Abstract
Despite the increasing need for antibiotics to fight infectious diseases, fewer new antibiotics are available on the market. Unfortunately, developing a new class of antibiotics is associated with high commercial risk. Therefore, modification or combination of existing antibiotics to improve their efficacy is a promising strategy. Herein, we conjugated the antibiotic, levofloxacin, with two peptides, i.e. an antimicrobial peptide indolicidin and a cell penetrating peptide (TAT). Glycolic acid and glycine linkers were used between levofloxacin and peptides. We developed an optimized condition for coupling of levofloxacin via its carboxylic group to glycolic acid using solid phase peptide synthesis (SPPS). Antibacterial and haemolytic assays were carried out on the conjugates and only the levofloxacin-indolicidin conjugate demonstrated moderate antibacterial activity. Interestingly, physical mixture of levofloxacin and indolicidin showed improvement in the activity against Gram-positive bacteria.
Keywords: Antibiotic, levofloxacin, indolicidin, TAT peptide, conjugation.
Current Drug Delivery
Title:Levofloxacin and Indolicidin for Combination Antimicrobial Therapy
Volume: 12 Issue: 1
Author(s): Khairunnisa Abdul Ghaffar, Waleed M. Hussein, Zeinab G. Khalil, Robert J. Capon, Mariusz Skwarczynski and Istvan Toth
Affiliation:
Keywords: Antibiotic, levofloxacin, indolicidin, TAT peptide, conjugation.
Abstract: Despite the increasing need for antibiotics to fight infectious diseases, fewer new antibiotics are available on the market. Unfortunately, developing a new class of antibiotics is associated with high commercial risk. Therefore, modification or combination of existing antibiotics to improve their efficacy is a promising strategy. Herein, we conjugated the antibiotic, levofloxacin, with two peptides, i.e. an antimicrobial peptide indolicidin and a cell penetrating peptide (TAT). Glycolic acid and glycine linkers were used between levofloxacin and peptides. We developed an optimized condition for coupling of levofloxacin via its carboxylic group to glycolic acid using solid phase peptide synthesis (SPPS). Antibacterial and haemolytic assays were carried out on the conjugates and only the levofloxacin-indolicidin conjugate demonstrated moderate antibacterial activity. Interestingly, physical mixture of levofloxacin and indolicidin showed improvement in the activity against Gram-positive bacteria.
Export Options
About this article
Cite this article as:
Ghaffar Abdul Khairunnisa, Hussein M. Waleed, Khalil G. Zeinab, Capon J. Robert, Skwarczynski Mariusz and Toth Istvan, Levofloxacin and Indolicidin for Combination Antimicrobial Therapy, Current Drug Delivery 2015; 12 (1) . https://dx.doi.org/10.2174/1567201811666140910094050
DOI https://dx.doi.org/10.2174/1567201811666140910094050 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
- 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
-
Alpha9Alpha10 Nicotinic Acetylcholine Receptors as Target for the Treatment of Chronic Pain
Current Pharmaceutical Design TNF-Related Apoptosis-Inducing Ligand (TRAIL) as a Pro-Apoptotic Signal Transducer with Cancer Therapeutic Potential
Current Pharmaceutical Design EGFR Inhibitors and Radiation in HNSCC
Current Cancer Therapy Reviews Heat Shock Factor 1-Regulated miRNAs Can Target Huntingtin and Suppress Aggregates of Mutant Huntingtin
MicroRNA Polyphenols and Aging
Current Aging Science Using Cytokines to Treat Cervical Intraepithelial and Invasive Neoplasia
Recent Patents on Anti-Cancer Drug Discovery Reversal of Multidrug Resistance by Natural Substances from Plants
Current Topics in Medicinal Chemistry Combined Cancer Therapy with Non-Conventional Drugs: All Roads Lead to AMPK
Mini-Reviews in Medicinal Chemistry Cisplatin Resistance and Transcription Factors
Current Medicinal Chemistry - Anti-Cancer Agents Involvement of Cytoskeleton in AhR-Dependent CYP1A1 Expression
Current Drug Metabolism Viral Disorder or Disordered Viruses: Do Viral Proteins Possess Unique Features?
Protein & Peptide Letters Central Nervous System Abnormalities in Fibromyalgia and Chronic Fatigue Syndrome: New Concepts in Treatment
Current Pharmaceutical Design Editorial (Thematic Issue: Improving Cancer Clinical Research and Trials with Hispanic Populations: Training and Outreach Efforts Between Moffitt Cancer Center and the Ponce School of Medicine)
Reviews on Recent Clinical Trials Oncolytic Viruses for Induction of Anti-Tumor Immunity
Current Pharmaceutical Biotechnology Synthesis, Structure Activity Relationship (SAR), and Biological Activities of Benzylideneacetophenones Derivatives
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry WNT Signaling in Stem Cell Biology and Regenerative Medicine
Current Drug Targets Challenges in Breast Cancer Control in Malaysia
Current Women`s Health Reviews Comparative Proteomics and Bioinformatics Analysis of Tissue from Non-Small Cell Lung Cancer Patients
Current Proteomics Secondary Metabolites from Cordyceps Species and Their Antitumor Activity Studies
Recent Patents on Biotechnology Obesity-Driven Inflammation and Colorectal Cancer
Current Medicinal Chemistry