scholarly journals Evaluation of the Antibacterial Activity and Efflux Pump Reversal of Thymol and Carvacrol against Staphylococcus aureus and Their Toxicity in Drosophila melanogaster

Molecules ◽  
2020 ◽  
Vol 25 (9) ◽  
pp. 2103 ◽  
Author(s):  
Zildene de Sousa Silveira ◽  
Nair Silva Macêdo ◽  
Joycy Francely Sampaio dos Santos ◽  
Thiago Sampaio de Freitas ◽  
Cristina Rodrigues dos Santos Barbosa ◽  
...  

The antibacterial activity and efflux pump reversal of thymol and carvacrol were investigated against the Staphylococcus aureus IS-58 strain in this study, as well as their toxicity against Drosophila melanogaster. The minimum inhibitory concentration (MIC) was determined using the broth microdilution method, while efflux pump inhibition was assessed by reduction of the antibiotic and ethidium bromide (EtBr) MICs. D. melanogaster toxicity was tested using the fumigation method. Both thymol and carvacrol presented antibacterial activities with MICs of 72 and 256 µg/mL, respectively. The association between thymol and tetracycline demonstrated synergism, while the association between carvacrol and tetracycline presented antagonism. The compound and EtBr combinations did not differ from controls. Thymol and carvacrol toxicity against D. melanogaster were evidenced with EC50 values of 17.96 and 16.97 µg/mL, respectively, with 48 h of exposure. In conclusion, the compounds presented promising antibacterial activity against the tested strain, although no efficacy was observed in terms of efflux pump inhibition.

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Johana Rondevaldova ◽  
Olga Leuner ◽  
Alemtshay Teka ◽  
Ermias Lulekal ◽  
Jaroslav Havlik ◽  
...  

Bacterial infections are in less-developed countries traditionally treated by remedies prepared from medicinal plants.Embelia schimperi(Vatke) is a plant used as a taenicide or disinfectant in Ethiopia, very often taken mixed with another plant species. In the present study, we examined two extracts prepared from seeds and twigs with leaves ofE. schimperiand its main present secondary metabolite embelin for their antibacterial combinatory effect with oxacillin and tetracycline against sensitive and resistantStaphylococcus aureusstrains. Minimum inhibitory concentrations were determined through the broth microdilution method, whereas the combinatory effect was evaluated through fractional inhibitory concentration sum (ΣFIC) indices. Results show many positive interactions and synergy occurring in embelin and oxacillin combinations against 4 out of 9 strains (ΣFIC 0.203–0.477) and for embelin and tetracycline combination against 3 out of 9 strains (ΣFIC 0.400–0.496). Moreover, the resistance to oxacillin has been overcome in 2 strains and to tetracycline in 3 strains. According to our knowledge, this is the first study showing antimicrobial combinatory effect ofE. schimperias well as of embelin. These findings can be used for the further research targeted on the development of new antistaphylococcal agents.


2015 ◽  
Vol 10 (2) ◽  
pp. 1934578X1501000
Author(s):  
Harizon ◽  
Betry Pujiastuti ◽  
Dikdik Kurnia ◽  
Dadan Sumiarsa ◽  
Yoshihito Shiono ◽  
...  

The new lupane-type triterpenoid, 3β-hydroxy-lup-9(11), 12-diene, 28-oic acid (1), along with two known lupane-type triterpenoids, lupeol (2) and lupan-3p-ol (3), were isolated from the bark of Sonnetaria alba. The structure of the new compound was elucidated on the basis of spectroscopic and mass spectrometric data analysis. Using the broth microdilution method, all compounds exhibited antibacterial activity against the Gram-positive bacteria Staphylococcus aureus ATCC 6538 and Streptococcus mutans ATCC 25175, with minimum inhibitory concentrations ranging from 15-33 to 35-55 ng/mL, respectively.


2019 ◽  
Vol 11 (03) ◽  
pp. 220-228
Author(s):  
Sumit Rai ◽  
Mukta Tandon ◽  
Narendra Pal Singh ◽  
Vikas Manchanda ◽  
Iqbal Rajinder Kaur

Abstract BACKGROUND: The Clinical and Laboratory Standards Institute recommends reporting minimum inhibitory concentration (MIC) values of vancomycin for Staphylococcus aureus. Commercial MIC strips are expensive, and the traditional broth microdilution method is cumbersome. With this background, we attempted to develop and standardize an in-house agar gradient method to determine MIC values of vancomycin for S. aureus. OBJECTIVES: To develop and validate an in-house vancomycin MIC strip, based on simple agar gradient method for S. aureus as per bioassay development guidelines. MATERIALS AND METHODS: Filter paper gradient strips were made in house and impregnated with varying concentrations of vancomycin to create an antibiotic gradient. During standardization, MICs of ninety clinical strains of S. aureus and ATCC 29213 were tested by the broth microdilution and commercial strip followed by the in-house strip. During the validation stage, MICs of ninety different clinical strains of S. aureus and ATCC 29213 were determined by the in-house strip followed by MIC detection by broth microdilution and commercial strips. A reading of more than ± 1log2 dilution compared with broth microdilution was considered as an outlier. RESULTS: During the initial stage, there were 7/90 outliers in the clinical strains, and no outliers were seen with the ATCC 29213 control strain. Corrective action included increasing precaution during the antibiotic impregnation on the strip. During validation stage, only 4/90 outliers were observed in the clinical strains. The commercial strips had 29/90 among clinical and 15/30 outliers in the control strain during the prevalidation phase. Despite maintaining cold chain during the validation phase, the outliers for commercial strip were 18/90 and 4/30 for clinical and control strains, respectively. CONCLUSION: Reporting vancomycin MIC for S. aureus may be attempted using the in-house method after validating it with a gold standard broth microdilution method and quality control as per protocol.


2018 ◽  
Vol 13 (3) ◽  
pp. 1934578X1801300 ◽  
Author(s):  
Marina Milenković ◽  
Jelena Stošović ◽  
Violeta Slavkovska

The subject of the study was the investigation of the chemical composition and antimicrobial activity of the essential oils (EOs) isolated from Calamintha sylvatica, C. vardarensis, C. nepeta and C. glandulosa, as well as their antibacterial activity in combination with antibiotics. The quantitative and qualitative analysis of EOs was performed using the GC/FID and GC/MS methods. The antimicrobial activity of EOs against six standard bacterial strains and one strain of yeast was tested using the broth microdilution method, while the antimicrobial activity of a combination of essential oils and gentamicin/ciprofloxacin was tested by the checkerboard method. The dominant components (> 10%) of the essential oils were: cis-piperitone epoxide and menthone ( C. sylvatica), pulegone and menthone ( C. vardarensis), pulegone and piperitenone ( C. nepeta), pulegone, piperitenone, menthone and piperitone ( C. glandulosa). EOs did not exhibit significant antimicrobial activity except the essential oil of C. vardarensis which was selectively active against Staphylococcus aureus (MIC - 21.25 μg/mL). The overall effect of essential oil-antibiotic combinations varied from synergistic (FICI ≤ 0.5) to antagonistic (FICI ≥ 2) depending on the bacterial strain tested.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Su-Hyun Mun ◽  
Ok-Hwa Kang ◽  
Dae-Ki Joung ◽  
Sung-Bae Kim ◽  
Yun-Soo Seo ◽  
...  

Sophoraflavanone B (SPF-B), a known prenylated flavonoid, was isolated from the roots ofDesmodium caudatum. The aim of this study was to determine the antimicrobial synergism of SPF-B combined with antibiotics against methicillin-resistantStaphylococcus aureus(MRSA). MRSA, a multidrug-resistant pathogen, causes both hospital- and community-acquired infections worldwide. The antimicrobial activity of SPF-B was assessed by the broth microdilution method, checkerboard dilution test, and time-kill curve assay. The MIC of SPF-B for 7 strains ofS. aureusranges from 15.6 to 31.25 μg/mL determined. In the checkerboard method, the combinations of SPF-B with antibiotics had a synergistic effect; SPF-B markedly reduced the MICs of theβ-lactam antibiotics: ampicillin (AMP) and oxacillin (OXI); aminoglycosides gentamicin (GET); quinolones ciprofloxacin (CIP) and norfloxacin (NOR) against MRSA. The time-kill curves assay showed that a combined SPF-B and selected antibiotics treatment reduced the bacterial counts below the lowest detectable limit after 24 h. These data suggest that the antibacterial activity of SPF-B against MRSA can be effectively increased through its combination with three groups of antibiotics (β-lactams, aminoglycosides, and quinolones). Our research can be a valuable and significant source for the development of a new antibacterial drug with low MRSA resistance.


Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5570
Author(s):  
Luiz Jardelino de Lacerda Neto ◽  
Andreza Guedes Barbosa Ramos ◽  
Thiago Sampaio de Freitas ◽  
Cristina Rodrigues dos Santos Barbosa ◽  
Dárcio Luiz de Sousa Júnior ◽  
...  

Products of natural origin remain important in the discovery of new bioactive molecules and are less damaging to the environment. Benzaldehyde is a product of the metabolism of plants, and similarly to oxygenated terpenes, it can have antibacterial activity against Staphylococcus aureus and toxic action against Drosophila melanogaster; we aimed to verify these activities. The broth microdilution tests determined the minimum inhibitory concentration (MIC) of benzaldehyde alone and in association with antibiotics and ethidium bromide (EtBr). Toxicity against Drosophila melanogaster was determined by fumigation tests that measured lethality and damage to the locomotor system. The results indicated that there was an association of norfloxacin and ciprofloxacin with benzaldehyde, from 64 μg/mL to 32 μg/mL of ciprofloxacin in the strain K6028 and from 256 μg/mL to 128 μg/mL of norfloxacin in the strain 1199B; however, the associations were not able to interfere with the functioning of the tested efflux pumps. In addition, benzaldehyde had a toxic effect on flies. Thus, the results proved the ability of benzaldehyde to modulate quinolone antibiotics and its toxic effects on fruit flies, thus enabling further studies in this area.


2021 ◽  
Vol 17 ◽  
Author(s):  
Lijuan Zhai ◽  
Lili He ◽  
Yuanbai Liu ◽  
Ko Ko Myo ◽  
Zafar Iqbal ◽  
...  

Background: Mononcyclic β-lactams are regarded as the most resistant class of β-lactams against a series of β-lactamases though possess limited antibacterial activity. Aztreonam being the first clinically approved monobactam needs broad-spectrum efficacy through structural modification. Objective: We strive to synthesize a number of monocyclic β-lactams by varying the substituents at N1, C3 and C4 positions of azetidinone ring and study the antimicrobial effect on variable bacterial strains. Methods: Seven new monobactam derivatives 23a-g, containing substituted-amidine moieties linked to the azetidinone ring via thiazole linker, were synthesized through multistep synthesis. The final compounds were investigated for their in vitro antibacterial activities using broth microdilution method, against ten bacterial strains of clinical interest. The minimum inhibitory concentrations (MICs) of newly synthesized derivatives were compared with aztreonam, ceftazidime and meropenem, existing clinical antibiotics. Results: All compounds 23a-g showed higher antibacterial activities (MIC 0.25 µg/mL to 64 µg/mL) against tested strains as compared to aztreonam (MIC 16 µg/mL to >64 µg/mL) and ceftazidime (MIC >64 µg/mL). However all compounds, except 23d, exhibited lower antibacterial activity against all tested bacterial strains as compared to meropenem. Conclusion: Compound 23d showed comparable or improved antibacterial activity (MIC 0.25 µg/mL to 2 µg/mL) to meropenem (MIC 1 µg/mL to 2 µg/mL) in case of seven bacterial species. Therefore, compound 23d may be valuable lead target for further investigations against multi-drug resistant Gram-negative bacteria.


2002 ◽  
Vol 46 (9) ◽  
pp. 3039-3041 ◽  
Author(s):  
Sofia Perea ◽  
Gloria Gonzalez ◽  
Annette W. Fothergill ◽  
William R. Kirkpatrick ◽  
Michael G. Rinaldi ◽  
...  

ABSTRACT The interaction between caspofungin acetate and voriconazole was studied in vitro by using 48 clinical Aspergillus spp. isolates obtained from patients with invasive aspergillosis. MICs were determined by the NCCLS broth microdilution method. Synergy, defined as a fractional inhibitory concentration (FIC) index of <1, was detected in 87.5% of the interactions; an additive effect, defined as an FIC index of 1.0, was observed in 4.2% of the interactions; and a subadditive effect, defined as an FIC index of 1.0 to 2.0, was found in 8.3% of the interactions. No antagonism was observed. Animal models are required to validate the in vivo significance of these in vitro data presented for the combination of caspofungin and voriconazole.


2018 ◽  
Vol 24 (4) ◽  
pp. 105-110
Author(s):  
D. V. Tapalski ◽  
P. A. Volotovski ◽  
A. I. Kozlova ◽  
A. Sitnik

Purpose — to evaluate the presence and duration of antibiotic activity of antibiotic-impregnated bone cement based coatings samples against antibiotic-sensitive and antibiotic-resistant microorganisms.Material and Methods. Bone cement based coatings impregnated with antibiotics (gentamycin, vancomycin, colistin, meropenem, fosfomycin) are formed on titanium (Ti) plates. A plate rinse was carried out; antibiotic concentrations in the rinsed solutions were estimated by a serial broth microdilution method. Antibacterial activity of the control and rinsed samples against the antibiotic-sensitive and multiple-antibiotic-resistant Staphylococcus aureus and Pseudomonas aeruginosa strains was estimated by a bilayer agar method.Results. The meropenem and fosfomycin concentrations in the rinsed solutions obtained at a one-fold (16 μg/ml for both antibiotics) and two-fold treatment (2 μg/ml for meropenem and 8 μg/ml for fosfomycin) were sufficient to suppress the growth of the control strains. One-fold rinse of samples with colistin eliminated their antibacterial activity completely. The marked activity of the samples with meropenem and fosfomycin persisted against the antibiotic-sensitive P. aeruginosa ATCC 27853 strain after 2 rinse cycles; single-rinsed samples with fosfomycin also maintained the activity against the extensively antibioticresistant P. aeruginosa BP-150 strain. Vancomycin-containing samples possessed the sufficient antibacterial activity against both methicillin-sensitive (MSSA) and methicillin-resistant (MRSA) S. aureus strains; two-fold rinse of the samples eliminated their bactericidal properties.Conclusion. Bone cement based coatings impregnated with fosfomycin and meropenem possess the most marked and long-lasting antibacterial activity, manifested mainly against the antibiotic-sensitive strains. 


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