Thiazolidinedione and thiazole derivatives potentiate norfloxacin activity against NorA efflux pump over expression in Staphylococcus aureus 1199B strains

Pereira, Pedro Silvino; Lima, Maria do Carmo Alves de; Neto, Pedro Paulo Marcelino; Oliveira-Tintino, Cícera Datiane de Morais; Tintino, Saulo Relison; Menezes, Irwin Rose Alencar de; Oliveira, Jamerson Ferreira de; Marchand, Pascal; Coutinho, Henrique Douglas Melo; Rodrigues, Maria do Desterro; Silva, Teresinha Gonçalves da

doi:10.1016/j.bmc.2019.07.006

Cited by 22 publications

(12 citation statements)

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“…Nevertheless, the isolated compound showed more potent antibiotic-enhancing activity against all strains, reducing the MIC of norfloxacin by up to 7 fold in comparison with the antibiotic alone. Studies have demonstrated that antibacterial resistance to norfloxacin is significantly mediated by the expression of efflux systems [38]. Therefore, it is hypothesized that the antibiotic-enhancing effects shown by the EOOO and safrole might involve inhibition of efflux pumps.…”

Section: Discussionmentioning

confidence: 99%

GC-MS Profile and Enhancement of Antibiotic Activity by the Essential Oil of Ocotea odorífera and Safrole: Inhibition of Staphylococcus aureus Efflux Pumps

et al. 2020

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Considering the evidence that essential oils, as well as safrole, could modulate bacterial growth in different resistant strains, this study aims to characterize the phytochemical profile and evaluate the antibacterial and antibiotic-modulating properties of the essential oil Ocotea odorífera (EOOO) and safrole against efflux pump (EP)-carrying strains. The EOOO was extracted by hydrodistillation, and the phytochemical analysis was performed by gas chromatography coupled to mass spectrometry (GC-MS). The antibacterial and antibiotic-modulating activities of the EOOO and safrole against resistant strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa were analyzed through the broth microdilution method. The EP-inhibiting potential of safrole in association with ethidium bromide or antibiotics was evaluated using the S. aureus 1199B and K2068 strains, which carry genes encoding efflux proteins associated with antibiotic resistance to norfloxacin and ciprofloxacin, respectively. A reduction in the MIC of ethidium bromide or antibiotics was used as a parameter of EP inhibition. The phytochemical analysis identified 16 different compounds in the EOOO including safrole as the principal constituent. While the EOOO and safrole exerted clinically relevant antibacterial effects against S. aureus only, they potentiated the antibacterial activity of norfloxacin against all strains evaluated by our study. The ethidium bromide and antibiotic assays using the strains of S. aureus SA1119B and K2068, as well as molecular docking analysis, indicated that safrole inhibits the NorA and MepA efflux pumps in S. aureus. In conclusion, Ocotea odorifera and safrole presented promising antibacterial and antibiotic-enhancing properties, which should be explored in the development of drugs to combat antibacterial resistance, especially in strains bearing genes encoding efflux proteins.

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Section: Discussionmentioning

confidence: 99%

GC-MS Profile and Enhancement of Antibiotic Activity by the Essential Oil of Ocotea odorífera and Safrole: Inhibition of Staphylococcus aureus Efflux Pumps

et al. 2020

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“…Thiazole derivatives NJ20 and NW05 were synthesized by Prof. Dr. Maria do Carmo at the Laboratory of Chemistry and Therapeutic Innovation—LQIT, UFPE [ 15 , 30 ]. All other reagents were purchased from Sigma Aldrich (St. Louis, MO, USA), with analytical grade: glutathione (GSH, PHR1359), 1,1,3,3-tetramethoxypropane (TMP, 108383), 2-Thiobarbituric acid (TBA, T5500), 5,5′-Dithiobis(2-nitrobenzoic acid) (DTNB, D8130), 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT, M5655) and 1,10-phenanthroline (131377).…”

Section: Methodsmentioning

confidence: 99%

“…Its nucleus has been reported to be responsible for most of its pharmacological actions. These compounds are known to influence the regulation of different molecular cascades and have several biological activities, such as antimicrobial [ 4 , 15 ], neurodegenerative [ 5 ], hypoglycemic [ 16 ], antitumor [ 17 ], anti-inflammatory [ 18 ], and antioxidant [ 19 ] activities, among others.…”

Section: Introductionmentioning

confidence: 99%

Neurolocomotor Behavior and Oxidative Stress Markers of Thiazole and Thiazolidinedione Derivatives against Nauphoeta cinerea

et al. 2022

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Thiazolidine compounds NJ20 {(E)-2-(2-(5-bromo-2-methoxybenzylidene)hydrazinyl)-4-(4-nitrophenyl)thiazole} and NW05 [(2-(benzo (d) (1,3) dioxol-4-ylmethylene)-N-(4-bromophenyl)-thiosemicarbazone] potentiated the effect of norfloxacin in resistant bacteria; however, there are no reports on their effects on Nauphoeta cinerea in the literature. The objective of this work was to evaluate the behavioral effects and oxidative markers of NW05 and NJ20 in lobster cockroach N. cinerea. To evaluate the behavioral study, a video tracking software was used to evaluate the locomotor points and the exploratory profile of cockroaches in the horizontal and vertical regions of a new environment. The total concentration of thiol and reduced glutathione (GSH), substances reactive to thiobarbituric acid (TBARS), free iron (II) content and mitochondrial viability were determined. The antioxidant potential was evaluated by the DPPH method. Both substances induced changes in the behavior of cockroaches, showing a significant reduction in the total distance covered and in the speed. In the cell viability test (MTT), there was a significant reduction for NJ20 (1 mM). NJ20 caused a significant increase in total levels of thiol and non-protein thiol (NPSH), although it also slightly increased the content of malondialdehyde (MDA). Both compounds (NW05 and NJ20) caused a significant reduction in the content of free iron at a concentration of 10 mM. In conclusion, the compound NJ20 caused moderate neurotoxicity (1 mM), but had good antioxidant action, while NW05 did not show toxicity or significant antioxidant activity in the model organism tested. It is desirable to carry out complementary tests related to the antioxidant prospection of these same compounds, evaluating them at different concentrations.

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“…Among natural compounds, quercetin, pyrogallol and tannic acid could inhibit NorA efflux pump in S. aureus and the pyrogallol could potentiate gentamicin and norfloxacin against S. aureus [8][9][10] . Moreover, some thiazolidinedione and thiazole derivatives were found to augment noffloxacin by interference with the activity of NorA efflux pump 11 . The objective of this study was the detection of efflux pump as a mechanism of resistance to antimicrobials in some (MDR) S. aureus isolates in addition to screening for some new agents that could act as EPIs and potentiate the effect of antimicrobial agents.…”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Sensitizing multi drug resistant Staphylococcus aureus isolated from surgical site infections to antimicrobials by efflux pump inhibitors

2020

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Background: Staphylococcus aureus is a common hospital acquired infections pathogen. Multidrug-resistant Methicillin-resist- ant Staphylococcus aureus represents a major problem in Egyptian hospitals. The over-expression of efflux pumps is a main cause of multidrug resistance. The discovery of efflux pump inhibitors may help fight multidrug resistance by sensitizing bacteria to antibiotics. This study aimed to investigate the role of efflux pumps in multidrug resistance. Methods: Twenty multidrug resistant S. aureus isolates were selected. Efflux pumps were screened by ethidium bromide agar cartwheel method and polymerase chain reaction. The efflux pump inhibition by seven agents was tested by ethidium bromide agar cartwheel method and the effect on sensitivity to selected antimicrobials was investigated by broth microdilu- tion method. Results: Seventy percent of isolates showed strong efflux activity, while 30% showed intermediate activity. The efflux genes mdeA, norB, norC, norA and sepA were found to play the major role in efflux, while genes mepA, smr and qacA/B had a minor role. Verapamil and metformin showed significant efflux inhibition and increased the sensitivity to tested antimicrobials, while vildagliptin, atorvastatin, domperidone, mebeverine and nifuroxazide showed no effect. Conclusion: Efflux pumps are involved in multidrug resistance in Staphylococcus aureus. Efflux pump inhibitors could increase the sensitivity to antimicrobials. Keywords: Staphylococcus aureus; multidrug resistance; efflux pump inhibitors.

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Thiazolidinedione and thiazole derivatives potentiate norfloxacin activity against NorA efflux pump over expression in Staphylococcus aureus 1199B strains

Cited by 22 publications

References 57 publications

GC-MS Profile and Enhancement of Antibiotic Activity by the Essential Oil of Ocotea odorífera and Safrole: Inhibition of Staphylococcus aureus Efflux Pumps

GC-MS Profile and Enhancement of Antibiotic Activity by the Essential Oil of Ocotea odorífera and Safrole: Inhibition of Staphylococcus aureus Efflux Pumps

Neurolocomotor Behavior and Oxidative Stress Markers of Thiazole and Thiazolidinedione Derivatives against Nauphoeta cinerea

Sensitizing multi drug resistant Staphylococcus aureus isolated from surgical site infections to antimicrobials by efflux pump inhibitors

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