scholarly journals Chemical, spectroscopic characterization, molecular modeling and antibacterial activity assays of a silver (I) complex with succinic acid

2021 ◽  
Vol 46 (2) ◽  
pp. 26-35
Author(s):  
José Alberto Paris Junior ◽  
Ana Júlia Salvador Rocchi ◽  
Bruno Torquato Biagioni ◽  
Maurício Cavicchioli ◽  
Rachel Temperani Amaral Machado ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Succinic Acid ◽  
Density Functional ◽  
Minimum Energy ◽  
Chemical Characterization ◽  
Spectroscopic Characterization ◽  
Bacterial Strains ◽  
Bidentate Coordination ◽  
Carboxylate Groups

A silver(I) complex with succinic acid in the form of succinate is presented. Chemical characterization confirms the molecular composition Ag2C4H4O4 for the complex. Infrared spectra suggest a bidentate coordination of both carboxylate groups of succinates to the two Ag(I) ions. Density functional theory (DFT) studies were used in the structures of succinic acid and Ag(I) succinate complex with coordination formula [Ag2(C4H4O4)] in order to optimize them to their minimum energy. The studies confirmed that each carboxylate group of the succinate anion is coordinated to one silver atom by the two oxygen in a bidentate mode and the bond lengths O···Ag theoretically determined range from 2.325 to 2.338 Å. The complex [Ag2(C4H4O4)] showed in vitro antibacterial activity against the bacterial strains of Staphylococcus aureus, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa complex. Anti-Mycobacterium tuberculosis analyses were also performed and the [Ag2(C4H4O4)] complex was shown to be active over M. tuberculosis H37Rv strain with MIC90 of 23.94 μg mL-1 while succinic acid itself showed a value higher than 25.00 μg mL-1.

scholarly journals Preliminary Investigation of the Antibacterial Activity of Antitumor Drug 3-Amino-1,2,4-Benzotriazine-1,4-Dioxide (Tirapazamine) and its Derivatives

2020 ◽  
Vol 10 (12) ◽  
pp. 4062 ◽  
Author(s):  
Evelina Polmickaitė-Smirnova ◽  
Jonas Šarlauskas ◽  
Kastis Krikštopaitis ◽  
Živilė Lukšienė ◽  
Zita Staniulytė ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Density Functional ◽  
Preliminary Investigation ◽  
Structural Features ◽  
Antitumor Drug ◽  
Additive Effects ◽  
Bacterial Strains ◽  
Functional Theory ◽  
Inhibitory Activities

The antitumor drug 3-amino-1,2,4-benzotriazine-1,4-dioxide (tirapazamine, TPZ (1)) along with a number of newly synthesized tirapazamine derivatives (TPZs) bearing substitutions at the 3-amine position of TPZ (1) were estimated for their antibacterial activity against representative Gram-negative Escherichia coli (ATCC 25922) and Salmonella enterica (SL 5676), as well as Gram-positive Staphylococcus aureus (ATCC 25923) bacterial strains. Their activities in terms of minimum inhibitory concentrations (MICs) varied in the range of 1.1 µM (0.25 µg/mL)–413 µM (128 µg/mL). Amongst the most potent derivatives (1–6), acetyl- and methoxycarbonyl-substituted TPZs (2 and 4) were the strongest agents, which exhibited approximately 4–30 fold greater activities compared to those of TPZ (1) along with the reference drugs chloramphenicol (CAM) and nitrofurantoin (NFT). The inhibitory activities of the compounds were highly impacted by their structural features. No reliable relationships were established between activities and the electron-accepting potencies of the whole set of studied compounds, while the activities of TPZ drug (1) and the structurally uniform set of molecules (2–6) were found to increase with an increase in their electron-accepting potencies obtained by means of density functional theory (DFT) computation. A greater steric, lipophilic and polar nature of the substituents led to a lower activity of the compounds. The combined antibacterial in vitro trial gave clear evidence that TPZs coupled with the commonly utilized antibiotics ciprofloxacin (Cipro) and nitrofurantoin (NFT) could generate enhanced (suggestive of partial and virtually complete synergistic) and additive effects. The strongest effects were defined for TPZs–NFT combinations, which resulted in a notable reduction in the MICs of di-N-oxides. These preliminary findings suggest that the synthesized novel di-N-oxides might be used as sole agents or applied as antibiotic complements.

Synthesis, Molecular Modelling and Antibacterial Activity Against Helicobacter pylori of Novel Diflunisal Derivatives as Urease Enzyme Inhibitors

2019 ◽  
Vol 16 (4) ◽  
pp. 392-400 ◽  
Author(s):  
Göknil Pelin Coşkun ◽  
Teodora Djikic ◽  
Sadık Kalaycı ◽  
Kemal Yelekçi ◽  
Fikrettin Şahin ◽  
...  
Keyword(s):  
Helicobacter Pylori ◽  
Antibacterial Activity ◽  
Enzyme Inhibitors ◽  
Binding Modes ◽  
Bacterial Strains ◽  
Urease Enzyme ◽  
H Pylori ◽  
Ulcer Treatment ◽  
Main Factor

Background:The main factor for the prolongation of the ulcer treatment in the gastrointestinal system would be Helicobacter pylori infection, which can possibly lead to gastrointestinal cancer. Triple therapy is the treatment of choice by today's standards. However, observed resistance among the bacterial strains can make the situation even worse. Therefore, there is a need to discover new targeted antibacterial therapy in order to make success in the eradication of H. pylori infections.Methods:The targeted therapy rule is to identify the related macromolecules that are responsible for the survival of the bacteria. Thus, 2-[(2',4'-difluoro-4-hydroxybiphenyl-3-yl)carbonyl]-N- (substituted)hydrazinocarbothioamide (3-13) and 5-(2',4'-difluoro-4-hydroxybiphenyl-3-yl)-4- (substituted)-2,4-dihydro-3H-1,2,4-triazole-3-thiones (14-17) were synthesized and evaluated for antibacterial activity in vitro against H. pylori.Results:All of the tested compounds showed remarkable antibacterial activity compared to the standard drugs (Ornidazole, Metronidazole, Nitrimidazin and Clarithromycin). Compounds 4 and 13 showed activity as 2µg/ml MIC value.Conclusion:In addition, we have investigated binding modes and energy of the compounds 4 and 13 on urease enzyme active by using the molecular docking tools.

scholarly journals Antimicrobial Activity and Chemical Characterization of a Non-Polar Extract of Saffron Stamens in Food Matrix

Foods ◽  
2021 ◽  
Vol 10 (4) ◽  
pp. 703
Author(s):  
Severino Zara ◽  
Giacomo L. Petretto ◽  
Alberto Mannu ◽  
Giacomo Zara ◽  
Marilena Budroni ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Fatty Acid Content ◽  
Chemical Characterization ◽  
Antimicrobial Activities ◽  
Added Value ◽  
Gas Chromatography Mass Spectrometry ◽  
Food Matrix ◽  
Bacterial Strains ◽  
By Products

The production of saffron spice generates large quantities of plant by-products: over 90% of the plant material collected is discarded, and a consideration fraction of this waste is plant stamens. This work investigated the chemical composition and the antimicrobial activities of the non-polar fraction extracted from four different saffron flower stamens. The chemical composition of ethereal extracts of the saffron stamens was qualitatively assessed by means of gas–chromatography-mass spectrometry (GC-MS) and nuclear magnetic resonance (NMR) analyses. These analyses revealed ethereal extracts to possess a high polyunsaturated fatty acid content. In vitro antibacterial activity of stamen extracts showed no large differences between Gram-positive and Gram-negative bacteria in terms of minimal inhibitory concentration (MIC). In food matrix microbial analysis of the bacterial strains belonging to the main foodborne pathogen species, including Staphylococcus aureus DSM 20231, Escherichia coli DSM 30083, and Listeria monocytogenes DSM 20600, using low-fat UHT milk, revealed a statistically significant reduction in the number of cells (particularly for E. coli and S. aureus with a complete elimination of the population of the two target bacteria following incubation in diethyl ether extracts of saffron stamen (DES) at high concentrations tested, both at 37 °C and 6 °C (for 48 h and 7 days, respectively). A synergic effect was observed when the pathogens were incubated at 6 °C with DES. This work shows these by-products to be excellent sources of bioactive compounds, which could be exploited in high-added-value products, such as food, cosmetics, and drugs.

scholarly journals Effect of Gold Nanoparticles and Silicon on the Bioactivity and Antibacterial Properties of Hydroxyapatite/Chitosan/Tricalcium Phosphate-Based Biomicroconcretes

Materials ◽  
2021 ◽  
Vol 14 (14) ◽  
pp. 3854
Author(s):  
Joanna Czechowska ◽  
Ewelina Cichoń ◽  
Anna Belcarz ◽  
Anna Ślósarczyk ◽  
Aneta Zima
Keyword(s):  
Gold Nanoparticles ◽  
Antibacterial Activity ◽  
Tricalcium Phosphate ◽  
Setting Time ◽  
Antibacterial Properties ◽  
Bone Substitutes ◽  
Bacterial Strains ◽  
Setting Times ◽  
Biological Studies

Bioactive, chemically bonded bone substitutes with antibacterial properties are highly recommended for medical applications. In this study, biomicroconcretes, composed of silicon modified (Si-αTCP) or non-modified α-tricalcium phosphate (αTCP), as well as hybrid hydroxyapatite/chitosan granules non-modified and modified with gold nanoparticles (AuNPs), were designed. The developed biomicroconcretes were supposed to combine the dual functions of antibacterial activity and bone defect repair. The chemical and phase composition, microstructure, setting times, mechanical strength, and in vitro bioactive potential of the composites were examined. Furthermore, on the basis of the American Association of Textile Chemists and Colorists test (AATCC 100), adapted for chemically bonded materials, the antibacterial activity of the biomicroconcretes against S. epidermidis, E. coli, and S. aureus was evaluated. All biomicroconcretes were surgically handy and revealed good adhesion between the hybrid granules and calcium phosphate-based matrix. Furthermore, they possessed acceptable setting times and mechanical properties. It has been stated that materials containing AuNPs set faster and possess a slightly higher compressive strength (3.4 ± 0.7 MPa). The modification of αTCP with silicon led to a favorable decrease of the final setting time to 10 min. Furthermore, it has been shown that materials modified with AuNPs and silicon possessed an enhanced bioactivity. The antibacterial properties of all of the developed biomicroconcretes against the tested bacterial strains due to the presence of both chitosan and Au were confirmed. The material modified simultaneously with AuNPs and silicon seems to be the most promising candidate for further biological studies.

scholarly journals The Design, Characterization and Antibacterial Activity of Heat and Silver Crosslinked Poly(Vinyl Alcohol) Hydrogel Forming Dressings Containing Silver Nanoparticles

Nanomaterials ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 96
Author(s):  
John Jackson ◽  
Helen Burt ◽  
Dirk Lange ◽  
In Whang ◽  
Robin Evans ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Antibacterial Activity ◽  
Silver Nitrate ◽  
Vinyl Alcohol ◽  
Unmet Need ◽  
Chemical Characterization ◽  
Wound Dressings ◽  
Poly Vinyl Alcohol ◽  
Burn Wound

The prompt treatment of burn wounds is essential but can be challenging in remote parts of Africa, where burns from open fires are a constant hazard for children and suitable medical care may be far away. Consequently, there is an unmet need for an economical burn wound dressing with a sustained antimicrobial activity that might be manufactured locally at low cost. This study describes and characterizes the novel preparation of a silver nitrate-loaded/poly(vinyl alcohol) (PVA) film. Using controlled heating cycles, films may be crosslinked with in situ silver nanoparticle production using only a low heat oven and little technical expertise. Our research demonstrated that heat-curing of PVA/silver nitrate films converted the silver to nanoparticles. These films swelled in water to form a robust, wound-compatible hydrogel which exhibited controlled release of the antibacterial silver nanoparticles. An optimal formulation was obtained using 5% (w/w) silver nitrate in PVA membrane films that had been heated at 140 °C for 90 min. Physical and chemical characterization of such films was complemented by in vitro studies that confirmed the effective antibacterial activity of the released silver nanoparticles against both gram positive and negative bacteria. Overall, these findings provide economical and simple methods to manufacture stable, hydrogel forming wound dressings that release antibiotic silver over prolonged periods suitable for emergency use in remote locations.

scholarly journals Production of a New Thiopeptide Antibiotic, TP-1161, by a Marine Nocardiopsis Species

2010 ◽  
Vol 76 (15) ◽  
pp. 4969-4976 ◽  
Author(s):  
Kerstin Engelhardt ◽  
Kristin F. Degnes ◽  
Michael Kemmler ◽  
Harald Bredholt ◽  
Espen Fj�rvik ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Molecular Taxonomy ◽  
Multidrug Resistant ◽  
Peptide Antibiotic ◽  
Indicator Organisms ◽  
Bacterial Strains ◽  
Pcr Screening ◽  
Vancomycin Resistant ◽  
Antibacterial And Antifungal

ABSTRACT Twenty-seven marine sediment- and sponge-derived actinomycetes with a preference for or dependence on seawater for growth were classified at the genus level using molecular taxonomy. Their potential to produce bioactive secondary metabolites was analyzed by PCR screening for genes involved in polyketide and nonribosomal peptide antibiotic synthesis. Using microwell cultures, conditions for the production of antibacterial and antifungal compounds were identified for 15 of the 27 isolates subjected to this screening. Nine of the 15 active extracts were also active against multiresistant Gram-positive bacterial and/or fungal indicator organisms, including vancomycin-resistant Enterococcus faecium and multidrug-resistant Candida albicans. Activity-guided fractionation of fermentation extracts of isolate TFS65-07, showing strong antibacterial activity and classified as a Nocardiopsis species, allowed the identification and purification of the active compound. Structure elucidation revealed this compound to be a new thiopeptide antibiotic with a rare aminoacetone moiety. The in vitro antibacterial activity of this thiopeptide, designated TP-1161, against a panel of bacterial strains was determined.

Synthesis and Antibacterial Activities of Amidine Substituted Monocyclic β-Lactams

2021 ◽  
Vol 17 ◽  
Author(s):  
Lijuan Zhai ◽  
Lili He ◽  
Yuanbai Liu ◽  
Ko Ko Myo ◽  
Zafar Iqbal ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Bacterial Species ◽  
Antimicrobial Effect ◽  
Antibacterial Activities ◽  
Lead Target ◽  
Bacterial Strains ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Clinical Interest

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.

Phytochemical Screening, Antibacterial and Synergistic activity of Dittrichia Viscosa Extracts against Multi-Resistant Pathogenic Bacteria

2019 ◽  
Vol 2 (1) ◽  
pp. 01-06
Author(s):  
Rhazi Fouzia
Keyword(s):  
Antibacterial Activity ◽  
Pathogenic Bacteria ◽  
Antibacterial Effect ◽  
Synergistic Activity ◽  
Phytochemical Screening ◽  
Bacterial Strains ◽  
Dittrichia Viscosa ◽  
Study Results ◽  
Ethanolic Extracts

Study contextual: Faced with the global problem of antimicrobial resistance, and the use of traditional medicine for the research of antibacterial biomolecules. Aim: our work focused on the valorization of a medicinal plant Dittrichia viscosa which has many therapeutic and culinary virtues worldwide. Methods: To do this, a phytochemical screening of the leafy stems of the plant is carried out according to a set of physicochemical reactions, as well as an in vitro evaluation of the antibacterial activity, of the aqueous and ethanolic extracts against multi-resistant bacterial strains, by microdilution technique on microplates. An evaluation of the synergistic interaction between extracts and weakened antibiotics against pathogenic bacteria was also highlighted in this study. Results: The tests revealed the richness of Dittrichia viscosa species by tannins, flavonoids, saponosides, sterols and triterpenes. As for the antibacterial effect, the MICs range from 0.858±0.29 to 66.66 ± 0.00 mg / ml and the MBCs from 4.300 ± 1.01 to 11.610 ± 2.31 mg / ml is an interesting antibacterial activity. Regarding the combination of extracts with antibiotics tested, it revealed a synergistic action inducing an amplification of the antibacterial power of Penicillin, Imipenem and Erythromycin with a rate that reaches 471%. Conclusion: The results of this study show that the aqueous and ethanolic extracts of Dittrichia viscosa have interesting and promising antibacterial activity in the pharmaceutical, food and cosmetic industries.

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