scholarly journals Kinetic, Thermodynamic, and Crystallographic Studies of 2-Triazolylthioacetamides as Verona Integron-Encoded Metallo-β-Lactamase 2 (VIM-2) Inhibitor

Biomolecules ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 72
Author(s):  
Yang Xiang ◽  
Yue-Juan Zhang ◽  
Ying Ge ◽  
Yajun Zhou ◽  
Cheng Chen ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Antibacterial Activity ◽  
Active Sites ◽  
Crystal Structure Analysis ◽  
Diffusion Method ◽  
Titration Calorimetry ◽  
Resistant Bacteria ◽  
Aliphatic Carboxylic Acid ◽  
E Coli ◽  
Fold Reduction

Inhibition of β-lactamases presents a promising strategy to restore the β-lactams antibacterial activity to resistant bacteria. In this work, we found that aromatic carboxyl substituted 2-triazolylthioacetamides 1a–j inhibited VIM-2, exhibiting an IC50 value in the range of 20.6–58.6 μM. The structure-activity relationship study revealed that replacing the aliphatic carboxylic acid with aromatic carboxyl improved the inhibitory activity of 2-triazolylthioacetamides against VIM-2. 1a–j (16 mg/mL) restored the antibacterial activity of cefazolin against E. coli cell expressing VIM-2, resulting in a 4–8-fold reduction in MICs. The isothermal titration calorimetry (ITC) characterization suggested that the primary binding 2-triazolylthioacetamide (1b, 1c, or 1h) to VIM-2 was a combination of entropy and enthalpy contributions. Further, the crystal structure of VIM-2 in complex with 1b was obtained by co-crystallization with a hanging-drop vapour-diffusion method. The crystal structure analysis revealed that 1b bound to two Zn(II) ions of the enzyme active sites, formed H-bound with Asn233 and structure water molecule, and interacted with the hydrophobic pocket of enzyme activity center utilizing hydrophobic moieties; especially for the phenyl of aromatic carboxyl which formed π-π stacking with active residue His263. These studies confirmed that aromatic carboxyl substituted 2-triazolylthioacetamides are the potent VIM-2 inhibitors scaffold and provided help to further optimize 2-triazolylthioacetamides as VIM-2 even or broad-spectrum MβLs inhibitors.

scholarly journals Antibacterial Activity of Polygonum pulchrum Blume Ethanol Extract on Staphylococcus aureus and Escherichia coli

2018 ◽  
Vol 3 (2) ◽  
pp. 26
Author(s):  
Asman Sadino ◽  
Idin Sahidin ◽  
Wahyuni Wahyuni
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Ethanol Extract ◽  
Inhibition Zone ◽  
Health Concern ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
E Coli ◽  
Weak Antibacterial Activity

The emergence of resistant bacteria strain has become a global health concern. It encourages the exploration of potential antibacterial agents, particularly from natural sources. The aim of this study was to investigate the antibacterial activity of ethanol extract of root, stems, leaves, and flowers of Polygonum pulchrum Blume against Staphylococcus aureus and Escherichia coli, through disc diffusion method using cup-plate method. Inhibition zone against S. aureus from roots, stems, leaves, and flowers ethanol extract were 3.5 mm, 2.5 mm, 2.25 mm, and 2.62 mm, respectively, while the inhibition zone against E. coli were 2.25 mm, 2.12 mm, 1.62 mm, and 1.75 mm, respectively. In conclusion, ethanol extract of root, stem, leaves, and flower of P. pulchrum Bl possessed weak antibacterial activity against S. aureus and E. coli.Keywords: P. pulchrum Bl, antibacterial, E. coli, S. aureus, cup-plate technique

scholarly journals Chemical Composition and Antibacterial Activity of Essential Oils from the Algerian Endemic Origanum glandulosum Desf. against Multidrug-Resistant Uropathogenic E. coli Isolates

Antibiotics ◽  
2020 ◽  
Vol 9 (1) ◽  
pp. 29 ◽  
Author(s):  
Larbi Zakaria Nabti ◽  
Farida Sahli ◽  
Hocine Laouar ◽  
Ahmed Olowo-okere ◽  
Joice Guileine Nkuimi Wandjou ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Chemical Composition ◽  
Essential Oils ◽  
Multidrug Resistant ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
E Coli ◽  
Broth Microdilution Method ◽  
Resistant Strains ◽  
Tract Infections

Antibiotics are becoming ineffective against resistant bacteria. The use of essential oils (EOs) may constitute an alternative solution to fight against multidrug-resistant bacteria. This study aims to determine the chemical composition of EOs from five populations of the endemic Algerian Origanum glandulosum Desf. and to investigate their potential antibacterial activity against multidrug-resistant uropathogenic E. coli strains. The EOs were obtained by hydrodistillation and their composition was investigated by gas chromatography/mass spectrometry (GC/MS). The antibacterial activity was evaluated by the disc diffusion method against eight E. coli strains (six uropathogenic resistant and two referenced susceptible strains). Minimum inhibitory and bactericidal concentrations (MIC/MBC) were obtained by the broth microdilution method. The main EO components were thymol (15.2–56.4%), carvacrol (2.8–59.6%), γ-terpinene (9.9–21.8%) and p-cymene (8.5–13.9%). The antibacterial tests showed that all the EOs were active against all the strains, including the multidrug-resistant strains. The EO from the Bordj location, which contained the highest amount of carvacrol (59.6%), showed the highest antibacterial activity (inhibition diameters from 12 to 24.5 mm at a dilution of 1/10). To our knowledge, this is the first description of the activity of O. glandulosum EOs against resistant uropathogenic strains. Our study suggests that O. glandulosum EO could be used in some clinical situations to treat or prevent infections (e.g., urinary tract infections) with multidrug-resistant strains.

scholarly journals Antibacterial activity of ethanolic leaf extract of Aquilaria malaccensis against multidrug-resistant Gram-negative pathogen

Food Research ◽  
2020 ◽  
Vol 4 (6) ◽  
pp. 1962-1968
Author(s):  
N.I.M. Jihadi ◽  
Y.Z.H-Y. Hashim ◽  
N.A. Rahim ◽  
K.M. Kamal ◽  
N.M. Noor ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Bacterial Infections ◽  
Leaf Extract ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Aquilaria Malaccensis ◽  
Crude Leaf Extract

The rapid emergence of resistant Gram-negative bacteria and the limited discovery of novel antibiotic is a global healthcare challenge. Many medicinal plants with potent bioactivities have been developed for the treatment of bacterial infections. Aquilaria malaccensis exhibits wide applications from perfumes and aromatic foods ingredients and great potential in medicines. In this study, crude leaf extract of A. malaccensis was evaluated for its antibacterial activity against several pathogenic Gram-negative bacteria. The leaves were processed and extracted by Soxhlet method using ethanol as the solvent. The antibacterial activity of the crude extract was tested by disc diffusion method, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against Acinetobacter baumannii (ATCC 19606), Klebsiella pneumoniae (ATCC 10031 and ATCC 700603) and Escherichia coli (ATCC 1129). Using the optimized method, the Soxhlet extract produced a yield of 178.41 mg/g. Treatment of the extract at 200 mg/mL displayed the largest inhibition zones of 14.0 mm and 9.7 mm against A. baumannii and K. pneumoniae ATCC 10031, respectively. In contrast, against E. coli and K. pneumoniae ATCC 700603, smaller zones of inhibitions of 3.3 mm were demonstrated. The MIC values of the extract were 32 mg/mL against A. baumannii and K. pneumoniae ATCC 10031 and 64 mg/mL against E. coli and K. pneumoniae ATCC 700603. The MBC values of the extract were consistent with the MIC values for all the bacteria investigated. Overall, this study was the first to show antibacterial activity of A. malaccensis leaves extract particularly against A. baumannii and K. pneumoniae and potentially develop for the treatment of resistant bacteria.

scholarly journals Essential Oils of Aerial Parts of Anaphalis margaritacea (L.) Benth.,Salvia leucantha Cav. and Thymus linearis Benth. From Uttarakhand Himalaya: Chemical Constituents and Antibacterial Activity

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
B. C. Joshi ◽  
Vinod Kumar ◽  
Bhuwan Chandra ◽  
N. D. Kandpal
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Chemical Constituents ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
E Coli ◽  
Aerial Parts ◽  
Ms Analysis ◽  
Uttarakhand Himalaya

The components present in the essential oils extracted from Anaphalis margaritacea (L.) Benth., Salvia leucantha Cav. and Thymus linearis Benth. were identified by GC and GC/MS analysis. The main compounds present in the oils were aromadendrene (20.0%) in S. leucantha, Phellandrene (12.5%), α-thujene (12.0%) in A. margaritacea and thymol (50.0%) in T. linearis. The antibacterial activity of all the three oils against E. coli, P. aeruginosa, S. aureus and S. typhi, has been studied. In the antibacterial activity S. typhi is the most resistant bacteria to all the tested oils whereas essential oil of T. linearis showed highest antibactericidal activity against S. aureus in diffusion method.

Antibacterial Activity of Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Kyoung- Sun Seo ◽  
Seong Woo Jin ◽  
Seongkyu Choi ◽  
Kyeong Won Yun
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Agent ◽  
Methanol Extract ◽  
The Other ◽  
Diffusion Method ◽  
E Coli ◽  
Agar Diffusion ◽  
Agar Diffusion Method ◽  
Crude Methanol Extract

The antibacterial activity of three Cupressaceae plants (Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa) was tested against three bacteria using the agar diffusion method. The ether and ethylacetate fraction of crude methanol extract from the three plants showed potent antibacterial activity against the tested microorganisms. The result showed that Staphylococcus aureus revealed the most sensitivity among the tested bacteria. Thujaoccidentalisether fraction and Thujaorientalis hexane fraction exhibited the highest antibacterial activity against Staphylococcus aureus. E. coli was shown the highest MIC values compared to the other two tested bacteria, which indicates the lowest antibacterial activity against the bacterium. This study promises an interesting future for designing a potentially active antibacterial agent from the three Cupressaceae plants.

Bioenhancing Effect of Cow Urine Distillate and Pepper Extract on Antibacterial Activity of Azadirachta Indica Leaves

1970 ◽  
Vol 9 (2) ◽  
pp. 3212-3214
Author(s):  
Pramod Dhakal ◽  
Ankit a Achary ◽  
Vedamurthy Joshi
Keyword(s):  
Antibacterial Activity ◽  
Azadirachta Indica ◽  
Pathogenic Bacteria ◽  
Ethanol Extract ◽  
Watery Diarrhea ◽  
Diffusion Method ◽  
E Coli ◽  
Drug Molecules ◽  
Cow Urine

Bioenhancers are drug facilitator which do not show the typical drug activity but in combination to enhance the activity of other molecule in several way including increase the bioavailability of drug across the membrane, potentiating the drug molecules by conformational interaction, acting as receptor for drug molecules and making target cell more receptive to drugs and promote and increase the bioactivity or bioavailability or the uptake of drugs in combination therapy. The objective of the present study was to evaluate the antibacterial and activity of combination in Azadirachta indica extract with cow urine distillate and pepper extract against common pathogenic bacteria, a causative agent of watery diarrhea. It has been found that Indian indigenous cow urine and its distillate also possess bioenhancing ability. Bioenhancing role of cow urine distillate (CUD) and pepper extract was investigated on antibacterial activity of ethanol extract of Azadirachta indica. Antibacterial activity of ethanol extract neem alone and in combination with CUD and pepper extract were determined the ATCC strains against Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and E-coli by cup plate diffusion method. Ethanol extract of neem has showed more effect on P. aeruginosa, E-coli than S. aureus and K. pneumonia with combination of CUD and pepper extract. CUD and pepper did not show any inhibition of test bacteria in low concentration. The antibacterial effect of combination of extract and CUD was higher than the inhibition caused by extract alone and is suggestive of the bioenhancing role of cow urine distillate and pepper. Moreover, inhibition of test bacteria was observed with less concentration of extract on combining with CUD

scholarly journals Phenotypic Antimicrobial Susceptibility of Escherichia coli from Raw Meats, Ready-to-Eat Meats, and Their Related Samples in One Health Context

2021 ◽  
Vol 9 (2) ◽  
pp. 326
Author(s):  
Frederick Adzitey ◽  
Nurul Huda ◽  
Amir Husni Mohd Shariff
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Resistance ◽  
Antimicrobial Susceptibility ◽  
Resistance Index ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
Disk Diffusion Method ◽  
E Coli ◽  
The Usa ◽  
Raw Meats

Meat is an important food source that can provide a significant amount of protein for human development. The occurrence of bacteria that are resistant to antimicrobials in meat poses a public health risk. This study evaluated the occurrence and antimicrobial resistance of E. coli (Escherichia coli) isolated from raw meats, ready-to-eat (RTE) meats and their related samples in Ghana. E. coli was isolated using the USA-FDA Bacteriological Analytical Manual and phenotypic antimicrobial susceptibility test was performed by the disk diffusion method. Of the 200 examined meats and their related samples, 38% were positive for E. coli. Notably, E. coli was highest in raw beef (80%) and lowest in RTE pork (0%). The 45 E. coli isolates were resistant ≥ 50% to amoxicillin, trimethoprim and tetracycline. They were susceptible to azithromycin (87.1%), chloramphenicol (81.3%), imipenem (74.8%), gentamicin (72.0%) and ciprofloxacin (69.5%). A relatively high intermediate resistance of 33.0% was observed for ceftriaxone. E. coli from raw meats, RTE meats, hands of meat sellers and working tools showed some differences and similarities in their phenotypic antimicrobial resistance patterns. Half (51.1%) of the E. coli isolates exhibited multidrug resistance. The E. coli isolates showed twenty-two different resistant patterns, with a multiple antibiotic resistance index of 0.0 to 0.7. The resistant pattern amoxicillin (A, n = 6 isolates) and amoxicillin-trimethoprim (A-TM, n = 6 isolates) were the most common. This study documents that raw meats, RTE meats and their related samples in Ghana are potential sources of antimicrobial-resistant E. coli and pose a risk for the transfer of resistant bacteria to the food chain, environment and humans.

scholarly journals Antibacterial Activity of Prismatomeris tetrandra K. Schum Root Extract against Antibiotic Resistance Bacteria

2018 ◽  
Vol 16 (5) ◽  
pp. 341-348
Author(s):  
On-Anong SOMSAP
Keyword(s):  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Culture Broth ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
Root Extract ◽  
Gram Negative Bacteria ◽  
Antibiotic Resistant ◽  
Gram Positive Bacteria ◽  
Colony Forming Units

Antibiotic resistance bacteria has become an increasing problem now today due to many factors. This study investigates the efficacy of Prismatomeris tetrandra K. Schum root extract as a new source of antibacterial activity for antibiotic resistant bacteria using agar well diffusion method. The results showed that S. aureus TISTR517 exhibited more sensitivity to P. tetrandra K. Schum root extract than other Gram-positive bacteria indicator strains. On the other hand, Gram-negative bacteria exhibited resistance to P. tetrandra K. Schum root extract. The study further showed the activity between P. tetrandra K. Schum root extract and gentamycin (10 µg), it revealed that MRSA142 was resistant to gentamycin (10µg) but sensitive to P. tetrandra K. Schum root extract. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) was evaluated by using S. aureus TISTR517 and MRSA142 as indicator strains. The MIC value was 0.59 mg/mL and 1.17 mg/mL for S. aureus TISTR517 and MRSA142, respectively. MBC assay demonstrated that the MBC value was 9.75 mg/mL and 150 mg/mL for S. aureus TISTR517 and MRSA142 respectively. The mode of action was investigated with the presence of P. tetrandra K. Schum root extract in the culture broth. The action of P. tetrandra K. Schum root extract was revealed of bacteriostatic activity due to the Optical density (OD) at 600 nm and Colony-Forming Units (CFU) of indicator strains were continuously decreased.

scholarly journals Antibacterial activity of ginger extracts and its essential oil on some of pathogenic bacteria

2010 ◽  
Vol 7 (3) ◽  
pp. 1159-1165
Author(s):  
Baghdad Science Journal
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Essential Oil ◽  
Pathogenic Bacteria ◽  
Cold Water ◽  
Water Extract ◽  
Ethanolic Extract ◽  
Hot Water ◽  
Diffusion Method ◽  
Resistant Bacteria

The antimicrobial activity of ginger extracts ( cold-water, hot-water, ethanolic and essential oil ) against some of pathogenic bacteria ( Escherichia coli , Salmonella sp , Klebsiella sp , Serratia marcescens, Vibrio cholerae , Staphylococcus aureus , Streptococcus sp) was investigated using Disc diffusion method , and the results were compared with the antimicrobial activity of 12 antibiotics on the same bacteria . The results showed that the ginger extracts were more effective on gram-positive bacteria than gram-negative . V. cholerae and S. marcescens,were the most resistant bacteria to the extracts used , while highest inhibition was noticed against Streptococcus sp (28 mm) . The ethanolic extract showed the broadest antibacterial activity ( 11 to 28 mm ) , in comparison with moderate activity of essential oil , it was observed that the cold-water extract was more effective on the bacteria than hot-water extract . Ginger ethanolic extract presented higher diameter of inhibition zone for Streptococcus sp than in Ciprofloxacin , Cefotaxime , Cefalotin , Cephalexin and Cephaloridine , also it was found a similarity between the higher inhibition zones of ethanolic extract of ginger and some antibiotics for S. aureus , E. coli , Salmonella sp and Klebsiella sp . V. cholerae and S. marcescens,also highly resistant to antibiotics . Phytochemical analysis of ethanolic extract of ginger revealed the present of glycosides, terpenoids, flavonids and phenolic compounds

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