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

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.

journal_name

J Inorg Biochem

journal_title

Journal of inorganic biochemistry

authors

Barbosa ASL,Guedes JS,da Silva DR,Meneghetti SMP,Meneghetti MR,da Silva AE,de Araujo MV,Alexandre-Moreira MS,de Aquino TM,de Siqueira Junior JP,de Araújo RSA,da Cruz RMD,Mendonça-Junior FJB

doi

10.1016/j.jinorgbio.2017.12.004

subject

Has Abstract

pub_date

2018-03-01 00:00:00

pages

80-88

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(17)30603-7

journal_volume

180

pub_type

杂志文章

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