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BIBTEX RIS

Synthesis and evaluation of the antibiotic and adjuvant antibiotic potential of organotin(IV) derivatives

2017; Elsevier BV; Volume: 180; Linguagem: Inglês

10.1016/j.jinorgbio.2017.12.004

1873-3344

Ana Soraya Lima Barbosa, Jéssica de Siqueira Guedes, Douglas Rozendo da Silva, Simoni Margareti Plentz Meneghetti, Mário R. Meneghetti, Amanda Evelyn da Silva, Morgana Vital de Araújo, Magna Suzana Alexandre‐Moreira, Thiago Mendonça de Aquino, José P. Siqueira-Júnior, Rodrigo Santos Aquino de Araújo, Ryldene Marques Duarte da Cruz, Francisco Jaime Bezerra Mendonça,

Antimicrobial agents and applications

A series of organotin(IV) derivatives was investigated in vitro for their antibiotic and adjuvant antibiotic properties (efflux pump inhibitors) against Staphylococcus aureus strains that overexpress efflux pump proteins for norfloxacin (SA-1199B), erythromycin (RN-4220) and tetracycline (IS-58). Most organotin(IV) compounds showed significant antibacterial activity with small Minimum Inhibitory Concentration (MIC) values, some of which were close to 1.0 μg/mL (3.1 μM), but this feature was also associated with substantial cytotoxicity. Nevertheless, the cytotoxicity of these organotin(IV) compounds can be overcome when they are used as antibiotic adjuvants. Their remarkable adjuvant antibiotic properties allow potentiation of the action of tetracycline (against IS-58 strain) by up to 128-fold. This likely indicates that they can act as putative inhibitors of bacterial efflux pumps. These results reinforce organotin(IV) complexes as promising antibacterial agents, and many of these complexes, if associated with antibiotics, can act as potential adjuvant antibiotic candidates.