial
  • Antifungal
  • Biofilm Inhibitor
  • Biofilm disruptor
  • Enzyme inhibitor

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Published Papers (2 papers)

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Research

15 pages, 5183 KiB  
Article
Characterization and Antibiofilm Activity of Mannitol–Chitosan-Blended Paste for Local Antibiotic Delivery System
by Leslie R. Pace, Zoe L. Harrison, Madison N. Brown, Warren O. Haggard and J. Amber Jennings
Mar. Drugs 2019, 17(9), 517; https://doi.org/10.3390/md17090517 - 2 Sep 2019
Cited by 14 | Viewed by 4089
Abstract
Mannitol, a polyalcohol bacterial metabolite, has been shown to activate dormant persister cells within bacterial biofilm. This study sought to evaluate an injectable blend of mannitol, chitosan, and polyethylene glycol for delivery of antibiotics and mannitol for eradication of Staphylococcal biofilm. Mannitol blends [...] Read more.
Mannitol, a polyalcohol bacterial metabolite, has been shown to activate dormant persister cells within bacterial biofilm. This study sought to evaluate an injectable blend of mannitol, chitosan, and polyethylene glycol for delivery of antibiotics and mannitol for eradication of Staphylococcal biofilm. Mannitol blends were injectable and had decreased dissociation and degradation in the enzyme lysozyme compared to blends without mannitol. Vancomycin and amikacin eluted in a burst response, with active concentrations extended to seven days compared to five days for blends without mannitol. Mannitol eluted from the paste in a burst the first day and continued through Day 4. Eluates from the mannitol pastes with and without antibiotics decreased viability of established S. aureus biofilm by up to 95.5% compared to blends without mannitol, which only decreased biofilm when loaded with antibiotics. Cytocompatibility tests indicated no adverse effects on viability of fibroblasts. In vivo evaluation of inflammatory response revealed mannitol blends scored within the 2–4 range at Week 1 (2.6 ± 1.1) and at Week 4 (3.0 ± 0.8), indicative of moderate inflammation and comparable to non-mannitol pastes (p = 0.065). Clinically, this paste could be loaded with clinician-selected antibiotics and used as an adjunctive therapy for musculoskeletal infection prevention and treatment. Full article
(This article belongs to the Special Issue Biofilm Inhibitors of Marine Origin)
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19 pages, 2933 KiB  
Article
Rhamnose Binding Protein as an Anti-Bacterial Agent—Targeting Biofilm of Pseudomonas aeruginosa
by Tse-Kai Fu, Sim-Kun Ng, Yi-En Chen, Yuan-Chuan Lee, Fruzsina Demeter, Mihály Herczeg, Anikó Borbás, Cheng-Hsun Chiu, Chung-Yu Lan, Chyi-Liang Chen and Margaret Dah-Tsyr Chang
Mar. Drugs 2019, 17(6), 355; https://doi.org/10.3390/md17060355 - 14 Jun 2019
Cited by 13 | Viewed by 4508
Abstract
More than 80% of infectious bacteria form biofilm, which is a bacterial cell community surrounded by secreted polysaccharides, proteins and glycolipids. Such bacterial superstructure increases resistance to antimicrobials and host defenses. Thus, to control these biofilm-forming pathogenic bacteria requires antimicrobial agents with novel [...] Read more.
More than 80% of infectious bacteria form biofilm, which is a bacterial cell community surrounded by secreted polysaccharides, proteins and glycolipids. Such bacterial superstructure increases resistance to antimicrobials and host defenses. Thus, to control these biofilm-forming pathogenic bacteria requires antimicrobial agents with novel mechanisms or properties. Pseudomonas aeruginosa, a Gram-negative opportunistic nosocomial pathogen, is a model strain to study biofilm development and correlation between biofilm formation and infection. In this study, a recombinant hemolymph plasma lectin (rHPLOE) cloned from Taiwanese Tachypleus tridentatus was expressed in an Escherichia coli system. This rHPLOE was shown to have the following properties: (1) Binding to P. aeruginosa PA14 biofilm through a unique molecular interaction with rhamnose-containing moieties on bacteria, leading to reduction of extracellular di-rhamnolipid (a biofilm regulator); (2) decreasing downstream quorum sensing factors, and inhibiting biofilm formation; (3) dispersing the mature biofilm of P. aeruginosa PA14 to improve the efficacies of antibiotics; (4) reducing P. aeruginosa PA14 cytotoxicity to human lung epithelial cells in vitro and (5) inhibiting P. aeruginosa PA14 infection of zebrafish embryos in vivo. Taken together, rHPLOE serves as an anti-biofilm agent with a novel mechanism of recognizing rhamnose moieties in lipopolysaccharides, di-rhamnolipid and structural polysaccharides (Psl) in biofilms. Thus rHPLOE links glycan-recognition to novel anti-biofilm strategies against pathogenic bacteria. Full article
(This article belongs to the Special Issue Biofilm Inhibitors of Marine Origin)
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