Abstract
Piperine, a trans-trans-isomer of 1-piperoyl-piperidine, was tested in combination with mupirocin for antimicrobial activity against Staphylococcus aureus strains including meticillin-resistant S. aureus. The combination markedly reduced the MIC of mupirocin and also lowered the mutation frequency. Enhanced accumulation and efflux of ethidium bromide from wild-type and mutant (Mup(r)-1) strains in the presence of piperine indicated that inhibition of efflux could be a possible mechanism of potentiation of mupirocin activity by piperine. The combination of piperine with mupirocin in a dermal infection model of mice showed better in vivo efficacy when compared with the commercially available formulation of 2 % mupirocin.
MeSH terms
-
Alkaloids / metabolism*
-
Alkaloids / therapeutic use
-
Animals
-
Anti-Bacterial Agents / metabolism*
-
Anti-Bacterial Agents / therapeutic use
-
Bacterial Proteins / antagonists & inhibitors*
-
Benzodioxoles / metabolism*
-
Benzodioxoles / therapeutic use
-
Disease Models, Animal
-
Drug Synergism
-
Enzyme Inhibitors / metabolism*
-
Enzyme Inhibitors / therapeutic use
-
Ethidium / metabolism
-
Female
-
Membrane Transport Proteins
-
Methicillin-Resistant Staphylococcus aureus / drug effects*
-
Methicillin-Resistant Staphylococcus aureus / enzymology*
-
Mice
-
Microbial Sensitivity Tests
-
Mupirocin / metabolism
-
Piperidines / metabolism*
-
Piperidines / therapeutic use
-
Polyunsaturated Alkamides / metabolism*
-
Polyunsaturated Alkamides / therapeutic use
-
Rodent Diseases / drug therapy
-
Staphylococcal Infections / drug therapy
-
Treatment Outcome
Substances
-
Alkaloids
-
Anti-Bacterial Agents
-
Bacterial Proteins
-
Benzodioxoles
-
Enzyme Inhibitors
-
MdeA protein, Staphylococcus aureus
-
Membrane Transport Proteins
-
Piperidines
-
Polyunsaturated Alkamides
-
Mupirocin
-
Ethidium
-
piperine