Abstract
A worldwide public health problem has resulted from the alarming spread of multi-drug resistant bacteria combined with the frequent occurrence of biofilm-type infections, creating a growing need for new therapies. In this study, we have demonstrated that novel cyclic lipopeptides, such as 1, cyclo-[D-Ala-(12-guanidinododecanoyl)Thr-D-Val-Val-DaThr-D-Asn], and 2, cyclo-[D-Ala-(12-guanidinododecanoyl)Dap-D-Val-Val-D-aThr-D-Asn], derived from the fusaricidin/ LI-F natural products efficiently inhibit the growth of Staphylococcus aureus biofilm in vitro at their minimum inhibitory concentrations (MICs). Complete S. aureus biofilm eradication was observed at 3 x MIC for 1 and 4 x MIC for 2. Promising in vivo activity was demonstrated by the ability of depsipeptide 1 to reduce the proliferation of methicillinresistant S. aureus US300 in a porcine wound model. Due to their unique structure and potent antibacterial and antibiofilm activities, cyclic lipopeptides that belong to the fusaricidin/LI-F family of antibiotics represent particularly attractive lead structures for the development of new antibacterial agents capable of treating complicated biofilm-associated infections.
Keywords: Antibiotics, biofilm, cyclic lipopeptides, eradication, fusaricidins/LI-Fs, MRSA, porcine model, wound.
Protein & Peptide Letters
Title:In Vitro and In Vivo Activities of Novel Cyclic Lipopeptides Against Staphylococcal Biofilms
Volume: 21 Issue: 4
Author(s): Nina Bionda, Irena Pastar, Stephen C. Davis and Predrag Cudic
Affiliation:
Keywords: Antibiotics, biofilm, cyclic lipopeptides, eradication, fusaricidins/LI-Fs, MRSA, porcine model, wound.
Abstract: A worldwide public health problem has resulted from the alarming spread of multi-drug resistant bacteria combined with the frequent occurrence of biofilm-type infections, creating a growing need for new therapies. In this study, we have demonstrated that novel cyclic lipopeptides, such as 1, cyclo-[D-Ala-(12-guanidinododecanoyl)Thr-D-Val-Val-DaThr-D-Asn], and 2, cyclo-[D-Ala-(12-guanidinododecanoyl)Dap-D-Val-Val-D-aThr-D-Asn], derived from the fusaricidin/ LI-F natural products efficiently inhibit the growth of Staphylococcus aureus biofilm in vitro at their minimum inhibitory concentrations (MICs). Complete S. aureus biofilm eradication was observed at 3 x MIC for 1 and 4 x MIC for 2. Promising in vivo activity was demonstrated by the ability of depsipeptide 1 to reduce the proliferation of methicillinresistant S. aureus US300 in a porcine wound model. Due to their unique structure and potent antibacterial and antibiofilm activities, cyclic lipopeptides that belong to the fusaricidin/LI-F family of antibiotics represent particularly attractive lead structures for the development of new antibacterial agents capable of treating complicated biofilm-associated infections.
Export Options
About this article
Cite this article as:
Bionda Nina, Pastar Irena, Davis C. Stephen and Cudic Predrag, In Vitro and In Vivo Activities of Novel Cyclic Lipopeptides Against Staphylococcal Biofilms, Protein & Peptide Letters 2014; 21 (4) . https://dx.doi.org/10.2174/09298665113206660101
DOI https://dx.doi.org/10.2174/09298665113206660101 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Drugs in Pediatric Ischemic Stroke
Current Drug Targets Drug-Induced Thromboembolic Events in Patients with Malignancy
Cardiovascular & Hematological Disorders-Drug Targets Uveitis in Rheumatic Diseases
Current Rheumatology Reviews The Human Microbiome Project, Personalized Medicine and the Birth of Pharmacomicrobiomics
Current Pharmacogenomics and Personalized Medicine Linezolid Induced Skin Reactions in a Multi Drug Resistant Infective Endocarditis Patient: A Rare Case
Current Drug Safety Arterial Ischemic Stroke in Neonates and Children: Review and Current Issues
Current Pediatric Reviews The Influence of Co-Ligands on Improving Tumor Targeting of <sup>99m</sup>Tc-HYNIC Conjugated Peptides
Mini-Reviews in Medicinal Chemistry Antimicrobial Precious-Metal Nanoparticles and their Use in Novel Materials
Recent Patents on Food, Nutrition & Agriculture Role of Bone Marrow in the Pathogenesis of Rheumatoid Arthritis
Current Rheumatology Reviews Fibrinogen Signal Transduction as a Mediator and Therapeutic Target in Inflammation:Lessons from Multiple Sclerosis
Current Medicinal Chemistry Ethnic and Geographical Differences in Ischaemic Stroke Among Young Adults
Current Vascular Pharmacology Kawasaki Disease and Its Treatment – An Update
Current Rheumatology Reviews Antibiotics in Endophthalmitis: Microbiological and Pharmacokinetic Considerations
Current Clinical Pharmacology Contrast Enhanced Sonography for Diagnosis of (Peri-) Splenic Pathology
Current Medical Imaging Current Developments in Therapeutic and Diagnostic Strategies for Q Fever: Glimpses of Patent Analysis
Recent Patents on Anti-Infective Drug Discovery Protective Effects of Astaxanthin on Nephrotoxicity in Rats with Induced Renovascular Occlusion
Combinatorial Chemistry & High Throughput Screening Natural Products Towards the Discovery of Potential Future Antithrombotic Drugs
Current Pharmaceutical Design Epidemiological Review of Gonococcal Infection
Current Women`s Health Reviews Adenotonsillar Disease
Recent Patents on Inflammation & Allergy Drug Discovery The Need for Diagnostic Criteria in Systemic Vasculitis
Current Immunology Reviews (Discontinued)