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J Inorg Biochem ; 180: 80-88, 2018 03.
Article in English | MEDLINE | ID: mdl-29247870

ABSTRACT

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 1.0µg/mL (3.1µM), 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.


Subject(s)
Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Organotin Compounds/chemical synthesis , Organotin Compounds/pharmacology , Animals , Anti-Bacterial Agents/chemistry , Cell Line , Mice , Microbial Sensitivity Tests , Organotin Compounds/chemistry , Staphylococcus aureus/drug effects , Tetracyclines/pharmacology
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