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Reversal of antibiotic resistance in Gram‐positive bacteria by the antihistaminic azelastine
Author(s) -
ELNAKEEB MOUSTAFA A.,
ABOUSHLEIB HAMIDA M.,
KHALIL AMAL M.,
OMAR HODA G.,
ELHALFAWY OMAR M.
Publication year - 2012
Publication title -
apmis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.909
H-Index - 88
eISSN - 1600-0463
pISSN - 0903-4641
DOI - 10.1111/j.1600-0463.2011.02823.x
Subject(s) - azelastine , antibiotics , antibiotic resistance , microbiology and biotechnology , staphylococcus aureus , staphylococcus epidermidis , antimicrobial , enterococcus faecium , drug resistance , medicine , pharmacology , bacteria , biology , genetics
El‐Nakeeb MA, Abou‐Shleib HM, Khalil AM, Omar HG, El‐Halfawy OM. Reversal of antibiotic resistance in Gram‐positive bacteria by the antihistaminic azelastine. APMIS 2012; 120: 215–20. Antibiotic resistance represents a serious problem that complicates microbial infection. The use of ‘helper compounds’ capable of enhancing the antimicrobial activity of antibiotics is being investigated. Azelastine, a new generation antihistaminic, possesses certain antibacterial activity and is capable of inducing alteration in the bacterial membrane permeability. Hence, we hypothesized that it could reverse resistance to antibiotics. Azelastine significantly increased the antibacterial activity of eight antibiotics belonging to five different classes (β‐lactams, macrolides, fluoroquinolones, aminoglycosides and tetracyclines) against nine Gram‐positive clinical isolates: five Staphylococcus aureus , two Staphylococcus epidermidis and two Enterococcus faecium , seven of which were multi‐drug resistant, reversing their resistance to the tested antibiotics. The synergistic effects of azelastine with the studied antibiotics increased with raising the pH from 5 to 8. Antibiotics did not affect the ability of azelastine to alter the permeability of a liposomal artificial membrane model, an effect thought to be critical for the interaction with antibiotics. The findings of this study present azelastine as a potential ‘helper compound’ that could reverse the resistance of multi‐drug resistant Gram‐positive clinical isolates to antibiotics.