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.
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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 |
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