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Modulation of Drug Resistance in Staphylococcus aureus with Coumarin Derivatives

2016; Hindawi Publishing Corporation; Volume: 2016; Linguagem: Inglês

10.1155/2016/6894758

2090-908X

Rodrigo Santos Aquino de Araújo, José Maria Barbosa‐Filho, Luciana Scotti, Luciana Scotti, Ryldene Marques Duarte da Cruz, Vivyanne dos Santos Falcão-Silva, José P. Siqueira-Júnior, Francisco Jaime Bezerra Mendonça,

Antifungal resistance and susceptibility

Semisynthetic and commercial coumarins were investigated for their antibacterial and adjuvant properties with antibiotic agents against norfloxacin, erythromycin, and tetracycline resistant Staphylococcus aureus as based on efflux mechanisms. The coumarins and certain commercial antibiotics had their Minimum Inhibitory Concentrations determined by broth microdilution assay against resistant S. aureus strains which overexpress efflux pump proteins. For evaluation of the modulatory activity, the antibiotics MICs were determined in the presence of the coumarin derivatives at subinhibitory concentration. Although the coumarins did not display relevant antibacterial activity (MIC ≥ 128 µ g/mL), they did modulate the antibiotics activities. Various coumarins, especially the alkylated derivatives in combination with antibiotics at subinhibitory concentrations, modulated antibiotic activity, reducing the MIC for tetracycline and norfloxacin by 2 to 8 times. Polar Surface Area (PSA) studies were performed and the fact that the presence of apolar groups is an important factor for the modulatory activity of coumarins was corroborated. Docking on the Penicillin-Binding Protein from MRSA identified that 18 is a potential ligand presenting low E b i n d i n g . The results indicate that coumarin derivatives modulated antibiotic resistance and may be used as potential antibiotic adjuvants, acting by bacterial efflux pump inhibition in S. aureus .