Antibacterial properties and carbonic anhydrase inhibition profiles of azido sulfonyl carbamate derivatives

Aim: The aim of this study was to identify inhibition of carbonic anhydrase I and II (CA I and II) isozymes by azido sulfonyl carbamates through both in vitro and in silico approaches and also to determine the drug-likeness properties and antibacterial activities of azido sulfonyl carbamates. Methods & Results: In vitro inhibition and molecular docking studies of azido sulfonyl carbamate derivatives (1–4) on isozymes were performed. Except for derivative 4, all derivatives inhibited human CA I and II. Almost all compounds had antibacterial effects. The docking results showed that compound 3 had the best results, with binding energy of -8.20 kcal/mol for human CA I and -8.24 kcal/mol for human CA II. Conclusion: Molecule 4 inhibited only CA I. Its usage as a potential chemotherapeutic agent specific to the CA I isozyme may be considered.

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Medicinal Plants: Antibacterial Effects and Chemical Composition of Essential Oil of Foeniculum vulgare

International Journal of Current Pharmaceutical Review and Research ◽

10.25258/ijcprr.v8i01.9082 ◽

2017 ◽

Vol 8 (01) ◽

Cited By ~ 2

Author(s):

Azadeh Foroughi ◽

Pouya Pournaghi ◽

Fariba Najafi ◽

Akram Zangeneh ◽

Mohammad Mahdi Zangeneh ◽

...

Keyword(s):

Chemical Composition ◽

Medicinal Plants ◽

Essential Oil ◽

Antibacterial Properties ◽

Screen Test ◽

Antibacterial Activities ◽

Gas Chromatography Mass Spectrometry ◽

Resistant Bacteria ◽

Antibacterial Effects ◽

Foeniculum Vulgare

Medicinal plants are considered modern resources for producing agents that could act as alternatives to antibiotics in demeanor of antibiotic-resistant bacteria. The aim of the study was to evaluate the chemical composition and antibacterial activities of essential oil of Foeniculum vulgare (FV) against Pseudomonas aeruginosa and Bacillus subtilis. Gas chromatography mass spectrometry was done to specify chemical composion. As a screen test to detect antibacterial properties of the essential oil, agar disk and agar well diffusion methods were employed. Macrobroth tube test was performed to determinate MIC. The results indicated that the most substance found in FV essential oil was Trans-anethole (47.41 %), also the essential oil of FV with 0.007 g/ml concentration has prevented P. aeruginosa and with 0.002 g/ml concentration has prevented B. subtilis from the growth. Thus, the research represents the antibacterial effects of the medical herb on test P. aeruginosa and B. subtilis. We believe that the article provide support to the antibacterial properties of the essential oil. The results indicate the fact that the essential oil from the plant can be useful as medicinal or preservatives composition.

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Coumaronochromone as antibacterial and carbonic anhydrase inhibitors from Aerva persica (Burm.f.) Merr.: experimental and first-principles approaches

Zeitschrift für Naturforschung C ◽

10.1515/znc-2020-0138 ◽

2020 ◽

Vol 0 (0) ◽

Author(s):

Muhammad Imran ◽

Ahmad Irfan ◽

Mohammed A. Assiri ◽

Sajjad H. Sumrra ◽

Muhammad Saleem ◽

...

Keyword(s):

Carbonic Anhydrase ◽

First Principles ◽

Molecular Electrostatic Potential ◽

Chemical Constituents ◽

Bacterial Strains ◽

Hirshfeld Analysis ◽

Carbonic Anhydrase Inhibition ◽

Inhibition Studies ◽

Lowest Unoccupied Molecular Orbitals

AbstractThe Aerva plants are exceptionally rich in phytochemicals and possess therapeutics potential. Phytochemical screening shows that Aerva persica (Burm.f.) Merr. contains highest contents i.e., total phenolics, flavonoids, flavonols, tannins, alkaloids, carbohydrates, anthraquinones and glycosides. In-vitro antibacterial and enzymatic (carbonic anhydrase) inhibition studies on methanol extracts of A. persica indicated the presence of biological active constituents within chloroform soluble portions. Investigation in the pure constituents on the chloroform portions of A. persica accomplished by column chromatography, NMR and MS analysis. The bioguided isolation yields four chemical constituents of coumaronochromone family, namely aervin (1-4). These pure chemical entities (1-4) showed significant antibacterial activity in the range of 60.05–79.21 µg/ml against various bacterial strains using ampicillin and ciprofloxacin as standard drugs. The compounds 1-4 showed promising carbonic anhydrase inhibition with IC50 values of 19.01, 18.24, 18.65 and 12.92 µM, respectively, using standard inhibitor acetazolamide. First-principles calculations revealed comprehensive intramolecular charge transfer in the studied compounds 1-4. The spatial distribution of highest occupied and lowest unoccupied molecular orbitals, ionization potential, molecular electrostatic potential and Hirshfeld analysis revealed that these coumaronochromone compounds would be proficient biological active compounds. These pure constituents may be used as a new pharmacophore to treat leaukomia, epilepsy, glaucoma and cystic fibrosis.

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A High-Throughput Metabolic Microarray Assay Reveals Antibacterial Effects of Black and Red Raspberries and Blackberries against Helicobacter pylori Infection

Antibiotics ◽

10.3390/antibiotics10070845 ◽

2021 ◽

Vol 10 (7) ◽

pp. 845

Author(s):

Candace Goodman ◽

Katrina N. Lyon ◽

Aitana Scotto ◽

Cyra Smith ◽

Thomas A. Sebrell ◽

...

Keyword(s):

Helicobacter Pylori ◽

High Throughput ◽

Antibacterial Properties ◽

Treatment Strategies ◽

Helicobacter Pylori Infection ◽

Antibacterial Effects ◽

Biolog System ◽

Freeze Dried ◽

H Pylori

Helicobacter pylori infection is commonly treated with a combination of antibiotics and proton pump inhibitors. However, since H. pylori is becoming increasingly resistant to standard antibiotic regimens, novel treatment strategies are needed. Previous studies have demonstrated that black and red berries may have antibacterial properties. Therefore, we analyzed the antibacterial effects of black and red raspberries and blackberries on H. pylori. Freeze-dried powders and organic extracts from black and red raspberries and blackberries were prepared, and high-performance liquid chromatography was used to measure the concentrations of anthocyanins, which are considered the major active ingredients. To monitor antibiotic effects of the berry preparations on H. pylori, a high-throughput metabolic growth assay based on the Biolog system was developed and validated with the antibiotic metronidazole. Biocompatibility was analyzed using human gastric organoids. All berry preparations tested had significant bactericidal effects in vitro, with MIC90 values ranging from 0.49 to 4.17%. Antimicrobial activity was higher for extracts than powders and appeared to be independent of the anthocyanin concentration. Importantly, human gastric epithelial cell viability was not negatively impacted by black raspberry extract applied at the concentration required for complete bacterial growth inhibition. Our data suggest that black and red raspberry and blackberry extracts may have potential applications in the treatment and prevention of H. pylori infection but differ widely in their MICs. Moreover, we demonstrate that the Biolog metabolic assay is suitable for high-throughput antimicrobial susceptibility screening of H. pylori.

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Flavone-Rich Fractions and Extracts from Oroxylum indicum and Their Antibacterial Activities against Clinically Isolated Zoonotic Bacteria and Free Radical Scavenging Effects

Molecules ◽

10.3390/molecules26061773 ◽

2021 ◽

Vol 26 (6) ◽

pp. 1773

Author(s):

Patchima Sithisarn ◽

Piyanuch Rojsanga ◽

Pongtip Sithisarn

Keyword(s):

Antibacterial Activities ◽

Inhibitory Effect ◽

Total Flavonoid ◽

Total Phenolic ◽

Antibacterial Effects ◽

E Coli ◽

Young Fruit ◽

Oroxylum Indicum ◽

Zoonotic Bacteria

Oroxylum indicum extracts from the seeds collected from Lampang and Pattani provinces in Thailand, and young fruits and flowers exhibited in vitro display antioxidant and antibacterial activities against clinically isolated zoonotic bacteria including Staphylococcus intermedius, Streptococcus suis, Pseudomonas aeruginosa, β-hemolytic Escherichia coli and Staphylococcus aureus. The orange crystals and yellow precipitates were obtained from the preparation processes of the seed extracts. The orange-red crystals from the seeds collected from Lampang province exhibited strong in vitro 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging effects (EC50 value = 25.99 ± 3.30 μg/mL) and antibacterial effects on S. intermedius and β-hemolytic E. coli while the yellow precipitate from the same source exhibited only antioxidant activity. Quantitative analysis of phytochemicals in O. indicum samples by spectrophotometric and HPLC techniques showed that they contained different amounts of total phenolic, total flavonoid and three major flavones; baicalin, baicalein and chrysin contents. Young fruit extract, which contained low amounts of flavone contents, still promoted antibacterial effects against the tested bacteria with IC50 values lower than 1 mg/mL and MIC values between 4 to 10 mg/mL in S. intermedius, S. aureus and S suis while higher IC50 and MIC values against P. aeruginosa and β-hemolytic E. coli were found. From scanning electron microscopy, the extract of the young fruit of O. indicum promoted morphological changes in the bacterial cells by disrupting the bacterial cell walls, inducing leakage of the cellular content, and generating the abnormal accumulation of cells. The mechanism of action of the extract for this antibacterial effect may be the disruption of the cell membrane and abnormal cell aggregations. Regression analysis of the results suggests the correlation between total phenolic and total flavonoid contents and antioxidant and antibacterial effects. Baicalin was found to have a high correlation with an inhibitory effect against β-hemolytic E. coli while three unidentified peaks, which could be flavones, showed high correlations with an inhibitory effect against S. intermedius, S. suis, P. aeruginosa and S. aureus.

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Protective effects of carbonic anhydrase inhibition in brain ischaemia in vitro and in vivo models

Journal of Enzyme Inhibition and Medicinal Chemistry ◽

10.1080/14756366.2021.1907575 ◽

2021 ◽

Vol 36 (1) ◽

pp. 964-976

Author(s):

Ilaria Dettori ◽

Irene Fusco ◽

Irene Bulli ◽

Lisa Gaviano ◽

Elisabetta Coppi ◽

...

Keyword(s):

Carbonic Anhydrase ◽

Protective Effects ◽

Brain Ischaemia ◽

In Vivo Models ◽

Carbonic Anhydrase Inhibition

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In Vitro Anti-Biofilm and Antibacterial Properties of Streptococcus downii sp. nov.

Microorganisms ◽

10.3390/microorganisms9020450 ◽

2021 ◽

Vol 9 (2) ◽

pp. 450

Author(s):

Maigualida Cuenca ◽

María Carmen Sánchez ◽

Pedro Diz ◽

Lucía Martínez-Lamas ◽

Maximiliano Álvarez ◽

...

Keyword(s):

Antibacterial Activity ◽

Quantitative Polymerase Chain Reaction ◽

Bacterial Load ◽

Antibacterial Properties ◽

Antibacterial Activities ◽

Oral Bacteria ◽

Periodontal Pathogens ◽

Biofilm Model ◽

Biofilm Development

The aim of this study was to evaluate the potential anti-biofilm and antibacterial activities of Streptococcus downii sp. nov. To test anti-biofilm properties, Streptococcus mutans, Actinomyces naeslundii, Veillonella parvula, Fusobacterium nucleatum, Porphyromonas gingivalis, and Aggregatibacter actinomycetemcomitans were grown in a biofilm model in the presence or not of S. downii sp. nov. for up to 120 h. For the potential antibacterial activity, 24 h-biofilms were exposed to S. downii sp. nov for 24 and 48 h. Biofilms structures and bacterial viability were studied by microscopy, and the effect in bacterial load by quantitative polymerase chain reaction. A generalized linear model was constructed, and results were considered as statistically significant at p < 0.05. The presence of S. downii sp. nov. during biofilm development did not affect the structure of the community, but an anti-biofilm effect against S. mutans was observed (p < 0.001, after 96 and 120 h). For antibacterial activity, after 24 h of exposure to S. downii sp. nov., counts of S. mutans (p = 0.019) and A. actinomycetemcomitans (p = 0.020) were significantly reduced in well-structured biofilms. Although moderate, anti-biofilm and antibacterial activities of S. downii sp. nov. against oral bacteria, including some periodontal pathogens, were demonstrated in an in vitro biofilm model.

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In VitroActivities of Daptomycin-, Vancomycin-, and Teicoplanin-Loaded Polymethylmethacrylate against Methicillin-Susceptible, Methicillin-Resistant, and Vancomycin-Intermediate Strains of Staphylococcus aureus

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.05312-11 ◽

2011 ◽

Vol 55 (12) ◽

pp. 5480-5484 ◽

Cited By ~ 45

Author(s):

Yuhan Chang ◽

Wen-Chien Chen ◽

Pang-Hsin Hsieh ◽

Dave W. Chen ◽

Mel S. Lee ◽

...

Keyword(s):

Staphylococcus Aureus ◽

High Performance ◽

Low Dose ◽

Antibacterial Activities ◽

High Dose ◽

Bone Cements ◽

Antibacterial Effects ◽

Methicillin Resistant ◽

Content Type

ABSTRACTThe objective of this study was to evaluate the antibacterial effects of polymethylmethacrylate (PMMA) bone cements loaded with daptomycin, vancomycin, and teicoplanin against methicillin-susceptibleStaphylococcus aureus(MSSA), methicillin-resistantStaphylococcus aureus(MRSA), and vancomycin-intermediateStaphylococcus aureus(VISA) strains. Standardized cement specimens made from 40 g PMMA loaded with 1 g (low-dose), 4 g (middle-dose) or 8 g (high-dose) antibiotics were tested for elution characteristics and antibacterial activities. The patterns of release of antibiotics from the cement specimens were evaluated usingin vitrobroth elution assay with high-performance liquid chromatography. The activities of broth elution fluid against differentStaphylococcus aureusstrains (MSSA, MRSA, and VISA) were then determined. The antibacterial activities of all the tested antibiotics were maintained after being mixed with PMMA. The cements loaded with higher dosages of antibiotics showed longer elution periods. Regardless of the antibiotic loading dose, the teicoplanin-loaded cements showed better elution efficacy and provided longer inhibitory periods against MSSA, MRSA, and VISA than cements loaded with the same dose of vancomycin or daptomycin. Regarding the choice of antibiotics for cement loading in the treatment ofStaphylococcus aureusinfection, teicoplanin was superior in terms of antibacterial effects.

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Chemical Composition, in vitro Cytotoxic, and Antibacterial Activities of Moroccan Medicinal Plants Euphorbia resinifera and Marrubium vulgare

Biointerface Research in Applied Chemistry ◽

10.33263/briac106.73437355 ◽

2020 ◽

Vol 10 (6) ◽

pp. 7343-7355

Keyword(s):

Medicinal Plants ◽

Solid Medium ◽

Chemical Compounds ◽

Antibacterial Activities ◽

Antibacterial Effects ◽

Animal Cells ◽

Aerial Parts ◽

Marrubium Vulgare ◽

Major Chemical

The purpose of our study was to bring elements of knowledge on the anticancer and antibacterial effects of two plants, widely used in Moroccan traditional pharmacopeia. These plants are: Marrubium vulgare and Euphorbia resinifera. The aerial parts of each plant were extracted successively with Hexane, Dichloromethane, and finally with methanol. The MTT-based method was applied to evaluate the cytotoxicity of the cancer cells: animal cells BSR and Vero and human cell RD. We evidenced an anticancer activity of the extract of the Marrubium vulgare and the dichloromethane extract of Euphorbia resinifera against the studied cells. The antibacterial activity was evaluated for three species of Rhodococcus: Rhodococcus equi, and strains GK1, GK3, grown in a liquid medium, or this medium solidified with agar. In the last test, the method is based on substance diffusion from well throughout the solid medium. The obtained profiles showed that the growth of bacteria is strongly inhibited by the extracts of Marrubium vulgare. However, the extracts of Euphorbia resinifera had no significant effect on bacterial growth. The chemical analysis of the raw extracts of Marrubium vulgare and Euphorbia resinifera by GC-MS analysis showed the presence of several major chemical compounds, mainly: octadecane, 2,6,10,15-tetramethylheptadecane, 2,6,10-trimethyltetradecane, linoleic acid, and deisopropylatrazine. Our observations an encouraging for deepening the studies of the extracts, in order to target better the active molecules, isolate them and to determine their mechanisms of action. The suggested studies would result in the much better valorization of these two medicinal plants.

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Preparation and in vitro osteogenic, angiogenic and antibacterial properties of cuprorivaite (CaCuSi4O10, Cup) bioceramics

RSC Advances ◽

10.1039/c6ra08145b ◽

2016 ◽

Vol 6 (51) ◽

pp. 45840-45849 ◽

Cited By ~ 25

Author(s):

Tian Tian ◽

Chengtie Wu ◽

Jiang Chang

Keyword(s):

Wound Healing ◽

Sol Gel ◽

Antibacterial Properties ◽

Antibacterial Activities ◽

Gel Method ◽

Sol Gel Method

Cuprorivaite firstly synthesized by sol–gel method with angiogenic and antibacterial activities for wound healing application.

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Antibacterial Effects of Levofloxacin, Erythromycin, and Rifampin in a Human Monocyte System againstLegionella pneumophila

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.42.12.3153 ◽

1998 ◽

Vol 42 (12) ◽

pp. 3153-3156 ◽

Cited By ~ 33

Author(s):

Aldona L. Baltch ◽

Raymond P. Smith ◽

Mary A. Franke ◽

Phyllis B. Michelsen

Keyword(s):

Antibacterial Activity ◽

Legionella Pneumophila ◽

Human Monocyte ◽

Antibacterial Activities ◽

Human Monocytes ◽

Antibacterial Effects ◽

In Vitro System ◽

Time Period ◽

Time Periods

ABSTRACT The antibacterial activities of levofloxacin, erythromycin, and rifampin against intracellular Legionella pneumophilaL-1033, serogroup 1, were studied. In an in vitro system utilizing adherent human monocytes, L. pneumophila L-1033, a phagocytosis time period of 1 h, and antibiotic (levofloxacin, erythromycin, and/or rifampin) at 1 to 10 times the MIC, the CFU/ml values for the monocyte lysate were determined during 0- to 4-day time periods. The decrease in CFU/ml with levofloxacin at pH 7.4 was rapid, occurring within 24 h, and was drug concentration dependent (P < 0.01). The decrease in CFU with rifampin was first observed at 48 h (P < 0.01), while only a minimal decrease in CFU/ml was observed with erythromycin. Combination of levofloxacin and rifampin and of levofloxacin and erythromycin at ten times their MICs significantly decreased the CFU/ml value (P < 0.01), to the value attained by levofloxacin alone, while combination of rifampin and erythromycin did not. Removal of levofloxacin after 24 h of incubation resulted in regrowth ofL. pneumophila L-1033, while a continued slow decrease in CFU/ml was seen following rifampin removal; CFU/ml values were unaffected by the removal of erythromycin. At 4 days, and even in assays performed following antibiotic removal, the CFU/ml value continued to be lower in the levofloxacin and rifampin assays than in the assays with erythromycin. Levofloxacin had a significantly higher bactericidal activity against L. pneumophila L-1033 than erythromycin or rifampin. In these assays, the addition of erythromycin or rifampin did not affect the antibacterial activity of levofloxacin.

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